International Union of Pharmacology. XII. Classification of opioid receptors

Pharmacological Reviews

Volumn 48, Issue 4, 1996, Pages 567-592

  Dhawan, B N ^a   Cesselin, F ^b   Raghubir, R ^a   Reisine, T ^c   Bradley, P B ^d   Portoghese, P S ^e   Hamon, M ^b  

^a CENTRAL DRUG RESEARCH INSTITUTE   (India)

^b PITIÉ SALPÊTRIÈRE HOSPITAL   (France)

^c UNIVERSITY OF PENNSYLVANIA   (United States)

^d UNIVERSITY OF BIRMINGHAM   (United Kingdom)

^e UNIVERSITY OF MINNESOTA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINO N [2 (3 HYDROXY 1 PYRROLIDINYL) 1 PHENYLETHYL] N METHYLPHENYLACETAMIDE; 3 [1 (3,4 DICHLORO N METHYLPHENYLACETAMIDO) 2 (1 PYRROLIDINYL)ETHYL]PHENOXYACETIC ACID; 3,4 DICHLORO N [1 ISOPROPYL 2 (1 PYRROLIDINYL)ETHYL] N METHYLBENZENEACETAMIDE; 3,4 DICHLORO N METHYL N [1 PHENYL 2 (1 PYRROLIDINYL)ETHYL]BENZENEACETAMIDE; 3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE; 4 [(3,4 DICHLOROPHENYL)ACETYL] 3 (1 PYRROLIDINYLMETHYL) 1 PIPERAZINECARBOXYLIC ACID METHYL ESTER; 4 [ALPHA (4 ALLYL 2,5 DIMETHYL 1 PIPERAZINYL) 3 HYDROXYBENZYL] N,N DIETHYLBENZAMIDE; ASIMADOLINE; DELTA OPIATE RECEPTOR; DELTA OPIATE RECEPTOR AGONIST; DELTA OPIATE RECEPTOR ANTAGONIST; DELTAKEPHALIN; DELTORPHIN; DIAMORPHINE; DYNORPHIN A [1-8][1 (N METHYLTYROSINE) 7 (N METHYLARGININE) 8 DEXTRO LEUCINE N ETHYLAMIDE]; ENADOLINE; ENKEPHALIN DERIVATIVE; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; ENKEPHALIN[2 DEXTRO PENICILLAMINE 5 PENICILLAMINE]; ENKEPHALIN[2,5 DEXTRO PENICILLAMINE]; GUANINE NUCLEOTIDE BINDING PROTEIN; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR AGONIST; KAPPA OPIATE RECEPTOR ANTAGONIST; KETAZOCINE; LEUCINE ENKEPHALIN[2 DEXTRO SERINE 6 THREONINE]; MORPHINE; MU OPIATE RECEPTOR; MU OPIATE RECEPTOR AGONIST; MU OPIATE RECEPTOR ANTAGONIST; N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZO[B]THIOPHENE 4 ACETAMIDE; N METHYL N [7 (1 PYRROLIDINYL) 1 OXASPIRO[4.5]DEC 8 YL]BENZENEACETAMIDE; N,N DIALLYLTYROSYL 2 METHYLALANYL 2 METHYLALANYLPHENYLALANYLLEUCINE; N,N DIALLYLTYROSYLGLYCYL ALPHA (2 AMINOETHYLTHIO)HYDROCINNAMOYLLEUCINE; NALOXONE; NALTREXONE; NALTRIBEN; NALTRINDOLE; OPIATE AGONIST; OPIATE ANTAGONIST; OPIATE RECEPTOR; RECEPTOR SUBTYPE; SPIRADOLINE; UNINDEXED DRUG;

CLASSIFICATION; CLONING; HUMAN; INTERNATIONAL COOPERATION; LIGAND BINDING; MOLECULAR BIOLOGY; NONHUMAN; PRACTICE GUIDELINE; PRIORITY JOURNAL; RECEPTOR BINDING; RECEPTOR DENSITY; RECEPTOR GENE; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; HUMANS; MOLECULAR BIOLOGY; PHARMACOLOGY; RECEPTORS, OPIOID;

EID: 0030472350     PISSN: 00316997     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (337)

1. ABOOD, M. E., NOEL, M. A., FARNWORTH, J. S., AND TAO, Q.: Molecular cloning and expression of a delta opioid receptor from rat brain. J. Neurosci. Res. 37: 714-719, 1994.
2. ADLER, M. W., AND GELLER, E. B.: The opioid system and temperature regulation. Annu. Rev. Pharmacol. Toxicol. 28: 429-449, 1988.
3. 3H][2-D-penicillamine, 5-D-penicillamine]-enkephalin binding to δ opiate receptors in the rat brain and neuroblastoma-glioma hybrid cell line (NG 108-15). Proc. Natl. Acad. Sci. USA 82: 2532-2537, 1985.
4. 2): a potent and fully specific agonist for the δ opioid receptor. Mol. Pharmacol. 35: 774-779, 1989.
5. ARNDT, J. O.: Opiate receptors in the CNS and their possible role in cardiovascular control. In Brain Peptides and Catecholamines in Cardiovascular Regulation, ed. by J. P. Buckley and C. M. Ferrario, pp. 137-151, Raven Press, New York, 1987.
6. ARVIDSSON, U., DADO, R. J., RIEDL, M., LEE, J. H., LAW, P. Y., LOH, H. H., ELDE, R., AND WESSENDORF, M. W.: δ-opioid receptor immunoreactivity: distribution in brain stem and spinal cord, and relationship to biogenic amines and enkephalin. J. Neurosci. 15: 1215-1235, 1995.
7. 3H]etorphine binding in guinea pig striatum after blockade of μ and δ sites. Life Sci. 31: 1287-1290, 1982.
8. BAAMONDE, A., DAUCÉ, V., RUIZ-GAYO, M., FULGA, I. G., TURCAUD, S., FOURNIÉ-ZALUSKI, M. C. AND ROQUES, B. P.: Antidepressant-type effects of endogenous enkephalins protected by systemic RB 101 are mediated by opioid delta and dopamine D1 receptor stimulation. Eur. J. Pharmacol. 216: 157-166, 1992.
9. BARBER, A., BARTOSZYK, G. D., BENDER, H. M., GOTTSCHLICH, R., GREINER, H. E., HARTING, J., MAULER, F., MINCK, K. O., MURRAY, R. D., AND SEYFRIED, C. A.: A pharmacological profile of the novel, peripherally-selective κ-opioid receptor agonist, EMD 61753. Br. J. Pharmacol. 113: 1317-1327, 1994a.
10. BARBER, A., BARTOSZYK, G. D., GREINER, H. E., MAULER, F., MURRAY, R. D., SEYFRIED, C. A., SIMON, M., BOTTSCHLICH, R., HARTING, J., AND LUES, I.: Central and peripheral actions of the novel κ-opioid receptor agonist, EMD 60400. Br. J. Pharmacol. 111: 843-851, 1994b.
11. BARE, L. A., MANSSON, E., AND YANG, D. M.: Expression of two variants of the human mu opioid receptor mRNA in SK-N-SH cells and human brain. FEBS Lett. 384: 213-216, 1994.
12. BAUSCH, S. S., PATTERSON, T. A., APLLEYARD, S. M., AND CHAVKIN, C.: Immunocytochemical localization of delta opioid receptor in mouse brain. J. Chem. Neuroanat. 8: 175-189, 1995.
13. BECKETT, A. H., AND CASY, A. F.: Synthetic analgesics: stereochemical considerations. J. Pharm. Pharmacol. 6: 986-1001, 1954.
14. BEFORT, K., MATTEI, M. G., ROECKEL, N., AND KIEFFER, B.: Chromosomal localization of the delta opioid receptor gene to human 1p 34,3- p36.1 and mouse 4D bands by in situ hybridization. Genomics 20: 143-145, 1994.
15. BELL, G., AND REISINE, T.: Molecular Biology of somatostatin receptors, Trends Neurosci. 16: 34-38, 1993.
16. BESSE, D., LOMBARD, M. C., ZAJAC, J. M., ROQUES, B. P., AND BESSON, J. M.: Pre- and postsynaptic distribution of mu, delta and kappa opioid receptors in the superficial layers of the dorsal horn of the rat spinal cord. Brain Res. 521: 15-22, 1990.
17. BILSKY, E. J., CALDERON, S. N., WANG, T., BERNSTEIN, R. N., DAVIS, P., HRUBY, V. J., MCNUTT, R. W., ROTHMAN, R. B., RICE, K. C., AND PORRECA, F.: SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist. J. Pharmacol. Exp. Ther. 273: 359-366, 1995.
18. BIRCH, P. J., HAYES, A. G., SHEEHAN, M. J., AND TYERS, M. B.: Nor-binaltorphimine: antagonistic profile at κ opioid receptors. Eur. J. Pharmacol. 144: 405-408, 1987.
19. 3H]-PL17. Mol. Pharmacol. 31: 326-333, 1987.
20. BOT, G., CHAHL, L. A., BRENT, P. J., AND JOHNSTON, P. A.: Effects of intracerebroventricularly administered mu., delta- and kappa-opioid agonists on locomotor activity of the guinea pig and the pharmacology of the locomotor response to U50,488H. Neuropharmacology 31: 825-833, 1992.
21. BOUHGOIN, S., BENOLIEL, J. J., COLLIN, E., MAUBORGNE, A., POHL, M., HAMON, M., AND CESSELIN, F.: Opioidergic control of the spinal release of neuropeptides: possible significance for the analgesic effects of opioids. Fundam. Clin. Pharmacol. 8: 307-321, 1994.
22. 6]enkephalin: covalent attachment via thiol-disulfide exchange. J. Biol. Chem. 262: 13434-13439, 1987.
23. 3H]-CI-977: a highly selective ligand for the κ-opioid receptor in both guinea-pig and rat forebrain. Mol. Neuropharmacol. 1: 23-29, 1990.
24. BRADBURY, A. F., SMYTH, D. G., SNELL, C. R., BIRDSALL, N. J. M., AND HULME, E. C.: C-fragment of lipoprotein has a high affinity for brain opiate receptors. Nature (Lond.) 260: 793-795, 1976.
25. 2]deltorphin II, in the rat. Eur. J. Pharmacol. 218: 69-73, 1992.
26. BROWNSTEIN, M. J.: A brief history of opiates, opioid peptides, and opioid receptors. Proc. Natl. Acad. Sci. USA 90: 5391-5393, 1993.
27. BUNZOW, J. R., GRANDY, D. K., AND KELLY, M.: Cloning, pharmacological characterization and distribution of a rat mu-opioid receptor: GenBank Accession No. U02083, 1993.
28. BUNZOW, J. R., SAEZ, C., MORTRUD, M., BOUVIER, C., WILLIAMS, J. T., Low, M., AND GRANDY, D. K.: Molecular cloning and tissue distribution of a putative member of the rat opioid receptor gene family that is not a μ, δ or κopioid receptor type. FEBS Lett. 347: 284-288, 1994.
29. BURKS, T. F., Fox, D. A., HIRNING, L. D., SHOOK, J. E., AND PORRECA, F.: Regulation of gastrointestinal function by multiple opioid receptors. Life Sci. 43: 2177-2181, 1988.
30. BUTELMAN, E. R., FRANCE, C. P., AND WOODS, J. H.: Apparent pA2 analysis on the respiratory depressant effects of alfentanil, etonitazene, ethylketocyclazocine (EKC) and Mr2033 in rhesus monkeys. J, Pharmacol. Exp. Ther. 264: 145-151, 1993.
31. 3H]deltorphin II. Life Sci. 50: PL75-PL78, 1992.
32. BZDEGA, T., CHIN, H., KIM, H., JUNG, H. H., KOZAK, C. A., AND KLEE W. A.: Regional expression and chromosomal localization of the S opiate receptor gene. Proc. Natl. Acad. Sci. USA 90: 9305-9309, 1993.
33. CHAILLET, P., COULAUD, A., ZAJAC, J. M., FOURNIÉ-ZALUSKI, M. C., COSTENTIN, J., AND ROQUES, B. P.: The μ rather than the δ subtype of opioid receptors appears to be involved in enkephalin induced analgesia. Eur. J. Pharmacol. 101: 83-90, 1984.
34. CHAN, J. S. C., CHIU, T. T., AND WONG, Y. H.: Activation of type II adenylyl cyclase by the cloned μ-opioid receptor: coupling to multiple G proteins. J. Neurochem. 65: 2682-2689, 1995.
35. CHANG, A. C., TAKEMORI, A. E., OJALA, W. H., GLEASON, W. B., PORTOGHESE, P. S.: κ opioid receptor selective affinity labels: electrophilic benzeneacetamides as κ-selective opioid antagoniste. J. Med. Chem. 37: 4490-4498, 1994.
36. 2): a potent and specific agonist for morphine (mu) receptors. Science (Wash. DC) 212: 75-77, 1981.
37. CHANG, K. J., WEI, E. T., KILLIAN, A., AND CHANG, J. K: Potent morphiceptin analogs: structure activity relationships and morphine like activities. J. Pharmacol. Exp. Ther. 227: 403-408, 1983.
38. CHANG, K. J., RIGDON, G. C., HOWARD, J. L., AND MCNUTT, R. W.: A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86. J. Pharmacol. Exp. Ther. 267: 852-857, 1993.
39. CHAVKIN, C., JAMES, I. F., AND GOLDSTEIN, A.: Dynorphin is a specific endogenous ligand of the κopioid receptor. Science (Wash. DC) 215: 413-415, 1982.
40. CHEN, Y., FAN, Y., LIU, L., MESTEK, A., TIAN, M. T., KOZAK, C. A., AND Yu, L.: Molecular cloning, tissue distribution and chromosomal localization of a novel member of the opioid receptor gene family. FEBS Lett. 347: 279-283, 1994.
41. CHEN, Y., MESTEK, A., LIU, J., HURLEY, J. A., AND Yu, L.: Molecular cloning and functional expression of a mu opioid receptor from rat brain. Mol. Pharmacol. 44: 8-12, 1993a.
42. CHEN, Y., MESTEK, A., LIU, J., AND Yu, L.: Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors. Biochem. J. 295: 625-628, 1993b.
43. + channel. J. Biol. Chem. 269: 7839-7842, 1994.
44. CHENG, P. Y., SVINGOS, A. L., WANG, H., CLARKE, C. L., JENAB, S., BECZKOWSKA, I. W., INTURRISI, C. E., AND PICKEL, V. M.: Ultrastructural immunolabeling shows prominent presynaptic vesicular localisation of δ-opioid receptor within both enkephalin- and nonenkephalin-containing axon terminals in the superficial layers of the rat cervical spinal cord. J. Neurosci. 15: 5976-5988, 1995.
45. CHILDERS, S. R.: Opioid receptor-coupled second messengers systems. Life Sci. 48: 1991-2003, 1991.
46. CHIU, T. H., YEH, M. H., TSAI, S. K., AND MOK, M. S.: Electrophysiological actions of alfentanil: intracellular studies in the rat locus coeruleus neurones. Br. J. Pharmacol. 110: 903-909, 1993.
47. CHNEIWEISS, H., GLOWINSKI, J., AND PRÉMONT, J.: Mu and delta opiate receptors coupled negatively to adenylate cyclase on embryonic neurons from mouse striatum in primary culture. J. Neurosci. 8: 3376-3382, 1988.
48. CHO, T. M., HASEGAWA, J., GE, B. L., AND LOH, H. H.: Purification to apparent homogeneity of a mu specific opioid receptor from brain. Proc. Natl. Acad. Sci. USA 83: 4138-4142, 1986.
49. 10]dynorphin A-(1-11) are highly selective for κ-opioid receptors. J. Med. Chem. 35: 4638-4639, 1992.
50. CLARK, C. R., BIRCHMORE, B., SHARIF, N. A., HUNTER, J. C., HILL, R. G., AND HUGHES, J.: PD 117302: a selective agonist for the κ-opioid receptors. Br. J. Pharmacol. 93: 618-626, 1988.
51. CLARK, J. A., LIU, L., PRICE, M., HERSH, B., EDELSON, M., AND PASTERNAK, G. W.: Kappa opiate receptor multiplicity: evidence for two U50,488-sensitive K1 subtypes and a novel k3 subtype. J. Pharmacol. Exp. Ther. 251: 461-468, 1989.
52. COHEN, M. L., SHUMAN, R. T., OSBORNE, J. J., AND GESELLCHEN, P. D.: Opioid agonist activity of ICI 174864 and its carboxypeptidase degradation product, LY281217. J. Pharmacol. Exp. Ther. 238: 769-772, 1986.
53. COMER, S. D., HOENICKE, E. M., SABLE, A. I., MCNUTT, R. W., CHANG, K. J., DE COSTA, B. R., MOSBERG, H. I., AND WOODS, J. H.: Convulsive effects of systemic administration of the delta opioid agonist BW373U86 in mice. J. Pharmacol. Exp. Ther. 267: 888-895, 1993.
54. 3H]naltrindole: a potent and selective ligand for labeling δ-opioid receptors. Brain Res. 604: 160-164, 1993.
55. CORBETT, A. D., PATERSON, S. J., MCKNIGHT, A. T., MAGNAN, J., AND KOSTERLITZ, H. W.: Dynorphin1-8 and dynorphin1-9 are ligands for the κ-subtype of opioid receptor. Nature (Lond.) 299: 79-81, 1982.
56. COSTELLO, G. F., MAIN, B. G., BARLOW, J. J., CARROLL, J. A., AND SHAW, J. S.: A novel series of potent and selective agonists at the opioid kappa-receptor. Eur. J. Pharmacol. 151: 475-478, 1988.
57. COTTON, R., GILES, M. B., MILLER, L., SHAW, J. S., AND TIMMS, D.: ICI 174,864: a highly selective antagonist for the δ opioid receptor. Eur. J. Pharmacol. 97: 331-332, 1984.
58. Cox, B. M., GOLDSTEIN, A., AND LI, C. H.: Opioid activity of a peptide, betaendorphin (61-91), derived from beta-lipotropin. Proc. Natl. Acad. Sci. USA 73: 1821-1823, 1976.
59. CRABTREE, B. L.: Review of naltrexone, a long-acting opiate antagonist. Clin. Pharmacol. 3: 273-280, 1984.
60. GRAIN, S. M., AND SHEN, K. F.: Opioids can evoke direct receptor-mediated excitatory effects on sensory neurons. Trends Pharmacol. Sci. 11: 77-81, 1990.
61. CRUCIANI, R. A., LUTZ, R. A., MUNSON, P. J., AND RODBARD, D.: Naloxonazine effect on the interaction of enkephalin analogs with mu-1, mu-2 and delta opioid binding sites in rat brain membranes. J. Pharmacol. Exp. Ther. 242: 15-20, 1987.
62. DADO, R. J., LAW, P. Y., LOH, H. H., AND ELDE, R.: Immunofluorescent identification of a delta (δ)-opioid receptor on primary afferent nerve terminals. Neuroreport 5: 341-344, 1993.
63. DE COSTA, B. R., BAND, L., ROTHMAN, R. B., JACOBSON, A. E., BYKOV, V., PERT, A., AND RICE, K. C.: Synthesis of an affinity ligand ("UPHIT") for in vivo acylation of the κ-opioid receptor. FEBS Lett. 249: 178-182, 1989.
64. 6 (O-tert-butyl): two new enkephalin analogs with both a good selectivity and a high affinity toward delta-opioid binding sites. J. Biol. Chem. 263: 4124-4130, 1988.
65. 5] enkephalin. FEBS Lett. 183: 439-443, 1985.
66. 3H]DSTBULET, a new highly potent and selective linear enkephalin analogue. Neurochem. Int. 16: 341-368, 1990.
67. DELFS, J., KONG, H., Yu, L., REISINE, T., AND CHESSELET, M. F.: Expression of the mu opioid receptor mRNA in rat brain: an in situ hybridization study at the single cell level. J. Comp. Neurol. 345: 46-68, 1994.
68. DEPAOLI, A. M., HURLEY, K. M., YASADA, K., REISINE, T., AND BELL, G.: Distribution of κ opioid receptor mRNA in adult mouse brain: an in situ hybridization histochemistry study. Mol. Cell. Neurosci. 5: 327-335, 1994.
69. 5] enkephalin in the rat. J. Pharmacol. Exp. Ther. 259: 725-731, 1991.
70. 2]deltorphin-I: a high affinity, delta selective opioid receptor ligand. Peptides 12: 825-830, 1991.
71. EMMERSON, P. J., LIU, M. R., WOODS, J. H., AND MEDZIHRADSKY, F.: Binding affinity and selectivity of opioids at mu, delta and kappa receptors in monkey brain membranes. J. Pharmacol. Exp. Ther. 271: 1630-1637, 1994.
72. ERSPAMER, V., MELCHIORRI, P., FALCONIERI ERSPAMER, G., NEGRI, L., CORSI, R., SEVERINI, C., BARRA, D., SIMMACO, M., AND KREIL, G.: Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for δ opioid binding sites. Proc. Natl. Acad. Sci. USA 86: 5188-5192, 1989.
73. EVANS, C. J., KEITH, D. E., JR., MORRISON, H., MAGENDZO, K., AND EDWARDS, R. H.: Cloning of a delta opioid receptor by functional expression. Science (Wash. DC) 258: 1952-1955, 1992.
74. FANG, F. G., FIELDS, H. L., AND LEE, N. M.: Action at the mu receptor is sufficient to explain the supraspinal effects of opiates. J. Pharmacol. Exp. Ther. 238: 1039-1044, 1986.
75. 3H] naltrindole binding to delta opioid receptors in mouse brain and mouse vas deferens: evidence for delta opioid receptor heterogeneity. J. Pharmacol. Exp. Ther. 268: 836-846, 1994.
76. 4]deltorphin and characterization of its δ opioid receptor binding properties. Life Sci. 51: PL189-PL193, 1992.
77. 3H]carfentanyl binding to mu opiate receptors in rat brain. Synapse 14: 154-159, 1993.
78. FOWLER, C. J., AND FRASER, G. L.: μ-, δ-, κ-opioid receptors and their subtypes. A critical review with emphasis on radioligand binding experiments. Neurochem. Int. 24: 401-426, 1994.
79. FOX-THRELKELD, J. A. E. T., DANIEL, E. E., CHRISTINCK, F., HRUBY, V. J., CIPRIS, S., AND WOSKOWSKA, Z.: Identification of mechanisms and sites of action of mu and delta receptor activation in the canine intestine. J. Pharmacol. Exp. Ther. 268: 689-700, 1994.
80. FRANCE, C. P., AND WOODS, J. H.: Naloxone benzoylhydrazone is a μ-selective opioid antagonist without κ agonist effects in rhesus monkeys. Behav. Pharmacol. 3: 133-141, 1992.
81. FRANCE, C. P., MEDZIHRADSKY, F., AND WOODS, J. H.: Comparison of kappa opioids in rhesus monkeys: behavioral effects and receptor binding affinities. J. Pharmacol. Exp. Ther. 268: 47-58, 1994.
82. FREY, A., AND KEBABIAN, J. W.: μ-opiate receptors in 7315c tumor tissue mediate inhibition of immunoreactive prolactin release and adenylate cyclase activity. Endocrinology 115: 1797-1804, 1984.
83. FREYE, E., SCHNITZLER, M., AND SCHENK, G.: Opioid-induced respiratory depression and analgesia may be mediated by different subreceptors. Pharm. Res. 8: 196-199, 1991.
84. FUKUDA, K., KATO, S., MORI, K., IWABE, N., MIYATA, T., NISHI, M., AND TAKESHIMA, H.: Primary structures and expression from cDNAs of rat opioid receptor delta and mu-subtypes. FEBS Lett. 327: 311-314, 1993.
85. FUKUDA, K., KATO, S., MORI, K., NISHI, M., TAKESHIMA, H., IWABE, N., MIYATA, T., HOUTANI, T., AND SUGIMOTO, T.: cDNA cloning and regional distribution of a novel member of the opioid receptor family. FEBS Lett. 343: 42-46, 1994.
86. GACEL, G., FOURNIÉ-ZALUSKI, M. C., AND ROQUES, B. P.: D-Tyr-Ser-Gly-Phe-Leu-Thr, a highly preferential ligand for delta opiate receptors. FEBS Lett. 118: 245-247, 1980.
87. GACEL, G., ZAJAC, J. M., DELAY-GOYET, P., DAUG., V., AND ROQUES, B. P.: Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. J. Med. Chem. 31: 374-383, 1988.
88. GACEL, G. A., FELLION, E., BAAMONDE, A., DAUG., V., AND ROQUES, B. P.: Synthesis, biochemical and pharmacological properties of BUBUC, a highly selective and systemically active agonist for in vivo studies of delta-opioid receptors. Peptides 11: 983-988, 1990.
89. 10] dynorphin-(1-11) is a higly potent and selective ligand for κ opioid receptors. Eur. J. Pharmacol. 106: 457-458, 1985.
90. GEORGOUSSI, Z., MILLIGAN, G., AND ZIOUDROU, C.: Immunoprecipitation of opioid receptor-Go-protein complexes using specific GTP binding-protein antisera. Biochem. J. 306: 71-76, 1995.
91. GILLAN, M. G. C., KOSTERLITZ, H. W., AND PATERSON, S. J.: Comparison of the binding characteristics of tritiated opiates and opioid peptides. Br. J. Pharmacol. 70: 481-490, 1980.
92. 3H]dynorphin A (1-9) in suspensions of guinea pig brain membranes. J. Neurochem. 45: 1034-1042, 1985.
93. GINTZLER, A. R., AND Xu, H.: Different G proteins mediate the opioid inhibition or enhancement of evoked [5-methionine]-enkephalin release. Proc. Natl. Acad. Sci. USA 88: 4741-4745, 1991.
94. GIROS, B., POHL, M., ROCHELLE, J. M., AND SELDIN, M. F.: Chromosomal localization of opioid peptide and receptor genes in the mouse. Life Sci. 56: PL369-PL375, 1995.
95. GOLDSTEIN, A., FISCHLI, W., LOWNEY, L. I., HUNKAPILLER, M., AND HOOD, L.: Porcine pituitary dynorphin: complete amino acid sequence of the biologically active heptadecapeptide. Proc. Natl. Acad. Sci. USA 78: 7219-7223, 1981.
96. GOLDSTEIN, A., LOWNEY, L. I., AND PAL, B. K.: Stereospecific and nonspecific interactions of the morphine congener levorphanol in subcellular fractions of mouse brain. Proc. Natl. Acad. Sci. USA 68: 1742-1747, 1971.
97. GOLDSTEIN, A., AND NAIDU, A.: Multiple opioid receptors: ligand selectivity profiles and binding site signatures. Mol. Pharmacol. 36: 265-272, 1989.
98. GREVEL, J., Yu, V., AND SADEE, W.: Characterization of a labile naloxone binding site (λ site) in rat brain. J. Neurochem. 44: 1647-1656, 1985.
99. GRUDT, T. J., AND WILLIAMS, J. T.: κ-opioid receptors also increase potassium conductance. Proc. Natl. Acad. Sci. USA 90: 11429-11432, 1993.
100. HADDAD, G. G., SCHAEFFER, J. I., AND CHANG, K. J.: Opposite effects of δ and μ-opioid receptor agonists on ventilation in conscious adult dogs. Brain. Res. 323: 73-82, 1984.
101. HAHN, E. F., AND PASTERNAK, G. W.: Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites. Life Sci. 31: 1385-1388, 1982.
102. HAMON, M.: Mechanisms of opiate-induced immunodepression: current concepts. In. Physiopathology of Illicit Drugs: Cannabis, Cocaine, Opiates, ed. by B. Nahas and C. Latour, Pergamon Press Adv. Biosci. series, vol. 80, pp. 277-283, 1991.
103. HANDA B. K., LAND, A. C., LORD, J. A., MORGAN, B. A., RANGE, M. J., AND SMITH, C. F.: Analogues of beta-LPH61-64 possessing selective agonist activity at mu-opiate receptors. Eur. J. Pharmacol. 70: 531-540, 1981.
104. HANDLER, C. M., GELLER, E. B., AND ADLER, M. W.: Effect of μ-, κ-, and δ-selective opioid agonists on thermoregulation in the rat. Pharmacol. Biochem. Behav. 43: 1209-1216, 1992.
105. HANDLER, C. M., PILIERO, T. C., GELLER, E. B., AND ADLER, M. W.: Effect of ambient temperature on the ability of mu-, kappa- and delta-selective opioid agonists to modulate thermoregulatory mechanisms in the rat. J. Pharmacol. Exp. Ther. 268: 847-855, 1994.
106. HANSEN, P. E., AND MORGAN, B. A.: Structure-activity relationship in enkephalin peptides. In The Peptides, ed. by J. Meienhofer and S. Udenfriend, vol. 6, pp. 269-321, Academic Press, New York, 1984.
107. HASSEN, A. H., FEUERSTEIN, G., AND FADEN, A. I.: Kappa opioid receptors modulate cardiorespiratory function in hindbrain nuclei of rat. J. Neurosci. 4: 2213-2221, 1984a.
108. HASSEN, A. H., FEUERSTEIN, G., AND FADEN, A I.: Selective cadiorespiratory effects mediated by mu opioid receptors in the nucleus ambiguus. Neuropharmacology 23: 407-415, 1984b.
109. 3H] CTOP binding to mu opioid receptors in rat brain. Life Sci. 42: 2541-2551, 1988.
110. 3H]CTOP), a potent and highly selective peptide for mu opioid receptors in rat brain. J. Pharmacol. Exp. Ther. 248: 73-80, 1989.
111. HAYES, A. G., BIRCH, P. J., HAYWARD, N. J., SHEEHAN, M. J., ROGERS, H., TYERS, M. B., JUDD, D. B., SCOPES, D. I. C., AND NAYLOR, A.: A series of novel, highly potent and selective agonists for the κ-opioid receptor. Br. J. Pharmacol. 101: 944-949, 1990.
112. HEYMAN, J. S, VAUGHT, J. L., RAFFA, R. B., AND PORRECA, F.: Can supraspinal delta-opioid receptors mediate antinociception? Trends Pharmacol. Sci. 9: 134-138, 1988.
113. HILLER, J. M., ZHANG, Y., BING, G., GIOANNINI, T. L., STONE, E. A., AND SIMON, E. J.: Immunohistochemical localization of mu-opioid receptors in rat brain using antibodies generated against a peptide sequence present in a purified mu-opioid binding protein. Neuroscience 62: 829-841, 1994.
114. HJORTH, S. A., THIRSTRUP, K., GRANDY, D. K, AND SCHWARTZ, T. W.: Analysis of selective binding epitopes for the κ-opioid receptor antagonist nor-binaltorphimine. Mol. Pharmacol. 47: 1089-1094, 1995.
115. 3-ke opioid receptor on Raji B lymphoma cells (Abstract). Soc. Neurosci. 21: 527, 1995.
116. HONDA, C. N., AND ARVIDSSON, U.: Immunohistochemical localization of delta-and mu-opioid receptors in primate spinal cord. Neuroreport 6: 1025-1028, 1995.
117. HORAN, P., DE COSTA, B. R., RICE, K. C., AND PORRECA, F.: Differential antagonism of U69,593- and bremazocine by (-)-UPHIT: evidence of kappa opioid receptor multiplicity in mice. J. Pharmacol. Exp. Ther. 257: 1154-1161, 1991.
118. HORAN, P., TAYLOR, J., YAMAMURA, H. I., AND PORRECA, F.: Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test. J. Pharmacol. Exp. Ther. 260: 1237-1243, 1992.
119. HORAN, P. J., DE COSTA, B. R., RICE, K., HAASETH, R. C., HRUBY, V. J., AND PORRECA, F.: Differential antagonism of bremazocine- and U69,593-induced antinociception by quadazocine: further functional evidence of opioid κ receptor multiplicity in the mouse. J. Pharmacol. Exp. Ther. 266: 926-933, 1993.
120. HUGHES, J., SMITH, T. W., KOSTERLITZ, H. W., FORTHERGILL, L. A., MORGAN, B. A., AND MORRIS, H. R.: Identification of two related pentapeptides from the brain with potent opiate agonist activity. Nature (Lond.) 258: 577-579, 1975.
121. HUNTER, J. C., LEIGHTON, G. E., MEECHAM, K. G., BOYLE, S. J., HORWELL, D. C., REES, D. C., AND HUGHES, J.: CI-977, a novel and selective agonist for the κ-opioid receptor. Br. J. Pharmacol. 101: 183-189, 1990.
122. HUTCHISON, M., KOSTERLITZ, H. W., LESIE, F. M., WATERFIELD, A. A., AND TERENIUS, L.: Assessment in the guinea pig ileum and mouse vas deferens of benzomorphana, which have antinociceptive activity but do not substitute for morphine in dependent monkey. Br. J. Pharmacol. 55: 541-546, 1975.
123. + channel. Biochem. Biophys. Res. Commun. 208: 302-308, 1995.
124. 2]deltorphin II, a novel and highly selective delta-opioid receptor agonist. Peptides 13: 1123-1126, 1992.
125. ITZHAK, Y.: Multiple opioid binding sites. In The Opiate Receptors, ed. by G. W. Pasternak, pp. 95-142, Humana Press, Clifton, NJ, 1988.
126. JAMES, I. F., AND GOLDSTEIN, A.: Site-directed alkylation of multiple opioid receptors. I. Binding selectivity. Mol. Pharmacol. 25: 337-342, 1984.
127. 2] deltorphin II, a highly selective δ agonist in vivo. Life Sci. 47: PL43-PL47, 1990.
128. JIANG, Q., SEBASTIAN, A., ARCHER, S., AND BIDLACK, J. M.: 5β-methyl-14β-(p-nitrocinnamoylamino)-7,8-dihydromorphinone and its corresponding N-cyclopropylmethyl analog, N-cyclopropylmethylnor-5β-methyl-14β-(p-nitrocinnamoylamino)-7,8- dihydromorphinone: mu-selective irreversible opioid antagonists. J. Pharmacol. Exp. Ther. 268: 1107-1113, 1994.
129. 6]enkephalin and naltrindole 5′-isothiocyanate: evidence for delta-receptor subtypes. J. Pharmacol. Exp. Ther. 257: 1069-1075, 1991.
130. JIN, W., LEE, N. M., LOH, H. H., AND THAYER, S. A.: Opioids mobilize calcium from inositol 1,4,5-trisphosphate-sensitive stores in NG108-15 cells. J. Neurosci. 14: 1920-1929, 1994.
131. JOHNSON, P. S., WANG, J. B., WANG, W. F., AND UHL, G. R.: Expressed mu opiate receptor couples to adenylate cyclase and phosphatidyl turnover. Neuroreport 5: 507-509, 1994.
132. KAKIDANI, H., FURUTANI, Y., TAKAHASHI, H., NODA, M., MORIMOTO, Y., HIROSE, T., ASAI, M., INAYAMA, S., NAKANISHI, S., AND NUMA, S.: Cloning and sequence analysis of cDNA for porcine β-neo-endorphin/dynorphin precursor. Nature (Lond.) 298: 245-249, 1982.
133. 2+ channel inhibition by κ opioid receptors expressed in Xenopus oocytes. Neuroreport 5: 2506-2508, 1994a.
134. 2+ and stimulation of cyclic AMP production by κ opioid receptors in Xenopus oocytes. Mol. Brain Res. 27: 258-264, 1994b.
135. KAUPMAN, D. L., XIA, J. R., KEITH, D. E., JR., NEWMAN, D., EVANS, C. J., AND LUSIS, A. J.: Localization of the delta opioid receptor to mouse chromosome 4 by linkage analysis. Genomics 19: 405-406, 1994.
136. KAZMIERSKI, W., WIRE, W. S., LUI, G. K, KNAPP, R. J., SHOOK, J. E., BURKS, T. F., YAMAMURA, H. I., AND HRUBY, V. J.: Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors. J. Med. Chem. 31: 2170-2177, 1988.
137. KEITH, D. E., JR., ANTON, B., AND EVANS, C. J.: Characterization and mapping of a delta opioid receptor clone from NG108-15 cells. Proc. West. Pharmacol. Soc. 36: 299-306, 1993.
138. KIEFFER, B. L.: Recent advances in molecular recognition and signal transduction of active peptides: receptors for opioid peptides. Cell. Mol. Neurobiol. 15: 615-635, 1995.
139. KIEFFER, B., BEFORT, K., GAVERIAUX-RUFF, C., AND HIRTH, C. G.: The delta opioid receptor: isolation of a cDNA by expression cloning and pharmaco-logical characterization. Proc. Natl. Acad. Sci. USA 89: 12048-12052, 1992.
140. KNAPP, R. J., MALATYNSKA, E., FANG, L., LI, X., BABIN, E., NGUYEN, M., SANTORO, G., VARGA, E. V., HRUBY, V. J., ROESKE, W. R., AND YAMAMURA, H.I. Intification of a human delta opioid receptor: cloning and expression. Life Sci. 54: PL463-PL469, 1994.
141. KNAPP, R. J., PORRECA, F., BURKS, T. F., AND YAMAMURA, H. I.: Mediation of analgesia by multiple opioid receptors, In Advances in Pain Research and Therapy, ed. by C. S. Hill Jr. and W. S. Fields, pp.247-289, Raven Press, New York, 1989.
142. 5]enkephalin: a selective high affinity radioligand for delta opioid receptors with exceptional specific activity. J. Pharmacol. Exp. Ther. 258: 1077-1083, 1991.
143. KONG, H., RAYNOR, K., YANO, H., TAKEDA, J., BELL, G., AND REISINE, T.: Agonists and antagonists bind to different domains of the cloned kappa opioid receptor. Proc. Natl. Acad. Sci. USA 91: 8042-8046, 1994.
144. KONG, H., RAYNOR, K., YASUDA, K., MOE, S. T., PORTOGHESE, P. S., BELL, G. I., AND REISINE, T.: A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding. J. Biol. Chem. 268: 23055-23058, 1993.
145. KONKOY, C. S., AND CHILDERS, S. R.: Dynorphin-selective inhibition of adenylyl cyclase in guinea pig cerebellum membranes. Mol. Pharmacol. 36: 627-633, 1989.
146. KONKOY, C. S., AND CHILDERS, S. R.: Relationship between kappa 1 opioid receptor binding and inhibition of adenylate cyclase in guinea pig brain membranes. Biochem. Pharmacol. 45: 207-216, 1993.
147. KORLIPARA, V. L., TAKEMORI, A. E., AND PORTOGHESE, P. S.: N-benzylaltrindoles as long-acting δ-opioid receptor antagonists. J. Med. Chem. 37: 1882-1885, 1994.
148. KOSTERLITZ, H. W., LORD, J. A. H., PATERSON, S. J., AND WATERFIELD, A. A.: Effects of changes in the structure of enkephalins and of narcotic analgesic drugs on their interactions with mu and delta receptors. Br. J. Pharmacol. 68: 333-342, 1980.
149. KOSTERLITZ, H. W., PATERSON, S. J., AND ROBSON, L. E.: Characterization of the κ-subtype of the opiate receptor in the guinea-pig brain. Br. J. Pharmacol. 73: 939-949, 1981.
150. KREIL, G., BARRA, D., SIMMACO, M., ERSPAMER, V., ERSPAMER, G, F., NEGRI, L., SEVERINI, C., CORSI, R., AND MELCHIORRI, P.: Deltorphin, a novel amphibian skin peptide with high selectivity and affinity for delta opioid receptors. Eur. J. Pharmacol. 162: 123-128, 1989.
151. KROMER, W.: The current statue of opioid research on gastrointestinal motility. Life Sci. 44: 579-589, 1989.
152. KROMER, W.: Voltage-clamp experiments reveal receptor type-dependent modulation of chloride secretion in the guinea pig colonie mucosa by intestinal opioids. Naunyn-Schmiedebergs Arch. Pharmacol. 344: 360-367, 1991.
153. 3H]U-69593, a highly selective ligand for the opioid κ receptor. Eur. J. Pharmacol. 109: 281-284, 1985.
154. LAHTI, R. A., VON VOIGTLANDEH, P. F., AND BARSUHN, C.: Properties of a selective kappa agonist, U-50, 488 H. Life Sci. 31: 2257-2260, 1982.
155. LAI, H. W. L., MINAMI, M., SATOH, M., AND WONG, Y. H.: Gz coupling to the rat κ-opioid receptor. FEBS Lett. 360: 97-99, 1995.
156. LAI, J., MA, S. W., ZHU, R. H., ROTHMAN, R. B., LENTES, K. U., AND PORRECA, F.: Pharmacological characterization of the cloned kappa opioid receptor as a kappa 1b subtype. Neuroreport 5: 2161-2164, 1994.
157. LAWRENCE, D. M. P., AND BIDLACK, J. M.: The kappa opioid receptor expressed on the mouse R1. 1 thymoma cell line is coupled to adenylyl cyclase through a pertussis toxin-sensitive guanine nucleotide-binding regulatory protein. J. Pharmacol. Exp. Ther. 266: 1678-1683, 1993.
158. LAZARUS, L. H., BRYANT, S. D., ATTILA, M., AND SALVADORI, S.: Frog skin opioid peptides: a case for environmental mimicry. Environ. Health Perspect. 102: 648-654, 1994.
159. LAZARUS, L. H., WILSON, W. E., DE CASTIGLIONE, R. D., AND GUGLIETTA, A.: Dermorphin gene sequence peptide with high affinity and selectivity for δ-opioid receptors. J. Biol. Chem. 264: 3047-3050, 1989.
160. LEANDER, J. D.: A kappa opioid effect: increased urination in the rat. J. Pharmacol. Exp. Ther. 224: 89-94, 1983.
161. LEMAIRE, S., MAGNAN, J., AND REGOLI, D.: Rat vas deferens: a specific bioassay for endogenous opioid peptides. Br. J. Pharmacol. 64: 327-329, 1978.
162. LEVINE, A. S., GRACE, M., BILLINGTON, C. J., AND PORTOGHESE, P. S.: Norbinaltorphimine decreases deprivation and opioid-induced feeding. Brain Res. 534: 60-64, 1990.
163. 3H]Sufentanyl, a superior ligand for μ-opiate receptors: binding properties and regional distribution in rat brain and spinal cord. Eur. J. Pharmacol. 87: 209-225, 1983.
164. LI, C. H., AND CHUNG, D.: Isolation and structure of an untriakontapeptide with opiate activity from camel pituitary glands. Proc. Natl. Acad. Sci. USA 73: 1145-1148, 1976.
165. LI, S., ZHU, J., CHEN, C., CHEN, Y. W., DERIEL, J. K., ASHBY, B., AND LIU-CHEN, L. Y.: Molecular cloning and expression of a rat κ opioid receptor. Biochem. J. 295: 629-633, 1993.
166. 3H]beta-funaltrexamine to opioid receptors in the rat forebrain: comparison with mu and delta receptor distribution. Brain Res. 544: 235-242, 1991.
167. LOOSE, M. D., AND KELLY, M. J.: Opioids act at μ-receptors to hyperpolarize neurons via an inwardly rectifying potassium conductance. Brain Res. 513: 15-23, 1990.
168. LORD, J. A. H., WATERFIELD, A. A., HUGHES, J., AND KOSTERLITZ, H. W.: Endogenous opioid peptides: multiple agonists and receptors. Nature (Lond.) 267: 495-499, 1977.
169. 2. J, Med. Chem. 38: 585-586, 1995.
170. MAGNAN, J., PATERSON S. J., TAVANI, A., AND KOSTERLITZ, H. W.: The binding spectrum of narcotic analgesic drugs with different agonist and antagonist properties. Naunyn-Schmiedebergs Arch. Pharmacol. 319: 197-205, 1982.
171. MAILMAN, D.: Morphine-neural interactions on canine intestinal absorption and blood flow. Br. J. Pharmacol. 81: 263-270, 1984.
172. MANNALACK, D. T., BEART, P. M., AND GUNDLACH, A. L.: Psychotomimetic σ-opiates and PCP. Trends Pharmacol. Sci. 7: 448-451, 1986.
173. MANSOUR, A., Fox, C. A., AKIL, H., AND WATSON, S. J.: Opioid-receptor mRNA expression in the rat CNS: anatomical and functional implications. Trends Neurosci. 18: 22-29, 1995.
174. MANSOUR, A., Fox, C. A., BURKE, S., MENG, F., THOMPSON, R. C., AKIL, H., AND WATSON, S. J.: Mu, delta, and kappa opioid receptor mRNA expression in the rat CNS: an in situ hybridization study. J. Comp. Neurol. 350: 412-438, 1994.
175. MANSOUR, A., KHACHATURIAN, H., LEWIS, M. E., AKIL, H., AND WATSON, S. J.: Anatomy of CNS opioid receptors. Trends Neurosci. 11: 308-314, 1988.
176. MANSOUR, A., LEWIS, M. E., KHACHATURIAN, H., AKIL, H., AND WATSON, S. J.: Pharmacological and anatomical evidence of selective μ, δ and κ opioid receptor binding in rat brain. Brain Res. 399: 69-79, 1986.
177. MARKI, A., OTVOS, F., TOTH, G., HOSZTAFI, S., AND BORSODI, A.: Characterization of kappa opioid receptors with tritiated norBNI. Analgesia 1: 557-560, 1995.
178. MARTIN, W. R., EADES, C. G., THOMPSON, J. A., HUPPLER, R. E., AND GILBERT, P. E.: The effects of morphine- and nalorphine-like drugs in the nondependent and morphine dependent chronic spinal dog. J. Pharmacol. Exp. Ther. 197: 517-532, 1976.
179. 19: a potent and selective κ opioid peptide. Eur. J. Pharmacol. 196: 161-167, 1991.
180. 5] enkephalin induced analgesia in the jimpy mouse: in vivo evidence for δ-receptor mediated analgesia. Eur. J. Pharmacol. 136: 405-407, 1987.
181. MAURER, R., GAEHWILER, B. H., BUCHER, H. H., HILL, R. C., AND ROEMER, D.: Opiate antagonist properties of an octapeptide somatostatin analog. Proc. Natl. Acad. Sci. USA 79: 4815-4817, 1982.
182. MCKENZIE, F. R., AND MILLIGAN, G.: δ-opioid-receptor-mediated inhibition of adenylate cyclase is transduced specifically by the guanine-nucleotide-binding protein Gi2. Biochem. J. 267: 391-398, 1990.
183. MCKNIGHT, A. T., CORBETT, A, D., MARCOLI, M., AND KOSTERLITZ, H. W.: The opioid receptors in the hamster vas deferens are of the δ-type. Neuropharmacoiogy 24: 1011-1018, 1985.
184. MCKNIGHT, A. T., AND REES, D. C.: Opioid receptors and their ligands. Neurotransmissions (Res. Biochem. Inc.) 7: 1-6, 1991.
185. MENG, F., XIE, G. X., THOMPSON, R., MANSOUR, A., GOLDSTEIN, A., WATSON, S., AND AKIL, H.: Cloning and pharmacological characterization of a rat kappa opioid receptor. Proc. Natl. Acad. Sci. USA 90: 9954-9958, 1993.
186. 1 receptor. Nature (Lond.) 377: 532-535, 1995.
187. MEYER, M. E., AND MEYER, M. E.: Behavioral effects of opioid peptide agonists DAMGO, DPDPE and DAKLI on locomotor activities. Pharmacol. Biochem. Behav. 45: 315-320, 1993.
188. MIHARA, S., AND NORTH, R. A.: Opioids increase potassium conductance in submucous neurones of guinea-pig caecum by activating delta-receptors. Br. J. Pharmacol. 88: 312-322, 1986.
189. MILLAN, M. J.: Kappa-opioid receptor-mediated antinociception in the rat. I. Comparative actions of mu- and kappa-opioids against noxious thermal, pressure and electrical stimuli. J. Pharmacol. Exp. Ther. 251: 334-341, 1989.
190. MILLAN, M. J., CZLONKOWSKI, A., LIPKOWSKI, A., AND HERZ, A.: Kappa-opioid receptor-mediated antinociception in the rat. II. Supraspinal in addition to spinal sites of action. J. Pharmacol. Exp. Ther. 251: 342-350, 1989.
191. MIN, B. H., AUGUSTIN, L. B., FELSHEIM, R. F., FUCHS, J. A., AND LOH, H. H.: Genomic structure and analysis of promoter sequence of a mouse μ opioid receptor gene. Proc. Natl. Acad. Sci. USA 91: 9081-9085, 1994.
192. MINAMI, M., ONOGI, T., NAKAGAWA, T., KATAO, Y., AOKI, Y., KATSUMATA, S., AND SATOH, M.: DAMGO, a mu-opioid receptor selective ligand, distinguishes mu- and kappa-opioid receptors at a different region from that for the distinction between mu- and delta-opioid receptors. FEBS Lett. 364: 23-27, 1995.
193. Minami,M. TOYA, T., KATAO, Y., MAEKAWA, K., NAKAMURA, S., ONOGI, T., KANEKO, S., AND SATOH, M.: Cloning and expression of a cDNA for the rat kappa-opioid receptor. FEBS Lett. 329: 291-295, 1993.
194. MISAWA, H., UEDA, H., KATADA, T., UI, M., AND SATOH, M.: A subtype of opioid kappa-receptor is coupled to inhibition of Gil-mediated phospholipase C activity in the guinea pig cerebellum. FEBS Lett. 361: 106-110, 1995.
195. MISAWA, H., UEDA, H., AND SATOH, M.: κ-opioid agonist inhibits phospholipase C, possibly via an inhibition of G-protein activity. Neurosci. Lett. 112: 324-327, 1990.
196. MOISES, H. C., RUSIN, K. I., AND MACDONALD, R. L.: μ-opioid receptor-mediated reduction of neuronal calcium current occurs via a Go-type GTP-binding protein. J. Neurosci. 14: 3642-3651, 1994a.
197. MOISES, H. C., RUSIN, K. I., AND MACDONALD, R. L.: μ- and κ-opioid receptors selectively reduce the same transient components of high-threshold calcium current in rat dorsal root ganglion sensory neurons. J. Neurosci. 14: 5903-5916, 1994b.
198. MOLLEREAU, C., PARMENTIEK, M., MAILLEUX, P., BUTOUR, J. L., MOISAND, C., CHALON, P., CAPUT, P., VASSART, G., AND MEUNIER, J. C.: ORL1, a novel member of the opioid receptor family. Cloning, functional expression and localization. FEBS Lett. 341: 33-38, 1994.
199. MOOLTEN, M. S., FISHMAN, J. B., CHEN, J. C., AND CARLSON, K. R.: Etonitazene: an opioid selective for the mu receptor types. Life Sci. 82: PL199-PL203, 1993.
200. MORIN-SURUN, M. P., BOUDINOT, E., GACEL, G., CHAMPAGNAT, J., ROQUES, B. P., AND DENAVIT-SAUBIÉ, M,: Different effects of μ and δ opiate agonists on respiration. Eur. J. Pharmacol. 98: 235-240, 1984.
201. MOSBERG, H. I., HURST, R., HRUBY, V. J., GEE, K., YAMAMURA, H. I., GALLIGAN, J. J., AND BURKS, T. F.: Bis-penicillinamine enkephalins possess highly improved specificity toward δ opioid receptors. Proc. Natl. Acad. Sci. USA 80: 5871-5874, 1983.
202. 125I-FK 33-824: a selective probe for autoradiographic labeling of μ opioid receptors in the brain. Peptides 7: 351-355, 1986.
203. MUCHA, R. F., AND HERZ, A.: Motivational properties of kappa and mu opioid receptor agonists studied with place and taste preference conditioning. Psychopharmacology 86: 274-280, 1985.
204. NAKANISHI, S., INOUE, A., KITA, T., NAKAMURA, M., CHANG, A. C. Y., COHEN, S. N., AND NUMA, S.: Nucleotide sequence of cloned cDNA for bovine corticotropin-beta-lipotropin precursor. Nature (Lond.) 278: 423-427, 1979.
205. NAKAZAWA, T., FURUYA, Y., KANEKO, T., AND YAMATSU, K.: Spinal kappa receptor-mediated analgesia of E-2078, a systemically active dynorphin analog, in mice. J. Pharmacol. Exp. Ther. 256: 76-81, 1991.
206. NEGRI, L., FALCONIERI ERSPAMER, G., SEVERINI, C., POTENZA, R. L., MELCHIORRI, P., AND ERSPAMER, V.: Dermorphin-related peptides from the skin of Phyllomedusa bicolor and their amidated analogs activate two μ opioid receptor subtypes that modulate antinociception and catalepsy in the rat. Proc. Natl. Acad. Sci. USA 89: 7203-7207, 1992.
207. 3H] TIPP. Life Sci. 53: PL57-PL62, 1993.
208. NEVIN, S. T., TOTH, G., WELTROWSKA, G., SCHILLER, P. W., AND BORSODI, A.: Synthesis and binding characteristics of tritiated TIPP[ψ], a highly specific and stable delta opioid antagonist. Life Sci. 56: PL225-PL230, 1995.
209. NIJSSEN, P. C. G., SEXTON, T., AND CHILDERS, S. R.: Opioid-inhibited adenylyl cyclase in rat brain membranes: lack of correlation with high-affinity opioid receptor binding sites. J. Neurochem. 59: 2251-2262, 1992.
210. NISHI, M., TAKESHIMA, H., FUKUDA, K., KATO S., AND MORI, K.: cDNA cloning and pharmacological characterization of an opioid receptor with high affinities for kappa-subtype selective ligands. FEBS Lett. 330: 77-80, 1993.
211. NOBLE F., AND Cox, B. M.: Differential regulation of D1 dopamine receptorand of A2a adenosine receptor-stimulated adenylate cyclase by μ-, δ1-, and δ2-opioid agonists in rat caudate putamen. J. Neurochem. 65: 125-133, 1995.
212. NOCK, B., GIORDANO, A. L., AND CICERO, T. J.: ICI 197067 is a selective ligand for the U-69593-sensitive kappa opiate binding site. Eur. J. Pharmacol. 162: 385-386, 1989.
213. NOCK, B., GIORDANO, A. L., CICERO, T. J., AND O'CONNOR, L. H.: Affinity of drugs and peptides for U-69,593-sensitive and -insensitive kappa opiate binding sites: the U-69,593-insensitive site appears to be the beta endorphin-specific epsilon receptor. J. Pharmacol. Exp. Ther. 254: 412-419, 1990.
214. NOCK, B., GIORDANO, A. L., MOORE, B. W., AND CICERO, T. J.: Properties of the putative epsilon receptor-identification in rat, guinea-pig, cow, pig and chicken brain. J. Pharmacol. Exp. Ther. 264: 349-359, 1993.
215. 3HIU-69593 binding sites in rat brain: evidence for κ opioid receptor subtypes. Eur. J. Pharmacol. 154: 27-34, 1988.
216. NODA, M., FURUTANI, Y., TAKAHASHI, H., TOYOSATO, M., HIROSE, T., INAYAMA, S., NAKANISHI, S., AND NUMA, S.: Cloning and sequence analysis of cDNA for bovine adrenal preproenkephalin. Nature (Lond.) 295: 202-206, 1982.
217. OLIANAS, M. C., AND ONALI, P.: Characterization of opioid receptors mediating stimulation of adenylate cyclase activity in rat olfactory bulb. Mol. Pharmacol. 42: 109-115, 1992.
218. 2+/calmodulin- and forskolin-stimulated enzyme activities in rat olfactory bulb. J. Neurochem. 63: 161-168, 1994.
219. 2-(alkylamidino)methyl] naltrindole derivatives as a novel class of kappa opioid receptor antagonists. J. Med. Chem. 36: 179-180, 1993.
220. ONALI, P., AND OLIANAS, M. C.: Naturally occurring opioid receptor agonists stimulate adenylate cyclase activity in rat olfactory bulb. Mol. Pharmacol. 39: 436-441, 1991.
221. ONOGI, T., MINAMI, M., KATAO, Y., NAKAGAWA, T., AOKI, Y., TOYA, T., KATSUMATA, S., AND SATOH, M.: DAMGO, a mu-opioid receptor selective agonist, distinguishes mu- and delta-opioid receptors around their first extracellular loop. FEBS Lett. 357: 93-97, 1995.
222. PASTERNAK, G. W., SIMANTOV, R., AND SNYDER S. H.: Characterization of an endogenous morphine-like factor (enkephalin) in mammalian brain. Mol. Pharmacol. 12: 504-513, 1976.
223. PASTERNAK, G. W., AND STANDIFER, K M.: Mapping of opioid receptors using antisense oligodeoxynucleotides: correlating their molecular biology and pharmacology. Trends Pharmacol. Sci. 16: 344-350, 1995.
224. PASTERNAK, G. W., AND WOOD, P. J.: Multiple mu opiate receptors. Life Sci. 38: 1889-1898, 1986.
225. PAUL, D., BODNAR, R. J., GISTRAK, M. A., AND PASTERNAK, G. W.: Different receptor subtypes mediate spinal and supraspinal analgesia in mice. Eur. J. Pharmacol. 168: 307-314, 1989.
226. PAUL, D., LEVISON, J. A., HOWARD, D. H., PICK, C. G., HAHN, E. F., AND PASTERNAK, G. W.: Naloxone benzoylhydrazone (NalBzOH) analgesia. J. Pharmacol. Exp. Ther. 255: 769-774, 1990.
227. PAZOS, A., AND FLOREZ, J.: A comparative study in rats of the respiratory depression and analgesia induced by μ- and δ-opioid agonists. Eur. J. Pharmacol. 99: 15-21, 1984.
228. PELTON, J. T., GULYA, K., HRUBY, V. J., DUCKLES, S. P., AND YAMAMURA, H. I.: Conformationally restricted analogs of somatostatin with high mu-opiate receptor specificity. Proc. Natl. Acad. Sci. USA 82: 236-239, 1985.
229. PELTON, J. T., KZAMIERSKI, W., GULYA, K., YAMAMURA, H. I., AND HRUBY, V. J.: Design and synthesis of Conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors. J. Med. Chem. 29: 2370-2375, 1986.
230. PERT, C. B., AND SNYDER, S. H.: Opiate receptor: demonstration in nervous tissue. Science (Wash. DC) 179: 1011-1014, 1973.
231. PFEIFFER, A., BRANTL, V., HERZ, A., AND EMRICH, H. M.: Psychotomimesis mediated by κ opiate receptors. Science (Wash. DC) 233: 774-776, 1986.
232. PICK, C. G., PAUL, D., AND PASTERNAK, G. W.: Nalbuphine, a mixed kappal and kappa3 analgesic in mice. J. Pharmacol. Exp. Ther. 262: 1044-1050, 1992.
233. POL, O., FERRER, I., AND PUIG, M. M.: Diarrhea associated with intestinal inflammation increases the potency of mu and delta opioids on the inhibition of gastrointestinal transit in mice. J. Pharmacol. Exp. Ther. 270: 386-391, 1994.
234. POLASTRON, J., BOYER, M. J., QUERTERMONT, Y., THOUVENOT, J. P., MEUNIER, J. C., AND JAUZAC, P.: μ-opioid receptors and not κ-opioid receptors are coupled to the adenylate cyclase in the cerebellum. J. Neurochem. 54: 562-570, 1990.
235. PORRECA, F., MOSBERG, H. I., HURST, R., HRUBY, V. J., AND BURKS, T. F.: Roles of mu, delta and kappa opioid receptors in spinal and supraspinal mediation of gastrointestinal transit effects and hot-plate analgesia in the mouse. J. Pharmacol. Exp. Ther. 230: 341-348, 1984.
236. PORRECA, F., MOSBERG, H. I., OMNAAS, J. R., BURKS, T, F., AND COWAN, A.: Supraspinal and spinal potency of selective opioid agonists in the mouse writhing test. J. Pharmacol. Exp. Ther. 240: 890-894, 1987.
237. PORTOGHESE, P. S.: A new concept on the mode of interaction of narcotic analgesics with receptors. J. Med. Chem. 8: 609-616, 1965.
238. PORTOGHESE, P. S., FAROUZ-GRANT, F., SULTANA, M., AND TAKEMORI, A. E.: 7′-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of δ1 opioid receptor-mediated antinociception in mice. J. Med. Chem. 38: 402-407, 1995.
239. PORTOGHESE, P. S., LARSON, D. L., SAYRE, L. M., FRIES, D. S., AND TAKEMORI, A. E.: A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities. J. Med. Chem. 23: 233-234, 1980.
240. PORTOGHESE, P. S., LIPKOWKSI, A. W., AND TAKEMORI, A. E.: Bimorphinans as highly selective potent kappa receptor antagonists. J. Med. Chem. 30: 238-239, 1987.
241. PORTOGHESE, P. S., MOE, S. T., AND TAKEMORI, A. E.: A selective δ1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for δ1 opioid receptor agonists and antagonists. J. Med. Chem. 36: 2572-2574, 1993.
242. PORTOGHESE, P. S., AND TAKEMORI, A. E.: TENA, a selective kappa opioid receptor antagonist. Life Sci. 36: 801-805, 1985.
243. PORTOGHESE, P. S., SULTANA, M., NAGASE, H., AND TAKEMORI, A. E.: A highly selective δ1-opioid receptor antagonist: 7-benzylidenenaltrexone. Eur. J. Pharmacol. 218: 195-196, 1992a.
244. PORTOGHESE, P. S., SULTANA, M., NELSON, W. L., KLEIN, P., AND TAKEMORI, A. E.: δ opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for S receptor subtypes. J. Med. Chem, 35: 4086-4091, 1992b.
245. PORTOGHESE, P. S., SULTANA, M., AND TAKEMORI, A. E.: Naltrindole, a highly ve and potent non-peptide δ opioid receptor antagonist. Eur. J. Pharmacol. 146: 185-186, 1988.
246. PRATHER, P. L., LOH, H. H., AND LAW, P. Y.: Interaction of δ-opioid receptors with multiple G proteins: a non-relationship between agonist potency to inhibit adenylyl cyclase and to activate G proteins. Mol. Pharmacol. 45: 997-1003, 1994.
247. PRATHER, P. L., MCGINN, T. M., CLAUDE, P. A., LIUCHEN, L. Y., LOH, H. H., AND LAW, P. Y.: Properties of a kappa-opioid receptor expressed in CHO cells: interaction with multiple G-proteins is not specific for any individual G alpha subunit and is similar to that of other opioid receptors. Mol. Brain Res. 29: 336-346, 1995.
248. 3H-naloxone benzoylhydrazone: a reversible κ and slowly dissociable mu opiate. Mol. Pharmacol. 35: 67-74, 1989.
249. PRIMI, M. P., FARGEAS, M. J., AND BUENO, L.: Central μ-, δ, and κ-opioid influences on intestinal water and electrolyte transport in dogs. Regul. Pept. 21: 107-115, 1988.
250. RAGHUBIR, R., PATNAIK, G. K., SHARMA, S. D., MATHUR, K. B., AND DHAWAN, B. N.: Pharmacological profile of two new analogues of metenkephalin. In Recent Progress in the Chemistry and Biology of Centrally Acting Peptides, ed. by B. N. Dhawan and R. S. Rapaka, pp. 167-174, Central Drug Research Institute, Lucknow, India, 1988.
251. RAGHUBIR, R., SRIMAL, R. C., AND DHAWAN, B. N.: Enkephalinergic modulation of cardiovascular effects of clonidine from ventral surface of medulla in cat. In Brain Neurotransmitter Mechanism and Hypertension, ed. by K. K. Tangri, S. Vrat, and A. K. Saxena, pp. 109-115, Kamla Printers, Lucknow, India, 1987.
252. RANDICH, A., ROBERTSON, J. D., AND WILLINGHAM, T.: The use of specific opioid agonists and antagonists to delineate the vagally mediated antinociceptive and cardiovascular effects of intravenous morphine. Brain Res. 603: 186-200, 1993.
253. RAYNOR, K., KONG, H., CHEN, Y., YASUDA, K., Yu, L., BELL, G., AND REISINE, T.: Pharmacological characterization of cloned kappa, delta and mu opioid receptors. Mol. Pharmacol. 45: 330-334, 1994.
254. RAYNOR, K., KONG, H., MESTEK, A., BYE, L. S., TIAN, M., Yu, J., AND REISINE, T.: Characterization of the cloned human mu opioid receptor. J. Pharmacol. Exp. Ther. 272: 423-428, 1995.
255. REINSCHEID, R. K., NOTHACKEH, H. P., BOURSON, A., ARDATI, A., HENNINGSEN, R. A., BUNZOW, J. R., GRANDY, D. K., LANGEN, H., MONSMA, F. J., JR., AND CIVELLI, O.: Orphanin FQ: a neuropeptide that activates an opioid like G protein-coupled receptor. Science (Wash. DC) 270: 792-794, 1995.
256. REISINE, T., AND BELL, G. I.: Molecular biology of opioid receptors. Trends Neurosci. 16: 506-510, 1993.
257. 2]-deltorphin-I binding sites in the rat brain. Neuroreport 4: 1143-1146, 1993.
258. RHIM, H., AND MILLER, R. J.: Opioid receptors modulate diverse types of calcium channels in the nucleus tractus solitarius of the rat. J. Neurosci. 14: 7608-7615, 1994.
259. RICHARDSON, A., DEMOLIOU-MASON, C., AND BARNARD, E. A.: Guanine nucleotide-binding protein-coupled and uncoupled states of opioid receptors and their relevance to the determination of subtypes. Proc. Natl. Acad. Sci. USA 89: 10198-10202, 1992.
260. 2] deltorphin precursors from skin of Phyllomedusa bicolor also contain genetic information for three dermorphin - related opioid peptides. Proc. Natl. Acad. Sci. USA 87: 4836-4839, 1990.
261. ROEMER, D., BUSCHER, H. H., HILL, R. C., PLESS, J., BAUER, W., CARDINAUX, F., CLOSSE, A., HAUSER, D., AND HUGUENIN, R.: A synthetic enkephalin analog with prolonged parenteral and oral analgesic activity. Nature (Lond.) 268: 547-549, 1977.
262. ROERIG, S. C., LOH, H. H., AND LAW, P. Y.: Identification of three separate guanine nucleotide-binding proteins that interact with the δ-opioid receptor in NG108-15 neuroblastoma X glioma hybrid cells. Mol. Pharmacol. 41: 822-831, 1992.
263. ROGERS H., BIRCH, P. J., HARRISON, S. M., PALMER, E., MANCHEE, G. R., JUDD, D. B., NAYLOR, A., SCOPES, D. I. C., AND HAYES, A. G.: GR 94839, a κ-opioid agonist with limited access to the central nervous system, has antinociceptive activity. Br, J. Pharmacol. 106: 783-789, 1992.
264. RÖMER, D., BÜSCHER, H., HILL, R. C., MAURER, R., PETCHER, T. J., WELLE, H. B. A., BAKEL, C. C. K, AND AKKERMAN, A. M.: Bremazocine: a potent, long-acting opiate kappa-agonist. Life Sci. 27: 971-978, 1980.
265. RÖMER, D., BÜSCHER, H. H., HILL, R. C., MAURER, R., PETCHER, T. J., ZEUGNER, H., BENSON, W., FINNER, E., MILKOWSKI, W., AND THIES, P. W.: An opioid benzodiazepine. Nature (Lond.) 298: 759-760, 1982.
266. ROSSI, G. C., PAN, Y. X., BROWN, G. P., AND PASTERNAK, G. W.: Antisense mapping the MOR-1 opioid receptor: evidence for alternative splicing and a novel morphine-6 beta-glucuronide receptor. FEBS Lett. 369:192-196, 1995.
267. ROTHMAN, R. B., BYKOV, V., XUE, B. G., XU, H., DE COSTA, B. R., JACOBSON, A. E., RICE, K. C., KLEINMAN, J. E., AND BRADY, L. S.: Interaction of opioid peptides and other drugs with multiple kappa receptors in rat and human brain: evidence for species differences. Peptides 13: 977-987, 1992.
268. SATOH, M., AND MINAMI, M.: Molecular pharmacology of the opioid receptors. Pharmacol. Ther. 68: 343-364, 1995.
269. SCHILLER, P. W., NGUYEN, T. M. D., WELTROWSKA, G., WILKES, B. C., MARSDEN,B.J., LEMIEUX, C., AND CHUNG, N. N.: Differential stereochemieal requirements of μ vs δ opioid receptors for ligand binding and signal transduction: development of a class of potent and highly δ-selective peptide antagonists. Proc. Natl. Acad. Sci. USA 89: 11871-11875, 1992.
270. SCHILLER, P. W., WELTROWSKA, G. NGUYEN, T. M. D., WILLKES, V. C., CHUNG, N. N., AND LEMI, E. U. X.: TIPP [ψ]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. J. Med. Chem. 36: 3182-3187, 1993.
271. SCHMAUSS, C.: Spinal κ-opioid receptor-mediated antinociception is stimulus specific. Eur. J. Pharmacol. 137: 197-205, 1987.
272. SCHMAUSS, C., AND YAKSH, T. L.: In vivo studies on spinal opiate receptor systems mediating antinociception. II. Pharmacological profiles suggesting a differential association of mu, delta and kappa receptors with visceral and cutaneous thermal stimuli in the rat. J. Pharmacol. Exp. Ther. 228: 1-11, 1984.
273. SCHOFIELD, P. R., MCFARLAND, K. C., HAYFLICK, J. S., WILCOX, J. N., CHO, T. M., ROY, S., LEE, N. M., LOH, H. H., AND SEEBURG, P. H.: Molecular characterization of a new immunoglobulin superfamily protein with potential roles in opioid binding and cell contact. EMBO J. 8: 489-495, 1989.
274. SCHULZ, R., WUSTER, M., AND HERZ, A.: Pharmacological characterization of the ε opiate receptor. J. Pharmacol. Exp. Ther. 216: 604-606, 1981.
275. SHAW, J. S., MILLER, L. TURNBULL, M. J., GORMLEY, J. J., AND MORLEY, J. S.: Selective antagonist at the opiate delta-receptors. Life Sci. 31: 1259-1262, 1982.
276. SHEN, K. F., AND CHAIN, S. M.: Cholera toxin-A subunit blocks opioid excitatory effects on sensory neuron action potential indicating mediation by Gs linked opioid receptors. Brain Res. 525: 225-231, 1990.
277. SHOOK, J. E., KAZMIERSKI, W, WIRE W. S., LEMCKE, P. K., HRUBY, V. J., AND BURKS, T. F.: Opioid receptor selectivity of β-endorphin in vitro and in vivo: mu, delta and epsilon receptors. J. Pharmacol. Exp. Ther. 246: 1018-1025, 1988.
278. 3H] etorphine to rat brain homogenate. Proc. Natl. Acad. Sci. USA 70: 1947-1949, 1973.
279. SOFUOGLU, M., PORTOGHESE, P. S., AND TAKEMORI, A. E.: Differential antagonism of delta opioid agonists by naltrindole and its benzofuran analog (NTB) in mice: evidence for delta opioid receptor subtypes. J. Pharmacol. Exp. Ther. 257: 676-680, 1991.
280. SPANAGEL, R., ALMEIDA, O. F. X., AND SHIPPENGERG, T. S.: Evidence that nor-binaltorphimine can function as an antagonist at multiple opioid receptor subtypes. Eur. J. Pharmacol. 264: 157-162, 1994.
281. SPIEGEL, K., AND PASTERNAK, G. W.: Meptazinol: a novel mu-1 selective analgesic. J. Pharmacol. Exp. Ther. 228: 414-419, 1984.
282. SRIMAL, R. C., RAGHUBIR, R., AND DHAWAN, B. N.: Cardiovascular response to enkephalin on topical application to ventral surface of medulla. In Current Statue of Centrally Acting Peptides, ed. by B. N. Dhawan, pp.77-83, Pergamon Press, Oxford, 1982.
283. STAPELFELD, A., HAMMOND, D. L., AND RAFFERTY, M. F.: Antinociception after intra-cerebroventricular administration of naltrindole in the mouse. Eur. J. Pharmacol. 214: 273-276, 1992.
284. STEIN, C.: Peripheral mechanisms of opioid analgesia. Anesth. Analg. 76: 182-191, 1993.
285. 4] deltorphin. J. Pharmacol. Exp. Ther. 266: 820-828, 1993.
286. SULLIVAN, A. F., DICKENSON, A. H., AND ROQUES, B. P.: δ-opioid mediated inhibitions of acute and prolonged noxious-evoked responses in rat dorsal horn neurones. Br. J. Pharmacol. 98: 1039-1049, 1989.
287. SURRATT, C. K, JOHNSON, P. S., MORIWAKI, A., SEIDLECK, B. K., BLASCHAK, C. J., WANG, J. B., AND UHL, G. R.: μOpiate receptor. Charged transmembrane domain amino acids are critical for agonist recognition and intrinsic activity. J. Biol. Chem. 269: 20548-20553, 1994.
288. TAKEMORI, A. E., SULTANA, M., NAGASE, H., AND PORTOGHESE, P. S.: Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone. Life Sci. 50: 1491-1495, 1992.
289. TALLENT, M., DICHTER, M. A., BELL, G. I., AND REISINE, T.: The cloned kappa opioid receptor couples to an N-type calcium current in undifferentiated PC-12 cells. Neuroscience 63: 1033-1040, 1994.
290. TAMIR, M., AND KUSHNER, L.: Expression of functional δ opioid receptor in Xenopus oocytes. Biochem. Biophys. Res. Commun. 193: 1224-1231, 1993.
291. TAUSSIG, R., SANCHEZ, S., RIFO, M., GOLMAN, A. G., AND BELARDETTI, F.: Inhibition of the omega conotoxin-sensitive calcium current by distinct G proteins. Neuron 8: 799-809, 1992.
292. TEMPEL, A., AND ZUKIN, R. S.: Neuroanatomical patterns of the μ, δ and κ opioid receptors of rat brain as determined by quantitative in vitro autoradiography. Proc. Natl. Acad. Sci. USA 84: 4308-4312, 1987.
293. TERENIUS, L.: Stereospecific interaction between narcotic analgesics and synaptic plasma membrane fraction of rat cerebral cortex. Acta Pharmacol. Toxicol. 32: 317-329, 1973.
294. THOMPSON, R. C., MANSOUR, A., AKIL, H., AND WATSON, S. J.: Cloning and pharmacological characterization of a rat μ opioid receptor. Neuron 11: 903-913, 1993.
295. TIVE L. A., PICK, C. G., PAUL, D., ROQUES, B. P., GACEL, G. A., AND PASTERNAK, G. W.: Analgesic potency of TRIMU-5: a mixed μ2 opioid receptor agonist/μ1 receptor antagonist. Eur. J. Pharmacol. 216: 249-255, 1992.
296. 5]enkephalin analogues with increased affinity and selectivity for δ opioid receptors. J. Med. Chem. 33: 249-253, 1990.
297. TSENG, L. F., TSAI, J. H. H., COLLINS, K. A., AND PORTOGHESE, P. S.: Spinal delta(2)-, but not delta(1)-, mu, or kappa-opioid receptors are involved in the tail-flick inhibition induced by beta-endorphin from nucleus raphe obscurus in the pentobarbital-anesthetized rat. Eur. J. Pharmacol. 277: 261-256, 1995.
298. TSU, R. C., CHAN, J. S. C., AND WONG, Y. H.: Regulation of multiple effectors by the cloned δ-opioid receptor: stimulation of phospholipase C and type II adenylyl cyclase. J. Neurochem. 64: 2700-2707, 1995.
299. + channel current by a μ-type opioid receptor. Mol. Pharmacol. 49: 793-798, 1994.
300. UHL, G. R., CHILDERS, S., AND PASTERNAK, G.: An opiate-receptor gene family reunion. Trends Neurosci. 17: 89-93, 1994.
301. 4]deltorphin with δ-opioid receptor subtypes in vivo. Eur. J. Pharmacol. 252: 133-137, 1994.
302. VANHOUTTE, P. M., HUMPHREY, P. P. A., AND SPEDDING, M.: X. International Union of Pharmacology recommendations for nomenclature of new receptor subtypes. Pharmacol. Rev. 48: 1-2, 1996.
303. 5] enkephalin. Life Sci. 45: 1001-1008, 1989.
304. VAUGHT, J. L., MATHIASEN, J. R., AND RAFFA, R. B.: Examination of the involvement of supraspinal and spinal mu and delta opioid receptors in analgesia using the mu receptor deficient CXBK mouse. J. Pharmacol. Exp. Ther. 245: 13-16, 1988.
305. VON VOIGTLANDER, P. F., LAHTI, R. A., AND LUDENS, J. H.: U-50,488H, a selective and structurally novel non-mu (kappa) opioid agonist. J. Pharmacol. Exp. Ther. 224: 7-12, 1983.
306. VON VOIGTLANDER, P. F., AND LEWIS, R. A.: Analgesic and mechanistic evaluation of spiradoline, a potent kappa opioid. J. Pharmacol. Exp. Ther. 246: 259-262, 1988.
307. WAKSMAN, G., HAMEL, E., FOURNIÉ-ZALUSKI, M. C., AND ROQUES, B. P.: Autoradiographic comparison of the distribution of the neutral endopeptidase "enkephalinase" and of mu and delta opioid receptors in rat brain. Proc. Natl. Acad. Sci. USA 83: 1523-1527, 1986.
308. 3H]Ohmefentanyl preferentially binds to μ-opioid receptors but also labels σ-sites in rat brain sections. Eur. J. Pharmacol. 193: 341-350, 1991.
309. WANG, J. B., IMIA, Y., EPPLER, C. M., GREGOR, P., SPIVAK, C. E., AND UHL, G. R.: μ Opiate receptor: cDNA cloning and expression. Proc. Natl. Acad. Sci. USA 90: 10230-10234, 1993.
310. WANG, J. B., JOHNSON, P. S., IMAI, Y., PERSICO, A. M., OZENBERGER, B. A., EPPLER, C. M., AND UHL, G. R.: cDNA cloning of an orphan opiate receptor gene family member and its splice variant. FEBS Lett. 348: 75-79, 1994a.
311. WANG, J. B., JOHNSON, P. S., PERSICO, A. M., HAWKINS, A. L., GRIFFIN, C. A., AND UHL. G. R.: Human μ opiate receptor: cDNA and genomic clones, pharmacologic characterization and chromosomal assignment. FEBS Lett. 338: 217-222, 1994b.
312. WANG, J. B. JOHNSON, P. S., Wu, J. M., WANG, W. F., AND UHL, G. R.: Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras. J. Biol. Chem. 269:42: 25966-25969, 1994c.
313. WANG, L., AND GINTZLER, A. R.: Bimodal opioid regulation of cyclic AMP
314. WARD, S. J., FRIES, D. S., LARSON, D. L., PORTOGHESE, P. S., AND TAKEMORI, A. E.: Opioid receptor binding characteristics of the non-equilibrium mu antagonist, beta-funaltrexamine (beta-FNA). Eur. J, Pharmacol. 107: 323-330, 1985.
315. WICK, M. J., MINNERATH, S. R., LIN, X. Q., ELDE, R., LAW, P. Y., AND LOH, H. H.: Isolation of a novel cDNA encoding a putative membrane receptor with high homology to the cloned mu, delta, and kappa opioid receptors. Mol. Brain Res. 27: 37-44, 1994.
316. Wild, K. D., CARLISI, V. J., MOSBEHG, H. I., BOWEN, W. D., PORTOGHESE, P. S., SULTANA, M., TAKEMORI, A. E., HRUBY, V. J., AND PORRECA, F.: Evidence for a single functional opioid delta receptor subtype in the mouse isolated vas deferens. J. Pharmacol. Exp. Ther. 264: 831-838, 1993a.
317. WILD, K. D., FANG, L., MCNUTT R. W., CHANG, K. J., TOTH, G., BORSODI, A., YAMAMURA, H. I., AND PORRECA, F.: Binding of BW 373U86, a non-peptidic δ opioid receptor agonist, is not regulated by guanine nucleotides and sodium. Eur. J. Pharmacol. Mol. Pharmacol. 246: 289-302, 1993b.
318. WILLIAMS, J. T., AND NORTH, R. A.: Opiate-receptor interactions on single locus coeruleus neurones. Mol. Pharmacol. 26: 489-497, 1984.
319. WIMPEY, T. L., AND CHAVKIN, C.: Opioids activate both an inward rectifier and a novel voltage-gated potassium conductance in the hippocampal formation. Neuron 6: 281-289, 1991.
320. WUARIN, J. P., AND DUDEK, F. E.: Direct effects of an opioid peptide selective for μ-receptors: intracellular recordings in the paraventricular and supraoptic nuclei of the guinea-pig. Neuroscience 36: 291-298, 1990.
321. WUSTER, M., SCHULZ, R., AND HERZ, A.: Specificity of opioide towards the μ-, δ-and ε- opiate receptors. Neurosci. Lett. 15: 193-198, 1979.
322. XIE, G., MIYAJIMA, A., AND GOLDSTEIN, A: Expression cloning of cDNA encoding a seven helix receptor from human placenta with affinity for κ opioid ligands. Proc. Natl. Acad. Sci. USA 89: 4124-4128, 1992.
323. XIE, G. X., MENG, F., MANSOUR, A., THOMPSON, R. C., HOVERSTEN, M. T., GOLDSTEIN, A., WATSON, S. J., AND AKIL, H.: Primary structure and functional expression of a guinea pig κ opioid (dynorphin) receptor. Proc. Natl. Acad. Sci. USA 91: 3779-3783, 1994.
324. XU, H., CHEN, J., AND Cm, Z. Q.: Ohmefentanyl-a new agonist for μ-opiate receptor. Sci. Sin, B 28: 604-511, 1985.
325. 125I]IOXY-AGO): a potent and selective radioligand for opioid μ receptors. Synapse 19: 105-111, 1995.
326. XUE, J. C., CHEN, C., ZHU, J., KUNAPULI, S., DERIEL, J. K., YU, L., AND LIU-CHEN, L. Y.: Differential binding domains of peptide and non-peptide ligands in the cloned rat κ opioid receptor. J. Biol. Chem. 269: 30195-30199, 1994.
327. 3H]naltrindole binding to δ-opioid receptors in rat brain. Life Sci. 50: PL119-PL124, 1992.
328. YASUDA, K., ESPINOSA, R., TAKEDA, J., LE BEAU, M., AND BELL, G. I.: Localization of the kappa opioid receptor gene to human chromosome band 8q11.2. Genomics 19: 596-597, 1994.
329. YASUDA, K., RAYNOR, K., KONG, H., BREDER, C. D., TAKEDA, J., REISINE, T., AND BELL, G. I: Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. Proc. Natl. Acad. Sci. USA 90: 6736-6740, 1993.
330. YEADON, M., AND KITCHEN, I.: Multiple opioid receptors mediate the respiratory depressant effects of fentanyl-like drugs in the rat. Gen. Pharmacol. 21: 665-664, 1990.
331. YOSHINO, H., NAKAZAWA, T., ARAKAWA, Y., KANEKO, T., TSUCHIYA, Y., MATSUNAGA, M., ARAKI, S., IKEDA, M., YAMATSU, K., AND TACHIBANA, S.: Synthesis and structure-activity relationships of dynorphin A(1-8) amide analogues. J. Med. Chem. 33: 206-212, 1990.
332. YU, V., RICHARDS, M. L., AND SADEE, W.: A human neuroblastoma cell line expresses mu and delta opioid receptor sites. J. Biol. Chem. 261: 1065-1070, 1986.
333. ZAGON, I. S., GIBO, D. M., AND MCLAUGHLIN, P. J.: Zeta, a growth related opioid receptor in developing rat cerebellum: identification and characterization. Brain Res. 551: 28-35, 1991.
334. ZAJAC, J. M., GACEL, G., PETIT, F., DODEY, P., ROSSIGNOL, P., AND ROQUES, B. P.: Enkephalin Tyr-D-Thr-Gly-Phe-Leu-Thr: a new highly potent and fully specific agonist for opiate delta receptors. Biochem. Biophys. Res. Commun. 111: 390-397, 1983.
335. ZASTAWNY, R. L., GEORGE, S. R., NGUYEN, T., CHENG, R., TSATSOS, J., BRIONESURBINA, R., AND O'DOWD, B. F.: Cloning, characterization, and distribution of a μ-opioid receptor in rat brain. J. Neurochem. 62: 2099-2105, 1994.
336. ZHANG, S. W., AND Yu, L. C.: Identification of dynorphins as endogenous ligands for an opioid receptor-like orphan receptor. J. Biol. Chem. 270: 22772-22776, 1995.
337. ZUKIN, R. S., EGHBALI, M., OLIVE, D., UNTERWALD, E. M., AND TEMPEL, A.: Characterization and visualization of rat and guinea pig brain kappa opioid receptors: evidence for κ1 and κ2 opioid receptors. Proc. Natl. Acad. Sci. USA 85: 4061-4065, 1988.