The δ-opioid receptor: Molecular pharmacology, signal transduction, and the determination of drug efficacy

Pharmacological Reviews

Volumn 51, Issue 3, 1999, Pages 503-532

  Quock, Raymond M ^a   Burkey, Thomas H ^c   Varga, Eva ^c   Hosohata, Yoshiaki ^c   Hosohata, Keiko ^c   Cowell, Scott M ^c   Slate, Cheryl A ^c   Ehlert, Frederick J ^b   Roeske, William R ^c,e   Yamamura, Henry I ^c,d,e  

^a WASHINGTON STATE UNIVERSITY   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c UNIVERSITY OF ARIZONA COLLEGE OF MEDICINE   (United States)

^d University of Arizona   (United States)

^e UNIVERSITY OF ARIZONA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,2,3,4,4A,5,12,12AALPHA OCTAHYDRO 4AALPHA (3 HYDROXYPHENYL) 2 METHYLQUINOLINO[2,3 G]ISOQUINOLINE; 4 [ALPHA (4 ALLYL 2,5 DIMETHYL 1 PIPERAZINYL) 3 HYDROXYBENZYL] N,N DIETHYLBENZAMIDE; 4 [ALPHA (4 ALLYL 2,5 DIMETHYL 1 PIPERAZINYL) 3 METHOXYBENZYL] N,N DIETHYLBENZAMIDE; ANTISENSE OLIGODEOXYNUCLEOTIDE; BIPHALIN; CALCIUM; CYCLIC AMP; DELTORPHIN; ENKEPHALIN DERIVATIVE; GUANINE NUCLEOTIDE BINDING PROTEIN; OPIATE AGONIST; POTASSIUM; PROTEIN KINASE; SIGMA OPIATE RECEPTOR;

ANALGESIA; ANTINOCICEPTION; CALCIUM TRANSPORT; DRUG EFFICACY; LIGAND BINDING; MOLECULAR CLONING; NONHUMAN; PHARMACODYNAMICS; POTASSIUM CONDUCTANCE; PRIORITY JOURNAL; PROTEIN DOMAIN; RECEPTOR DOWN REGULATION; RECEPTOR INTRINSIC ACTIVITY; REVIEW; SIGNAL TRANSDUCTION;

EID: 0032866115     PISSN: 00316997     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (291)

1. Abood ME, Noel MA, Farnsworth JS and Tao Q (1994) Molecular cloning and expression of a δ-opioid receptor from rat brain. J Neurosci Res 37:714-719.
2. Adams JU, Chen X, Deriel JK, Adler MW and Liu-Chen LY (1994) Intracerebroventricular treatment with an antisense oligodeoxynucleotide to κ-opioid receptors inhibited κ-agonist-induced analgesia in rats. Brain Res 667:129-132.
3. Albert PR and Morris SJ (1994) Antisense knockouts: Molecular scalpels for the dissection of signal transduction. Trends Pharmacol Sci 15:250-254.
4. Allouche S, Polastron J and Jauzac P (1996) The δ-opioid receptor regulates activity of ryanodine receptors in the human neuroblastoma cell line SK-N-BE. J Neurosci Methods 67:2461-2470.
5. Ariëns EJ (1954) Affinity and intrinsic activity in the theory of competitive inhibition, part I. Problems and theory. Arch Int Pharmacodyn Ther 99:32-49.
6. Augustin LB, Felsheim RF, Min BH, Fuchs SM, Fuchs JA and Loh HH (1995) Genomic structure of the mouse δ opioid receptor gene. Biochem Biophys Res Commun 207:111-119.
7. βγ. J Biol Chem 271:21309-21315.
8. Ballanyi K, Lalley PM, Hoch B and Richter DW (1997) cAMP-dependent reversal of opioid- and prostaglandin-mediated depression of the isolated respiratory network in newborn rats. J Physiol(Lond) 504:127-134.
9. Beddell CR, Clark RB, Lowe LA and Wilkinson S (1977) A conformational analysis for leucine-enkephalin using activity and binding data of synthetic analogues. Br J Pharmacol 61:351-356.
10. Befort K, Tabbara L, Bausch S, Chavkin C, Evans C and Kieffer BL (1996a) The conserved aspartate residue in the third putative transmembrane domain of the δ-opioid receptor is not the anionic counterpart for cationic opiate binding but is a constituent of the receptor binding site. Mol Pharmacol 49:216-223.
11. γS binding: A tool to evaluate functional activity of a cloned opioid receptor transiently expressed in COS cells. Neurochem Res 21:1301-1307.
12. Befort K, Tabbara L, Kling D, Maigret B and Kieffer BL (1996c) Role of aromatic transmembrane residues of the δ-opioid receptor in ligand recognition. J Biol Chem 271:10161-10168.
13. βγ subunits. J Neurochem 70:635-645.
14. 2 enkephalinamides following D-isomer substitutions at position five. Life Sci 23:99-104.
15. 4)deltorphin antinociception by supraspinal but not spinal administration of an antisenae oligodeoxynucleotide to an opioid delta receptor. Life Sci 55:PL37-PL43.
16. Bilsky EJ, Calderon SN, Wang T, Bernstein RN, Davis P, Hruby VJ, McNutt RW, Rothman RB, Rice KC and Porreca F (1995) SNC80, a selective nonpeptidic and systemically active opioid delta agonist. J Pharmacol Exp Ther 273:359-366.
17. Birnbaumer L, Abramowitz I and Brown AM (1990) Receptor-effector coupling by G-proteins. Biochim Biophys Acta 1031:163-224.
18. Black JW and Leff P (1983) Operational models of pharmacological agonism. Proc R Soc Lond B 220:141-162.
19. Blume AJ (1978) Opiate binding to membrane preparations of neuroblastoma x glioma hybrid cells NG 108-15: Effects of ions and nucleotides. Life Sci 22:1843-1852.
20. + and GTP. Proc Natl Acad Sci USA 76:5626-5630.
21. Bunzow JR, Saez C, Mortrud M, Bouvier C, Williams JT, Low M and Grandy DK (1994) Molecular cloning and tissue distribution of a putative member of the rat opioid receptor gene family that is not a μ, δ or κ opioid receptor type. FEBS Lett 347:284-288.
22. Bunzow JR, Zhang G, Bouvier C, Saez C, Ronnekleiv OK, Martin JK and Grandy DK (1995) Characterization and distribution of a cloned rat μ-opioid receptor. J Neurochem 64:14-24.
23. 2) a potent opioid peptide: Receptor binding and analgesic properties. Peptides 3:869-871.
24. Burt AR, Carr IC, Mullaney I, Anderson NG and Milligan G (1996) Agonist activation of p42 and p44 mitogen-activated protein kinases following expression of the mouse δ opioid receptor in rat-1 fibroblasts: Effects of receptor expression levels and comparisons with G-protein activation. Biochem J 320:227-235.
25. Búzás B, Izenwasser S, Portoghese PS and Cox BM (1994) Evidence for delta opioid receptor subtypes regulating adenylyl cydase activity in rat brain. Life Sci 54: PL101-PL106.
26. Búzás B, Rosenberger J and Cox BM (1997) Regulation of δ-opioid receptor mRNA levels by receptor-mediated and direct activation of the adenylyl cyclase-protein kinase A pathway. J Neurochem 68:610-615.
27. Calderon SN, Rothman RB, Porreca F, Flippen-Anderson JL, McNutt RW, Xu H, Smith LE, Bilsky EJ, Davis P and Rice KC (1994) Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-((αR)-α((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl)-N,N-diethylbenzamide (SNC 80): A highly selective nonpeptide δ opioid receptor agonist. J Med Chem 37:2125-2128.
28. Chang K-J, Blanchard SG and Cuatrecasas P (1984) Benzomorphan sites are ligand recognition sites of putative ε-receptors. Mol Phormocol 26:484-488.
29. Chang K-J, Hazum E and Cuatrecasas P (1981a) Novel opiate binding sites selective for benzomorphan drugs. Proc Notl Acad Sci USA 78:4141-4145.
30. Chang K-J, Hazum E, Killan A and Cuatrecasas P (1981b) Interactions of ligands with morphine and enkephalin receptors are differentially regulated by guanine nucleotides. Mol Pharmacol 20:1-7.
31. Chang K-J, Rigdon GC, Howard JL and McNutt RW (1993) A novel potent and selective nonpeptidic delta opioid receptor agonist BW373U86. J Pharmacol Exp Ther 267:852-857.
32. Chen XH, Adams JU, Geller EB, Deriel JK, Adler MW and Liu-Chen LY (1995a) An antisense oligodeoxynucleotide to μ-opioid receptors inhibits μ-opioid receptor agonist-induced analgesia in rats. Eur J Pharmacol 278:105-108.
33. Chen XH, Geller EB, Deriel JK, Liu-Chen LY and Adler MW (1995b) Antisense oligodeoxynucleotides against μ- or κ-opioid receptors block agonist-induced body temperature changes in rats. Brain Res 688:237-241.
34. Chen Y, Fan Y, Liu J, Mestek A, Tian M, Kozak CA and Yu L (1994) Molecular cloning tissue distribution and chromosomal localization of a novel member of the opioid receptor gene family. FEBS Lett 347:279-283.
35. Chen Y, Mestek A, Liu J, Hurley JA and Yu L (1993a) Molecular cloning and functional expression of a μ-opioid receptor from rat brain. Mol Pharmacol 44:8-12.
36. Chen Y, Mestek A, Liu J and Yu L (1993b) Molecular cloning of a rat κ-opioid receptor reveals sequence similarities to the μ and δ opioid receptors. Biochem J 295:625-628.
37. 2)deltorphin I. Eur J Pharmacol 230:85-88.
38. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
39. Chien CC, Brown G, Pan YX and Pasternak GW (1994) Blockade of U50,488H analgesia by antisense oligodeoxynucleotides to a κ-opioid receptor. Eur J Pharmacol 253:R7-R8.
40. Childers SR (1991) Opioid receptor-coupled second messenger systems. Life Sci 48:1991-2003.
41. Clark AJ (1926a) The reaction between acetylcholine and muscle cells. J Physiol (Lond) 61:530-546.
42. Clark AJ (1926b) The antagonism of acetylcholine by atropine. J Physiol (Lond) 61:547-556.
43. Clark AJ (1933) The Mode of Action of Drugs on Cells, E Arnold and Co., London.
44. Clark AJ (1937) General Pharmacology (Heubner W and Schüller J eds) Springer-Verlag, Berlin.
45. Claude PA, Wotta DR, Zhang XH, Prather PL, McGinn TM, Erickson LJ, Loh HH and Law PY (1996) Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists. Proc Natl Acad Sci USA 93:5715-5719.
46. Collier HOJ and Roy AC (1974) Morphine-like drugs inhibit the stimulation by E prostaglandins of cyclic AMP formation by rat brain homogenate. Nature (Lond) 248:24-27.
47. 3H]Naltrindole: A potent and selective ligand for labeling δ-opioid receptors. Brain Res 604:160-164.
48. Costa T, Wurster M, Gramsch C and Herz A (1985) Multiple states of opioid receptors may modulate adenylate cydase in intact neuroblastoma x glioma hybrid cells. Mol Pharmacol 28:146-154.
49. Cotton R, Giles MG, Miller L, Shaw JS and Timm D (1984) ICI 174864: A highly selective antagonist for the opioid δ-receptor. Eur J Pharmacol 97:331-332.
50. Cowan A, Zhu XZ, Mosberg HI, Omnaas JR and Porreca F (1988) Direct dependence studies in rats with agents selective for different types of opioid receptor. J Pharmacol Exp Ther 246:950-955.
51. 353 located within the COOH-terminal tail of the δ opiate receptor is involved in receptor down-regulation. J Biol Chem 271:4073-4076.
52. Dhawan BN, Cesselin F, Raghubir R, Reisine T, Bradley PB, Portoghese PS and Hamon M (1996) International Union of Pharmacology XII classification of opioid receptors. Pharmacol Rev 48:567-592.
53. Dickenson AH (1997) Plasticity: Implications for opioid and other pharmacological interventions in specific pain states. Behav Brain Sci 20:392-403.
54. Edsall SA, Knapp RJ, Vanderah TW, Roeske WR, Consroe P and Yamamura HI (1996) Antisense oligodeoxynucleotide treatment to the brain cannabinoid receptor inhibits antinociception. Neuroreport 7:593-596.
55. Ehlert FJ (1985) The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium. Mol Pharmacol 28:410-421.
56. Emmerson PJ, Liu MR, Woods JH and Medzihradsky F (1994) Binding affinity and selectivity of opioids at mu, delta and kappa receptors in monkey brain membranes. J Pharmacol Exp Ther 271:1630-1637.
57. Erspamer V, Melchiorri P, Falconieri-Erspamer G, Negri L, Corsi R, Severini C, Barra D, Simmaco M and Kreil G (1989) Deltorphins: A family of naturally occurring peptides with high affinity and selectivity for S opioid binding sites. Proc Natl Acad Sci USA 86:5188-5192.
58. Evans CJ, Keith DE Jr, Morrison H, Magendzo K and Edwards RH (1992) Cloning of a delta opioid receptor by functional expression. Science (Wash DC) 258:1952-1955.
59. + conductance of DRG neurons and neuroblastoma x DRG neuron hybrid F11 cells. Brain Res 696:97-105.
60. + channels in sensory ganglion neurons. Brain Res 558:166-170.
61. + currents in F11 neuroblastoma x DRG neuron hybrid cells via cholera toxin-sensitive receptors. Brain Res 605:214-220.
62. Frederickson RCA, Smithsich EL, Shuman R and Bemis KG (1981) Metkephamid, a systemically active analog of methionine enkephalin with potent opioid alphareceptor activity. Science (Wash DC) 211:603-606.
63. Fukuda K, Kato S, Mori K, Nishi M and Takeshima H (1993) Primary structures and expression from cDNAs of rat opioid receptor δ- and μ-subtypes. FEBS Lett 327:311-314.
64. Fukuda K, Kato S, Mori K, Nishi M, Takeshima H, Iwabe N, Miyata T, Houtani T and Sugimoto T (1994) cDNA cloning and regional distribution of a novel member of the opioid receptor family. FEBS Lett 343:42-46.
65. Fukuda K, Kato S, Morikawa H, Shoda T and Mori K (1996) Functional coupling of the δ-, μ- and κ-opioid receptors to mitogen-activated protein kinase as arachidonate release in Chinese hamster ovary cells. J Neurochem 67:1309-1316.
66. Furchgott RF (1966) The use of β-haloalkylamines in the differentiation of receptors and in determination of dissociation constants of receptor-agonist complexes, in Advances in Drug Research (Harper NJ and Simmonds AB eds) vol 3, pp 21-55, Academic Press, London.
67. Furchgott RF and Bursztyn P (1967) Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasympathetic receptors. Ann N Y Acad Sci 144:882-893.
68. Gacel G, Dauge V, Preuze P, Delay-Goyet P and Roques BP (1988) Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for δ opioid receptors. J Med Chem 31:1891-1897.
69. Galligan JJ, Mosberg HI, Hurst R, Hruby VJ and Burks TF (1984) Cerebral delta opioid receptors mediate analgesia but not the intestinal motility effects of intracerebroventricularly administered opioids. J Pharmacol Exp Ther 229:641-648.
70. Garzón J, Juarros JL, Castro MA and Sánchez-Blazquez P (1995) Antibodies to the cloned μ-opioid receptor detect various molecular weight forms in areas of mouse brain. Mol Pharmacol 47:738-744.
71. i2 transducer proteins. Life Sci 55:PL205-PL212.
72. m GTPase activity in mouse periaqueductal grey matter. Eur J Neurosci 9:1194-1200.
73. Gilbert PE and Martin WR (1976) The effects of morphine- and nalorphine-like drugs in the non-dependent morphine-dependent and cyclazocine-dependent chronic spinal dog. J Pharmacol Exp Ther 198:66-82.
74. Gillan MGC, Kosterlitz HW and Magnan J (1981) Unexpected antagonism in the rat vas deferens by benzomorphans which are agonists in other pharmacological tests. Br J Pharmacol 72:13-15.
75. Gilman AG (1987) G-proteins: Transducers of receptor generated signals. Annu Rev Biochem 66:6615-6649.
76. Gilman AG (1994) G proteins and regulation of adenylyl cyclase. Biosci Rep 15:65-97.
77. Goldstein A (1987) Binding selectivity profiles for ligands of multiple receptor types: Focus on opioid receptors. Trends Pharmacol Sci 8:456-459.
78. Goldstein A, Aronow L and Kalman SM (1974) Principles of drug action, in The Basis of Pharmacology, 2nd ed., John Wiley and Sons, New York.
79. Goode TL and Raffa RB (1997) An examination of the relationship between μ-opioid antinociceptive efficacy and G-protein coupling using pertussis and cholera toxins. Life Sci 60:107-113.
80. Gourley DRH and Beckner SK (1973) Antagonism of morphine analgesia by adenine adenosine and adenine nucleotides. Proc Soc Exp Biol Med 144:774-778.
81. Halford WP, Gebhardt BM and Carr DJJ (1995) Functional role and sequence analysis of a lymphocyte orphan opioid receptor. J Neuroimmunol 59:91-101.
82. Hamm HE (1998) The many faces of G protein signaling. J Biol Chem 273:669-672.
83. Harnett MM and Klaus GGB (1988) G protein regulation of receptor signaling. Immunol Today 9:315-320.
84. o regulates neuronal calcium channels. Nature (Lond) 325:445-447.
85. Heyman JS, Mulvaney SA, Mosberg HI and Porreca F (1987) Opioid δ-receptor involvement in supraspinal and spinal antinociception in mice. Brain Res 420: 100-108.
86. Heyman JS, Vaught JL, Raffa RB and Porreca F (1988) Can supraspinal δ-opioid receptors mediate antinociception? Trends Pharmacol Sci 9:134-138.
87. 2 opioid receptor populations in rat brain. Brain Res 719:85-95.
88. Ho IK, Loh HH and Way EL (1972) Effect of cyclic AMP on morphine analgesia tolerance and physical dependence. Nature (Lond) 238:397-398.
89. Ho IK, Loh HH and Way EL (1973) Cyclic adenosine monophosphate antagonism of morphine analgesia. J Pharmacol Exp Ther 185:336-346.
90. Horan PJ, Mattia A, Bilsky EJ, Weber S, Davis TP, Yamamura HI, Malatynska E, Appleyard SM, Slaninova J, Misicka A, Lipkowski AW, Hruby VJ and Porreca F (1993) Antinociceptive profile of biphalin, a dimeric enkephalin analog. J Pharmacol Exp Ther 265:1446-1454.
91. 2-adrenergic receptors by sodium. J Biol Chem 265:21590-21595.
92. Hosford DA and Haigler HJ (1981) Cyclic AMP morphine met-enkephalin and neuronal firing. J Pharmacol Exp Ther 219:496-504.
93. Hosohata K, Burkey TH, Alfaro-Lopez J, Varga E, Hruby VJ, Roeske WR and Yamamura HI (1998) Endomorphin-1 and endomorphin-2 are partial agonists at the human μ-opioid receptor. Eur J Pharmacol 346:111-114.
94. Hsia JA, Moss J, Hewlett EL and Vaughan M (1984) ADP-ribosylation of adenylate cyclase by pertussis toxin: Effects on inhibitory agonist binding. J Biol Chem 259:1086-1090.
95. Hughes J, Smith TW, Kosterlitz HW, Fothergill LA, Morgan BA and Morris HR (1975) Identification of two related pentapeptides from the brain with potent agonist activity. Nature (Lond) 258:577-579.
96. Huidobro-Toro JP, Caturay EM, Ling N, Lee NM, Loh HH and Way EL (1982) Studies on the structural prerequisites for the activation of the β-endorphin receptor on the rat vas deferens. J Pharmacol Exp Ther 222:262-269.
97. Izenwasser S, Búzás B and Cox BM (1993) Differential regulation of adenylyl cyclase activity by mu and delta opioids in rat caudate putamen and nucleus accumbens. J Pharmacol Exp Ther 267:145-152.
98. 6)enkephalin and naltrindole 5′-isothiocyanate: Evidence for delta receptor subtypes. J Pharmacol Exp Ther 257:1069-1075.
99. Jin W, Lee NM, Loh HH and Thayer SA (1992) Dual excitatory and inhibitory effects of opioids on intracellular calcium in neuroblastoma x glioma hybrid NG108-15 cells. Mol Pharmacol 42:1083-1089.
100. Jin W, Lee NM, Loh HH and Thayer SA (1994) Opioids mobilize calcium from inositol 1,4,5-triphosphate-sensitive stores in NG108-15 cells. J Neurosci 14:1920-1929.
101. 3H-β-endorphin in rat brain. Life Sci 31:1381-1384.
102. Kamei J, Saitoh A, Ohsawa M, Suzuki T, Misawa M, Nagase H and Kasuya Y (1995) Antinociceptive effects of the selective non-peptidic δ-opioid receptor agonist TAN-67 in diabetic mice. Eur J Pharmacol 276:131-135.
103. Kenakin T (1996) The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol Rev 48:413-463.
104. Kest B, Lee CE, McLemore GL and Inturrisi CE (1996) An antisense oligodeoxynucleotide to the delta opioid receptor (DOR-1) inhibits morphine tolerance and acute dependence in mice. Brain Res Bull 39:185-188.
105. Kieffer BL (1995) Recent advances in molecular recognition and signal transduction of active peptidea: Receptors for opioid peptides. Cell Mol Neurobiol 15:615-635.
106. Kieffer BL, Befort K, Gaveriaux-Ruff C and Hirth CG (1992) The δ-opioid receptor: Isolation of a cDNA clone by expression cloning and pharmacological characterization. Proc Natl Acad Sci USA 89:12048-12052.
107. Kieffer BL, Befort K, Gaveriaux-Ruff C and Hirth CG (1994) The δ-opioid receptor: Isolation of a cDNA clone by expression cloning and pharmacological characterization. Proc Natl Acad Sci USA 91:1193.
108. Kitchen I, Slowe SJ, Matthes HWD and Kieffer BL (1997) Quantitative autoradiographic mapping of μ-, δ- and κ-opioid receptors in knockout mice lacking the μ-opioid receptor gene. Brain Res 778:73-88.
109. Knapp RJ, Landsman R, Waite S, Malatynska E, Varga E, Haq W, Hruby VJ, Roeske WR, Nagase H and Yamamura HI (1995a) Properties of TAN-67, a nonpeptidic δ-opioid receptor agonist, at cloned human δ- and μ-opioid receptors. Eur J Pharmacol 291:129-134.
110. Knapp RJ, Malatynska E, Collins N, Fang L, Wang JY, Hruby VJ, Roeske WR and Yamamura HI (1995b) Molecular biology and pharmacology of cloned opioid receptors. FASEB J 9:516-525.
111. Knapp RJ, Malatynska E, Fang L, Li X, Babin E, Nguyen M, Santoro G, Varga EV, Hruby VJ, Roeske WR and Yamamura HI (1994) Identification of a human delta opioid receptor: Cloning and expression. Life Sci 54:PL463-PL469.
112. Kong H, Raynor K, Yano H, Takada J, Bell GI and Reisine T (1994) Agonists and antagonists bind to different domains of the cloned κ opioid receptor. Proc Natl Acad Sci USA 91:8042-8046.
113. Kong H, Raynor K, Yasuda K, Moe S, Portoghese P, Bell GI and Reisine T (1993) A single residue aspartic acid 95 in the delta opioid receptor specifies selective high affinity agonist binding. J Biol Chem 268:23055-23058.
114. Kreil G, Barra D, Simmaco M, Erspamer V, Erepamer GF, Negri L, Severini C, Corsi R and Melchiorri P (1989) Deltorphin, a novel amphibian skin peptide with high selectivity and affinity for δ opioid receptors. Eur J Pharmacol 162:123-128.
115. Kurose H, Katada T, Amano T and Ui M (1983) Specific uncoupling by islet-activating protein pertussis toxin of negative signal transduction via α-adrenergic cholinergic and opiate receptors in neuroblastoma x glioma hybrid cells. J Biol Chem 258:4870-4875.
116. Lachowicz JE, Shen Y, Monsma FJ Jr and Sibley DR (1995) Molecular cloning of a novel G protein-coupled receptor related to the opiate receptor family. J Neurochem 64:34-40.
117. Lai J, Bilsky EJ and Porreca F (1995) Treatment with antisense oligodeoxynucletoide to a conserved sequence of opioid receptors inhibits antinociceptive effects of delta subtype selective ligands. J Recept Signal Transduct Res 15:643-650.
118. 2-agonist antinociception. Neuroreport 5:1049-1052.
119. Lane-Ladd SB, Pineda J, Boundy VA, Pfeuffer T, Krupinski J, Aghajanian GK and Nestler EJ (1997) CREB (cAMP response element-binding protein) in the locus coeruleus: Biochemical physiological and behavioral evidence for a role in opiate dependence. J Neurosci 17:7890-7901.
120. Langley JN (1905) On the reaction of cells and of nerve-endings to certain poisons chiefly as regards the reaction of striated muscle to nicotine and to curari. J Physiol (Lond) 33:374-413.
121. Law PY, Hom DS and Loh HH (1985a) Multiple affinity states of opiate receptor in neuroblastoma x glioma NG 103-15 hybrid cells: Opiate agonist association rate is a function of receptor occupancy. J Biol Chem 260:3561-3569.
122. Law PY, Hom DS and Loh HH (1991) Opioid receptor desensitization and high affinity state. J Pharmacol Exp Ther 256:710-716.
123. Law PY and Loh HH (1993) δ-Opioid receptor activates cAMP phosphodiesterase activities in neuroblastoma x glioma NG108-15 hybrid cells. Mol Pharmacol 43: 684-693.
124. Law P-Y, Loh HH and Li CH (1979) Properties and localization of β-endorphin receptor in rat brain. Proc Natl Acad Sci USA 76:5455-5459.
125. Law PY, Louie AK and Loh HH (1985b) Effect of pertussis toxin treatment on the down-regulation of opiate receptors in neuroblastoma x glioma NG108-15 hybrid cells. J Biol Chem 260:14818-14823.
126. Law PY, Wu J, Koehler JE and Loh HH (1981) Demonstration and characterization of the opiate inhibition of striatal adenylate cyclase. J Neurochem 36:1834-1846.
127. Lazareno S, Farries T and Birdsall NJM (1993) Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors m1-m4. Life Sci 52:449-456.
128. Levy RA, Goldstein BD and Elyjiw MM (1981) Analgesia following local injection of dibutyryl cyclic nucleotides at sites in the rat CNS. Eur J Pharmacol 71:139-142.
129. Li S, Zhu J, Chen C, Chen YW, Deriel JK, Ashby B and Liu-Chen LY (1993) Molecular cloning and expression of a rat κ opioid receptor. Biochem J 295:629-633.
130. 284 of the human δ opioid receptor is required for SNC121 binding but not binding of pCl-DPDPE, deltorphin II or naltrindole. Analgesia 1:539-542.
131. Li X Varga EV, Stropova D, Zalewska T, Malatynska E, Knapp RJ, Roeske WR and Yamamura HI (1996) δ-Opioid receptor: The third extracellular loop determines naltrindole selectivity. Eur J Pharmacol 300:R1-R2.
132. Liao S, Lin J, Shenderovich MD, Han Y, Hosohata K, Davis P, Qui W, Porreca F, Yamamura HI and Hruby VJ (1997) The stereochemical requirements of the novel δ-opioid selective dipeptide antagonist TMT-TIC. Bioorg Med Chem Lett 7:3049-3052.
133. Lipkowaki AW, Konecka AM and Scroczynska I (1982) Double-enkephalins-synthesis, activity on guinea-pig ileum, and analgesic effect. Peptides 3:697-700.
134. Lipkowski AW, Konecka AM, Scroczynska I, Przewlocki R, Stala L and Tam SW (1987) Bivalent opioid peptide analogues with reduced distances between pharmacophores. Life Sci 40:2283-2288.
135. Lord JA, Waterfield AA, Hughes J and Kosterlitz HW (1977) Endogenous opioid peptides: Multiple agonists and receptors. Nature (Lond) 267:495-499.
136. 35S]thio)triphosphate binding. Mol Pharmacol 44:115-123.
137. Lou L and Pei G (1997) Modulation of protein kinase C and cAMP-dependent protein kinase by δ-opioid. Biochem Biophys Res Commun 238:626-629.
138. Mackay D (1966) The mathematics of drug-receptor interactions. J Pharm Pharmacol 18:201-222.
139. Mak CK, Avalos M, Randall PK, Kwan S-W, Abell CW, Neumeyer JL, Whisennand R and Wilcox RE (1996) Improved models for pharmacological null experiments: Calculation of drug efficacy at recombinant D1A dopamine receptors stably expressed in clonal cell lines. Neuropharmacology 35:549-570.
140. Malatynska E, Wang Y, Knapp RJ, Santoro G, Waite S, Roeske WR and Yamamura HI (1995) Human S opioid receptor: A stable cell line for functional studies of opioids. Neuroreport 8:613-616.
141. Malatynska E, Wang Y, Knapp RJ, Waite S, Calderon S, Rice K, Hruby VJ, Yamamura HI and Roeske WR (1996) Human delta opioid receptor: Functional studies on stably transfected Chinese hamster ovary cells after acute and chronic treatment with the selective nonpeptidic agonist SNC-80. J Pharmacol Exp Ther 278:1083-1089.
142. Mansour A, Fox CA, Akil H and Watson SJ (1995) Opioid-receptor mRNA expression in the rat CNS: Anatomical and functional implications. Trends Neurosci 18:22-29.
143. Mansour A, Khachaturian H, Lewis ME, Akil H and Watson SJ (1988) Anatomy of CNS opioid receptors. Trends Neurosci 11:308-314.
144. Mansson E, Bare L and Yang D (1994) Isolation of a human K opioid receptor cDNA from placenta. Biochem Biophys Res Commun 202:1431-1437.
145. Martin WR, Eades CG, Thompson JA, Huppler RE and Gilbert PE (1976) The effects of morphine- and nalorphine-like drugs in the non-dependent and morphine-dependent chronic spinal dog. J Pharmacol Exp Ther 197:517-532.
146. Matthes HWD, Smadja C, Valverde O, Vonesch J-L, Foutz AS, Boudinot E, Denavit-Saubié M, Severini C, Negri L, Roques BP, Maldonado R and Kieffer BL (1998) Activity of the δ-opioid receptor is partially reduced, whereas activity of the κ-receptor is maintained in mice lacking the μ-receptor. J Neurosci 18:7285-7295.
147. 2)deltorphin II in mice: Evidence for delta receptor subtypes. J Pharmacol Exp Ther 258:583-587.
148. 12. Biochem J 267:391-398.
149. McPhillips JJ (1994) Drug testing in humans, in Modern Pharmacology (Craig CR and Stitzel RE eds) 4th ed., pp 85-91, Little, Brown & Company, Boston.
150. Meng F, Hoversten MT, Thompson RC, Taylor L, Watson SJ and Akil H (1995) A chimeric study of the molecular basis of affinity and selectivity of the κ and the δ opioid receptors: Potential role of extracellular domains. J Biol Chem 270:12730-12736.
151. Meng F, Ueda Y, Hoversten MT, Thompson RC, Taylor L, Watson SJ and Akil H (1996) Mapping the receptor domains critical for the binding selectivity of δ-opioid receptor liganda. Eur J Pharmacol 311:285-292.
152. Meng F, Xie GX, Thompson RC, Mansour A, Goldstein A, Watson SJ and Akil H (1993) Cloning and pharmacological characterization of a rat κ opioid receptor. Proc Natl Acad Sci USA 90:9954-9958.
153. Merkouris M, Dragatsis I, Megaritis G, Konidakis G, Zioudrou C, Milligan G and Georgoussi Z (1996) Identification of the critical domains of the δ-opioid receptor involved in G protein coupling using site-specific synthetic peptides. Mol Pharmacol 60:985-993.
154. Metzger TG and Ferguson DM (1995) On the role of extracellular loops of opioid receptors in conferring ligand selectivity. FEBS Lett 378:1-4.
155. Meunier J-C (1997) Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor. Eur J Pharmacol 840:1-15.
156. 1 receptor. Nature (Lond) 377:532-535.
157. Min BH, Augustin LB, Felsheim RF, Fuchs JA and Loh HH (1994) Genomic structure and analysis of promoter sequence of a mouse μ opioid receptor gene. Proc Natl Acad Sci USA 91:9081-9085.
158. 5)enkephalin from binding to the δ-opioid receptor. Mol Pharmacol 50:1413-1422.
159. Minami M, Onogi T, Toya T, Katao Y, Hosoi Y, Maekawa K, Katsumata S, Yabuuchi K and Satoh M (1994) Molecular cloning and in situ hybridization histochemistry for rat μ-opioid receptor. Neurosci Res 18:315-322.
160. Minami M and Satoh M (1995) Molecular biology of the opioid receptors: Structures, functions and distributions. Neurosci Res 23:121-145.
161. Minami M, Toya T, Katao Y, Maekawa K, Nakamura S, Onogi T, Kaneko S and Satoh M (1993) Cloning and expression of a cDNA for the rat κ-opioid receptor. FEBS Lett 329:291-295.
162. Miotto K, Magendzo K and Evans CJ (1995) Molecular characterization of opioid receptors, in The Pharmacology of Opioid Peptides (Tseng LF ed) pp 57-71, Harwood Academic Publishers.
163. Misicka A, Lipkowski AW, Horvath R, Davis P, Porreca F, Yamamura HI and Hruby VJ (1997) Structure-activity relationship of biphalin: The synthesis and biological activities of new analogues with modifications in positions 3 and 4. Life Sci 60:1263-1269.
164. 2)deltorphin II-induced locomotor hyperactivity. Life Sci 59:69-73.
165. Mollereau C, Parmentier M, Mailleux P, Butour J-L, Moisand C, Chalon P,
166. 2+ current in NG108-15 cells. J Neurochem 65:1403-1406.
167. Mosberg HI, Hurst R, Hruby VJ, Gee K, Akiyama K, Yamamura HI and Burks TF (1983a) Cyclic penicillamine containing enkephalin analogs display profound delta receptor selectivities. Life Sci 33 (Suppl 1):447-450.
168. Mosberg HI, Hurst R, Hruby VJ, Gee K, Yamamura HI, Galligan JJ and Burks TF (1983b) Bis-penicillamine enkephalins possess highly improved specificity toward 8 opioid receptors. Proc Natl Acad Sci USA 80:5871-5874.
169. 2 and delta opioid binding in the central nervous system of C57BL/6BY and CXBK (opioid receptor-deficient) mice. Brain Res 360:108-116.
170. o in smooth muscle. Mol Pharmacol 60:870-877.
171. Nagase H, Wakita H, Kawai K, Endoh T, Matsura H, Tanaka C and Takezawa Y (1994) Syntheses of non-peptidic delta opioid agonists and their structure activity relationships. Jpn J Pharmacol 64 (Suppl 1):35-39.
172. Narita M and Tseng LF (1995) Stimulation of spinal δ-opioid receptors in mice selectively enhances the attenuation of δ-opioid receptor-mediated antinociception by antisense oligodeoxynucleotide. Eur J Pharmacol 284:185-189.
173. Narita M and Tseng LF (1998) Evidence for the existence of the β-endorphin-sensitive "ε-opioid receptor" in the brain: The mechanisms of e-mediated antinociception. Jpn J Pharmacol 76:233-253.
174. Negri L, Potenza RL, Corsi R and Melchiorri P (1991) Evidence for two subtypes of δ opioid receptors in rat brain. Eur J Pharmacol 192:335-336.
175. Nestler EJ and Aghajanian GK (1997) Molecular and cellular basis of addiction. Science (Wash DC) 278:58-63.
176. Nickerson M (1956) Receptor occupancy and tissue response. Nature (Lond) 178: 697-698.
177. Nishi M, Takeshima H, Fukuda K, Kato S and Mori K (1993) cDNA cloning and pharmacological characterization of an opioid receptor with high affinities for κ subtype-selective ligands. FEBS Lett 330:77-80.
178. Nishi M, Takeshima H, Mori M, Nakagawara K and Takeuchi T (1994) Structure and chromosomal mapping of genes for the mouse κ-opioid receptor and an opioid receptor homologue (MOR-C). Biochem Biophys Res Commun 205:1353-1357.
179. North RA, Williams JT, Surprenant A and Christie MJ (1987) μ and δ receptors belong to a family of receptors that are coupled to potassium channels. Proc Natl Acad Sci USA 84:5487-5491.
180. O'Dowd BF, Scheideler MA, Nguyen T, Cheng R, Rasmussen JS, Marchese A, Zastawny R, Heng HHQ, Tsui LC, Shi XM, Asa S, Puy L and George SR (1995) The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes GPR7 and GPR8 expressed in discrete areas of the brain. Genomics 28:84-91.
181. Onogi T, Minami M, Katao Y, Nakagawa T, Aoki Y, Toya T, Katsumata S and Satoh M (1995) DAMGO, a μ-opioid receptor selective agonist, distinguishes between μ- and δ-opioid receptors around their first extracellular loops. FEBS Lett 357:93-97.
182. 2-adrenergic receptor: How structure elucidates function. Annu Rev Pharmacol Toxicol 32:167-183.
183. Pasternak GW (1993) Pharmacological mechanisms of opioid analgesics. Clin Neuropharmacol 16:1-18.
184. Pasternak GW, Childers SR and Snyder SH (1980) Opiate analgesia: Evidence for mediation by a subpopulation of opiate receptors. Science (Wash DC) 208:514-516.
185. Pasternak GW and Standifer KM (1995) Mapping of opioid receptors using antisense oligodeoxynucleotides: Correlating their molecular biology and pharmacology. Trends Pharmacol Sci 16:344-350.
186. Pei G, Kieffer BL, Lefkowitz RJ and Freedman NJ (1995) Agonist-dependent phosphorylation of the mouse δ-opioid receptor: Involvement of G protein coupled receptor kinases but not protein kinase C. Mol Pharmacol 48:173-177.
187. Pert CB and Snyder SH (1973) Opiate receptor: Its demonstration in nervous tissue. Science (Wash DC) 179:1011-1014.
188. Pert CB and Snyder SH (1974) Opiate receptor binding of agonists and antagonists affected differentially by sodium. Mol Pharmacol 10:868-879.
189. Pfeiffer A, Brantl V, Herz A and Emrich HM (1986) Psychotomimesis mediated by κ opiate receptors. Science (Wash DC) 233:774-776.
190. 5)enkephalin in the mouse. J Pharmacol Exp Ther 241:393-400.
191. Porreca F, Mosberg HI, Hurst R, Hruby VJ and Burks TF (1984) 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.
192. Portoghese PS (1965) A new concept on the mode of interaction of narcotic analgesics with receptors. J Med Chem 8:809-816.
193. Portoghese PS (1989) Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists. Trends Pharmacol Sci 10:230-236.
194. Portoghese PS, Lipkowskj AW and Takemori AE (1986) Bimorphinans as a highly selective potent K opioid receptor antagonist. Life Sci 34:1287-1292.
195. Portoghese PS, Sultana M, Nagase H and Takemori AE (1988) Application of the message-address concept in the design of highly potent and selective non-peptide δ opioid receptor antagonists. J Med Chem 31:281-282.
196. 1-opioid receptor antagonist: 7-Benzylidenenaltrexone. Eur J Pharmacol 218: 195-196.
197. Priestley T, Turnbull MJ and Wei E (1986) In vivo evidence for the selectivity of ICI 154129 for the delta-opioid receptor. Neuropharmacology 24:107-110.
198. Przewlocki R, Costa T, Lang J and Herz A (1987) Pertussis toxin abolishes the antinociception mediated by opioid receptors in rat spinal cord. Eur J Pharmacol 144:91-95.
199. Quock RM, Hosohata Y, Knapp RJ, Burkey TH, Hosohata K, Zhang X, Rice KC, Nagase H, Hruby VJ, Porreca F, Roeske WR and Yamamura HI (1997) Relative efficacies of δ-opioid receptor agonists at the cloned human δ-opioid receptor. Eur J Pharmacol 326:101-104.
200. i2α antisense oligonucleotide differentiates morphine antinociception, constipation and acute dependence in mice. Life Sci 58:PL73-PL76.
201. Raffa RB, Martinez RP and Connelly CD (1994) G-protein antisense oligodeoxynucleotides and μ-opioid supraspinal antinociception. Eur J Pharmacol 258:R5-R7.
202. Raynor K, Kong H, Chen Y, Yasuda K, Yu L, Bell GI and Reisine T (1994) Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptors. Mol Pharmacol 45:330-334.
203. Raynor K, Kong H, Law S, Heerding J, Tallent M, Livingston F, Hines J and Reisine T (1996) Molecular biology of opioid receptors. NIDA Res Monogr 161:83-103.
204. Raynor K, Kong H, Mestek A, Bye LS, Tian M, Liu J, Yu L and Reisine T (1995) Characterization of the cloned human mu opioid receptor. J Pharmacol Exp Ther 272:423-428.
205. Reinscheid RK, Nothacker HP, Bourson A, Ardati A, Henningsen RA, Bunzow JR, Grandy DK, Langen H, Monsma FJ and Civelli O (1995) Orphanin FQ: A neuropeptide that activates an opioidlike G protein-coupled receptor. Science (Wash DC) 270:792-794.
206. Reisine T (1995) Opiate receptors. Neuropharmacology 34:463-472.
207. Reisine T and Bell GI (1993) Molecular biology of opioid receptors. Trends Neurosci 16:506-510.
208. Reisine T, Kong H, Yasuda K, Raynor K, Tallent M and Bell GI (1994) Molecular-biology of kappa-opioid and delta-opioid receptors. Regul Pept Suppl I:S5-S6.
209. Remmers AE, Clark MJ, Liu XY and Medzihradsky F (1998) Delta opioid receptor down-regulation is independent of functional G protein yet is dependent on agonist efficacy. J Pharmacol Exp Ther 287:625-632.
210. Rens-Domiano S and Hamm HE (1995) Structural and functional relationships of heterotrimeric G-proteins. FASEB J 9:1059-1066.
211. + and guanyl nucleotides. J Biol Chem 255:820-823.
212. Rossi G, Pan YX, Cheng J and Pasternak GW (1994) Blockade of morphine analgesia by an antisense oligodeoxynucleotide against the mu receptor. Life Sci 54:PL375-PL379.
213. Rossi GC, Leventhal L, Bolan E and Pasternak GW (1997) Pharmacological characterization of orphanin FQ/nociceptin and its fragments. J Pharmacol Exp Ther 282:858-865.
214. Rossi GC, Leventhal L and Pasternak GW (1996) Naloxone sensitive orphanin FQ-induced analgesia in mice. Eur J Pharmacol 311:R7-R8.
215. Rossi GC, Standifer KM and Pasternak GW (1995) Differential blockade of morphine and morphine-6β-glucuronide analgesia by antisense oligodeoxynucleotides directed against MOR-1 and G-protein α subunits in rats. Neurosci Lett 198:99-102.
216. Ruffolo RR Jr (1982) Important concepts of receptor theory. J Auton Pharmacol 8:277-295.
217. Samama P, Cotecchia S, Costa T and Lefkowitz RJ (1993) A mutation-induced activated state of the beta-2-adrenergic receptor: Extending the ternary complex model. J Biol Chem 268:4625-4636.
218. Sánchez-Blazquez P, Garcia-Espana A and Garzón J (1995) In vivo injection of antisense oligodeoxynucleotides to G alpha subunits and supraspinal analgesia evoked by mu and delta opioid agonists. J Pharmacol Exp Ther 275:1590-1596.
219. Sánchez-Blazquez P and Garzón J (1988) Pertussis toxin differentially reduces the efficacy of opioids to produce supraspinal analgesia in the mouse. Eur J Pharmacol 152:357-361.
220. 8 alpha enhances the supraspinal antinociception induced by morphine beta-endorphin and clonidine in mice. Life Sci 51:PL237-PL242.
221. i3 transducer proteins. Life Sci 53:PL129-PL134.
222. Sánchez-Blazquez P and Garzón J (1998) Delta opioid receptor subtypes activate inositol-signaling pathways in the production of antinociception. J Pharmacol Exp Ther 285:820-827.
223. i2 transducer proteins on mu/delta opioid-mediated supraspinal antinociception. Life Sci 53:PL381-PL386.
224. Satoh M and Minami M (1995) Molecular pharmacology of the opioid receptors. Pharmacol Ther 68:343-364.
225. Schiller PW, Nguyen TMD, Weltrowska G, Wilkes BC, Marsden BJ, Lemieux C and Chung NN (1992) Differential stereochemical 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.
226. Schulz R, Wüster M and Herz A (1981) Pharmacological characterization of the ε-opiate receptor. J Pharmacol Exp Ther 216:604-606.
227. 35S]thio)triphosphate binding in rat brain membranes. Life Sci 59:659-668.
228. Sharif NA and Hughes J (1989) Discrete mapping of brain mu and delta opioid receptors using selective peptides: Quantitative autoradiography species differences and comparison with kappa receptors. Peptides 10:499-522.
229. Sharma SK, Klee WA and Nirenberg M (1977) Opiate-dependent modulation of adenylate cyclase. Proc Natl Acad Sci USA 74:3365-3369.
230. Sharma SK, Nirenberg M and Klee WA (1975) Morphine receptors as regulators of adenylate cyclase activity. Proc Natl Acad Sci USA 72:590-594.
231. Sheldon RJ, Riviere PJ, Malarchik ME, Mosberg HI, Burks TF and Porreca F (1990) Opioid regulation of mucosal ion transport in the mouse isolated jejunum. J Pharmacol Exp Ther 253:144-151.
232. 2+-dependent secretion in human small-cell lung carcinoma cells. J Neurosci 16:3672-3684.
233. Silbert BS, Lipkowski AW, Cepeda MS, Szyfelbein SK, Osgood PF and Carr DB (1991) Analgesic activity of a novel bivalent opioid peptide compared to morphine via different routes of administration. Agents Actions 33:382-387.
234. 35S]thio)-triphosphate binding. Proc Natl Acad Sci USA 92:7242-7246.
235. 3H]etorphine to rat-brain homogenate. Proc Natl Acad Sci USA 70:1947-1949.
236. Simonin F, Befort K, Gaveriaux-Ruff C, Matthes H, Nappey V, Lannes B, Micheletti G and Kieffer B (1994) The human δ opioid receptor: Genomic organization, cDNA cloning, functional expression, and distribution in human brain. Mol Pharmacol 46:1015-1021.
237. Simonin F, Gaveriaux-Ruff C, Befort K, Matthes H, Lannes B, Micheletti G, Mattei M-G, Charron G, Bloch B and Kieffer B (1995) Kappa opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system. Proc Natl Acad Sci USA 92:7006-7010.
238. 2+ from intracellular stores in undifferentiated NG108-15 cells. J Neurochem 66:1462-1467.
239. Sofuoglu M, Portoghese PS and Takemori AE (1991) 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.
240. 5-enkephalin-induced analgesia. Eur J Pharmacol 324:R1-R2.
241. Sora I, Takahashi N, Funada M, Ujike H, Revay RS, Donovan DM, Miner LL and UhI GR (1997b) Opiate receptor knockout mice define mu receptor roles in endogenous nociceptive responses and morphine-induced analgesia. Proc Natl Acad Sci USA 94:1544-1549.
242. Spiegel AM, Shenker A and Weinstein LS (1992) Receptor effector coupling by G proteins: Implications for normal and abnormal signal transduction. Endocr Rev 13:536-565.
243. Standifer KM, Chien CC, Wahlestedt C, Brown GP and Pasternak GW (1994) Selective loss of δ opioid analgesia and binding by antisense oligodeoxynucleotides to a δ opioid receptor. Neuron 12:805-810.
244. Standifer KM and Pasternak GW (1997) G proteins and opioid receptor-mediated signalling. Cell Signal 9:237-248.
245. Standifer KM, Rossi GC and Pasternak GW (1996) Differential blockade of opioid analgesia by antisense oligodeoxynucleotides directed against various G protein a subunite. Mol Pharmacol 50:293-298.
246. Starke K (1977) Regulation of noradrenaline release by presynaptic receptor systems. Rev Physiol Biochem Pharmacol 77:1-124.
247. Stephenson RP (1956) A modification of receptor theory. Br J Pharmacol 11:379-393.
248. Strader CD, Fong TM, Graziano MP and Tota MR (1995) The family of G-protein-coupled receptors. FASEB J 9:745-754.
249. Strosberg AD (1991) Structure/function relationship of proteins belonging to the family of receptors coupled to GTP-binding proteins. Eur J Biochem 196:1-10.
250. Suh HH and Tseng LF (1990) Delta but not mu-opioid receptors in the spinal cord are involved in antinociception induced by β-endorphin given intracerebroventricularly in mice. J Pharmacol Exp Ther 253:981-986.
251. Suzuki T, Tsuji M, Mori T, Misawa M, Endoh T and Nagase H (1995) Effects of a highly selective nonpeptide δ opioid receptor agonist TAN-67 on morphine-induced antinociception in mice. Life SCi 57:155-168.
252. Takemori AE, Larson DL and Portoghese PS (1980) The irreversible narcotic antagonistic and reversible agonist properties of the fumarate methyl ester derivative of naltrexone. EUr J Pharmacol 70:445-451.
253. Takemori AE and Portoghese PS (1992) Selective naltrexone-derived opioid receptor antagonists. Annu Rev Pharmacol Toxicol 32:239-269.
254. i in ND8-47 neuroblastoma x dorsal root ganglion hybrid cells is mediated through G protein-coupled &-opioid receptors and desensitized by chronic exposure to opioid. J Neurochem 65:1612-1621.
255. i2 protein α subunit sequence inhibits an opioid-induced increase in the intracellular free calcium concentration in ND8-47 neuroblastoma x dorsal root ganglion hybrid cells. Mol Pharmacol 48:189-193.
256. Tang T, Kiang JG and Cox BM (1994) Opioids acting through delta receptors elicit a transient increase in the intracellular free calcium concentration in dorsal root ganglion-neuroblastoma hybrid ND8-47 cells. J Pharmacol Exp Ther 270:40-46.
257. Taussig R, Sánchez S, Rifo M, Gilman AG and Belardetti F (1992) Inhibition of the ω-conotoxin-sensitive calcium current by distinct G proteins. Neuron 8:799-809.
258. Terenius L (1973) Stereospecific interaction between narcotic analgesics and a synaptic plasma membrane fraction of rat cerebral cortex. Acta Pharmacol Toxicol (Kbh) 32:317-320.
259. Thomas JM, Frazier JS, Hu Z and Hoffman BB (1995) Phosphorylation of cyclic AMP response element-binding protein and induction of c-fos gene expression on withdrawal from chronic treatment with carbachol in NG108-15 cells. Mol Pharmacol 48:593-600.
260. Thompson RC, Mansour A, Akil H and Watson SJ (1993) Cloning and pharmacological characterization of a rat μ opioid receptor. Neuron 11:903-913.
261. 2-adrenergic receptor activation of G proteins: Evidence for a precoupled receptor/G protein state. Mol Pharmacol 45:524-531.
262. 35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells. Mol Pharmacol 47:848-854.
263. Tseng LF and Collins KA (1994) Antisense oligodeoxynucleotide to a δ-opioid receptor given intrathecally blocks i.c.v. administered β-endorphin-induced antinociception in the mouse. Life Sci 55:PL127-PL131.
264. Tseng LF and Collins KA (1995) Pretreatment with pertussis toxin blocks morphinebut not β-endorphin-induced antinociception in the mouse. Eur J Pharmacol 294:345-348.
265. Tseng LF and Collins KA (1996) Pretreatment with pertussis toxin differentially modulates morphine- and β-endorphin-induced antinociception in the mouse. J Pharmacol Exp Ther 279:39-46.
266. Tseng LF, Collins KA and Kampine JP (1994) Antisense oligodeoxynucleotide to a δ-opioid receptor selectively blocks the spinal antinociception induced by δ-but not μ- or κ-opioid receptor agonists in the mouse. Eur J Pharmacol 258:R1-R3.
267. Tseng LF, Narita M and Kampine JP (1995) Pretreatment with β-endorphin facilitates the attenuation of δ-opioid receptor-mediated antinociception caused by δ-opioid receptor antisense oligodeoxynucleotide. Eur J Pharmacol 287:169-172.
268. Tseng LF, Narita M, Mizoguchi H, Kawai K, Mizusuna A, Kamei J, Suzuki T and Nagase H (1997) Delta opioid receptor-mediated antinociceptive properties of a nonpeptidic delta opioid receptor agonist (-)TAN-67 in the mouse spinal cord. J Pharmacol Exp Ther 280:600-605.
269. Tsu RC, Chan JSC and Wong YH (1995) Regulation of multiple effectors by the cloned δ-opioid receptor: Stimulation of phospholipase C and type II adenylyl cyclase. J Neurochem 64:2700-2707.
270. Ueda H, Nozaki M and Satoh M (1991) Multiple opioid receptors and GTP-binding proteins. Comp Biochem Physiol C 98:157-169.
271. Valiquette M, Vu HK, Yue SY, Wahlestedt C and Walker P (1996) Involvement of Trp-284, Val-296 and Val-297 of the human δ-opioid receptor in binding of δ-selective ligands. J Biol Chem 271:18789-18796.
272. 4)deltorphin with δ-opioid receptor subtypes in vivo. Eur J Pharmacol 252:133-137.
273. Varga EV, Li X, Stropova D, Zalewska T, Landsman RS, Knapp RJ, Malatynska E, Kawai K, Mizusura A, Nagase H, Calderon SN, Rice K, Hruby VJ, Roeake WR and Yamamura HI (1996) The third extracellular loop of the human δ opioid receptor determines the selectivity of δ opioid agonists. Mol Pharmacol 50:1619-1624.
274. Vaughn LK, Wire WS, Davis P, Shimohigashi Y, Toth G, Knapp RJ, Hruby VJ, Burks TF and Yamamura HI (1990) Differentiation between rat brain and mouse vas deferens 6 opioid receptors. Eur J Pharmacol 177:99-101.
275. Vaught JL, Mathiasen JR and Raffa RB (1988) 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.
276. Wang JB, Imai Y, Eppler CM, Gregor P, Spivak CE and Uhl GR (1993) μ Opioid receptor: cDNA cloning and expression. Proc Natl Acad Sci USA 90:10230-10234.
277. Wang JB, Johnson PS, Imai Y, Persico AM, Ozenberger BA, Eppler CM and Uhl GR (1994a) cDNA cloning of an orphan opiate receptor gene family member and its splice variant. FEBS Lett 348:75-79.
278. Wang JB, Johnson PS, Persico AM, Hawkins AL, Griffin CA and Uhl GR (1994b) Human μ opioid receptor: cDNA and genomic clones: Pharmacologic characterization and chromosomal assignment. FEBS Lett 338:217-222.
279. Wang JF, Ren MF, Xue JC and Han JS (1993) Cyclic AMP mediates mu and delta but not kappa opioid analgesia in the spinal cord of the rat. Life Sci 52:1955-1960.
280. Wang WW, Shahrestanifar M, Jin J and Howells RD (1995) Studies on μ and δ opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Proc Natl Acad Sci USA 92:12436-12440.
281. Ward SJ, Portoghese PS and Takemori AE (1982) Pharmacological characterization in vivo of the novel opiate β-funaltrexamine. J Pharmacol Exp Ther 220:494-498.
282. Weiss B, Davidkova G and Zhang SP (1997) Antisense strategies in neurobiology. Neurochem Int 31:321-348.
283. Wick MJ, Minnerath SR, Lin W, Elde R, Law PY and Loh HH (1994) Isolation of a novel cDNA encoding a putative membrane receptor with high homology to the cloned μ, δ and κ opioid receptors. Mol Brain Res 27:37-44.
284. Wong C, Su Y, Watkins WD and Chang K (1994) Opioid agonist binding affinity is increased by magnesium in the presence of guanosine diphosphate but decreased by magnesium in the presence of guanyl-5′-yl imidodiphosphate. J Pharmacol Exp Ther 268:653-661.
285. Wüster M, Schulz R and Herz A (1979) Specificity of opioids towards the μ-, δ- and ε-opiate receptors. Neurosci Lett 15:193-198.
286. Xie G, Meng F, Mansour A, Thompson RC, Hoversten MT, Goldatein A, Watson SJ and Akil H (1994) Primary structure and functional expression of a guinea pig κ opioid (dynorphin) receptor. Proc Natl Acad Sci USA 91:3779-3783.
287. 3H]naltrindole binding to δ-opioid receptors in rat brain. Life Sci 50:PLH9-PL124.
288. Yasuda K, Raynor K, Kong H, Breder C, Takeda J, Reisine T and Bell GI (1993) Cloning and functional comparison of κ and δ opioid receptors from mouse brain. Proc Natl Acad Sci USA 90:6736-6740.
289. Zaki PA, Bilsky EJ, Vanderah TW, Lai J, Evans CJ and Porreca F (1996) Opioid receptor types and subtypes: The δ receptor as a model. Annu Rev Pharmacol Toxicol 36:379-401.
290. Zhu J, Chen C, Xue J-C, Kunapuli S, Deriel JK and Liu-Chen L-Y (1995) Cloning of a human κ opioid receptor from the brain. Life Sci 56:201-207.
291. Zhu X, Chunhe W, Cheng Z, Wu Y, Zhou D and Pei G (1997) The carboxyl terminus of mouse δ-opioid receptor is not required for agonist-dependent activation. Biochem Biophys Res Commun 232:513-516.