LY303870, a centrally active neurokinin-1 antagonist with a long duration of action

Journal of Pharmacology and Experimental Therapeutics

Volumn 280, Issue 2, 1997, Pages 774-785

  Iyengar, S ^a   Hipskind, P A ^a   Gehlert, D R ^a   Schober, D ^a   Lobb, K L ^a   Nixon, J A ^a   Helton, D R ^a   Kallman, M J ^a   Boucher, S ^b   Couture, R ^b   Li, D L ^a   Simmons, R M A ^a  

^a ELI LILLY AND COMPANY   (United States)

^b UNIVERSITÉ DE MONTRÉAL   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

LANEPITANT; NEUROKININ 1 RECEPTOR AGONIST; TACHYKININ RECEPTOR; TACHYKININ RECEPTOR ANTAGONIST;

ADOLESCENT; ANALGESIC ACTIVITY; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFECT; DRUG POTENCY; DRUG RECEPTOR BINDING; ENANTIOMER; GUINEA PIG; INTRAPERITONEAL DRUG ADMINISTRATION; INTRATHECAL DRUG ADMINISTRATION; MALE; MOUSE; NEUROPHARMACOLOGY; NOCICEPTION; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT; TAIL FLICK TEST;

ANIMALS; DRUG SYNERGISM; ELECTROSHOCK; FORMALDEHYDE; GUINEA PIGS; HUMANS; INDOLES; INJECTIONS, SPINAL; MALE; MICE; MICE, INBRED STRAINS; MOTOR ACTIVITY; PAIN; PEPTIDE FRAGMENTS; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NEUROKININ-1; SPECIES SPECIFICITY; SPINAL CORD; STARTLE REACTION; SUBSTANCE P;

EID: 15444339989     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (106)

1. 125I-substance P binding in the rat spinal cord following constriction injury of the sciatic nerve. Brain Res. 596: 259-268, 1992.
2. ABBOTT, F. V., FRANKLIN, K. B. J. AND WESTBROOK, R. F.: The formalin test: Scoring properties of the first and second phases of the pain response in rats. Pain 60: 91-102, 1995.
3. ACHARD, D., TRUCHON, A. AND PEYRONEL, J.-F.: Perhydrothio-pyranopyroles derivatives: A novel series of potent and selective nonpeptide NK1 antagonists. Bioorg. Med. Chem. Lett. 4: 669-672, 1994.
4. BARBER, R. P., VAUGHN, J. E., SLEMMON, J. R., SALVATERRA, P. M., ROBERTS, E. AND LEEMAN, S. E.: The origin, distribution and synaptic relationships of substance P axons in rat spinal cord. J. Comp. Neurol. 184: 331-352, 1979.
5. BARROW, C. J., DOLEMAN, M. S., BOOBKO, M. A. AND COOPER, R.: Structure determination, pharmacological evaluation, and structure-activity studies of a new cyclic peptide substance P antagonist containing the new amino acid 3-phenyl-β-hydroxytyrosine, isolated from Aspergillus flavipes. J. Med. Chem. 37: 356-363, 1994.
6. BERESFORD, I. J. M., BIRCH, P. J., HAGAN, R. M. AND IRELAND, S. J.: Investigation into species variants in tachykinin NK-1 receptors by use of the non-peptide antagonist, CP-96,345. Br. J. Pharmacol. 104: 292-293, 1991.
7. BIRCH, P. J., BERESFORD, I. J. M., ROGERS, H., HAGAN, R. M., BAILEY, F., HAYES, A. G., HARRISON, S. M. AND IRELAND, S. J.: Profile of the activity of the NK-1 antagonist GR82334 in acute nociceptive tests. Br. J. Pharmacol. 105: 134P, 1992.
8. BRADFORD, M. M.: A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem. 72: 248P, 1976.
9. CELLIER, E., PICARD, P., FAYOLLE, C., HIPSKIND, P. A., IYENGAR, S. AND COUTURE, R.: Peripheral effects of three novel non-peptide NK-1 receptor antagonists in the anesthetized rat. Eur. J. Pharmacol. 318: 377-385, 1996.
10. CODERRE, T. J., FUNDYTUS, M. E., MCKENNA, J. E., DALAL, S. AND MELZACK, R.: The formalin test: A validation of the weighted-scores method of the behavioral pain rating. Pain 54: 43-50, 1993a.
11. CODERRE, T. J., KATZ, J., VACCARINO, A. L. AND MELZACK, R.: Contribution of central plasticity to pathological pain: Review of clinical and experimental evidence. Pain 52: 259-285, 1993b.
12. CODERRE, T. J. AND MELZACK, R.: The contribution of excitatory amino acids to central sensitization and persistent nociception after formalin-induced tissue injury. J. Neurosci. 12: 3665-3670, 1992.
13. COUTURE, R., GUPTA, A., KEROUAC, R., ESCHER, E. AND REGOLI, D.: Spinal actions of substance P analogues on cardiovascular responses in the rat: A structure-activity analysis. Can. J. Physiol. Pharmacol. 65: 412-418, 1987.
14. DAM, T. V. AND QUIRION, R.: Pharmacological characterization and autoradiographic localization of substance P receptors in guinea pig brain. Peptides 7: 855-864, 1986.
15. DANKS, J. A., ROTHMAN, R. B., CASCIERI, M. A., CHICHI, G. G., LIANG, T. AND HERKENHAM, M.: A comparative autoradiographic study of the distributions of substance P and eledoisin binding sites in rat brain. Brain Res. 385: 273-281, 1986.
16. DICKENSEN, A. H. AND SULLIVAN, A. F.: Peripheral origins and central modulation of subcutaneous formalin-induced activity of rat dorsal horn neurons. Neurosci. Lett. 83: 207-211, 1987.
17. DOUGHERTY, P. M., PALECEK, J., PALECKOVA,V. AND WILLIS, W. D.: Neurokinin 1 and 2 antagonists attenuate the responses and NK1 antagonists prevent the sensitization of primate spinothalamic tract neurons after intradermal capsaicin. J. Neurophysiol. 72: 1464-1475, 1994.
18. DUBNER, R.: Pain and hyperalgesia following tissue injury: New mechanisms and new treatments. Pain 44: 213-214, 1991.
19. DUBNER, R. AND RUDA, M. A.: Activity dependent neuronal plasticity following tissue injury and inflammation. Trends Neurosci. 15: 96-103, 1992.
20. DURUISSON, D. AND DENNIS, S. G.: The formalin test: A quantitative study of the analgesic effects of morphine, meperidine and brain stem stimulation in rats and cats. Pain 4: 161-174, 1977.
21. DUGGAN, A. W. AND HENDRY, I. A.: Laminar localization of the sites of release of immunoreactive substance P in the dorsal horn with antibody-coated microelectrodes. Neurosci. Lett. 68: 134-140, 1986.
22. DUNNETT, C. W.: New tables for multiple comparisons with a control. Biometrics 20: 482-491, 1964.
23. 1 receptor antagonist. Eur. J. Pharmacol. 250: 403-413, 1993.
24. FARDIN, V., FOUCAULT, F., BOCK, M. D. AND GARRET, C.: Binding profile of RP 67,580, a new non-peptide SP antagonist: Comparison with CP 96,345. Br. J. Pharmacol. 105: 80P, 1992.
25. 1 receptor antagonist, FK888. Br. J. Pharmacol. 107: 785-789, 1992.
26. GARCES, Y. I., RABITO, S. F., MINSHALL, R. D. AND SAGEN, J.: Lack of potent antinociceptive activity of substance P antagonist CP-96,345 in the spinal cord. Life Sci. 52: 353-360, 1992.
27. GARRET, C., CARRUETTE, A., FARDIN, V., MOUSSAOUI, S., PEYRONEL, J. F., BLANCHARD, J. C. AND LANDURON, P. M.: Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc. Natl. Acad. Sci. U.S.A. 88: 10208-10211, 1991.
28. 3H]-LY303870, a novel, non-peptide radioligand for the NK-1 receptor. J. Neurochem. 66: 1095-1102, 1996.
29. GITTER, B. D., BRUNS, R. F., WATERS, D. C., THRELKELD, P., NIXON, J. L., LOBB, K. A., MASON, N. R., FOREMAN, M., MCNULTY, A., STENGEL, P., SILBAUGH, S. D., SCHOBER, D., GEHLERT, D. R., PHEBUS, L., IYENGAR, S., CALLIGARO, D., REGOLI, D. AND HIPSKIND, P.: Pharmacological characterization of LY303870: A novel, potent and selective non-peptide substance P (NK-1) receptor antagonist. J. Pharmacol. Exp. Biol. 275: 737-744, 1995.
30. GITTER, B. D., WATERS, D. C., BRUNS, R. F., MASON, N. R., NIXON, J. A. AND HOWBERT, J. J.: Species differences in affinities of non-peptide antagonists for substance P receptors. Eur. J. Pharmacol. 187: 237-238, 1991.
31. GO, V. L. W. AND YAKSH, T. L.: Release of substance P from the cat spinal cord. J. Physiol. (Lond.) 391: 141-167, 1987.
32. GRACELY, R. H., LYNCH, S. A. AND BENNETT, G. J.: Painful neuropathy: Altered central processing maintained dynamically by peripheral input. Pain 51: 2175-2194, 1992.
33. GUARD, S. AND WATSON, S. P.: Tachykinin receptor subtypes: Classification and membrane signalling mechanisms. Neurochem. Int. 18: 149-165, 1991.
34. HEAPY, C. G., JAMIESON, A. AND RUSSELL, N. J. W.: Afferent C-fibre and a-delta activity in models of inflammation. Br. J. Pharmacol. 90: 164P, 1987.
35. HELTON, D. R., BERGER, J. E., CZACHURA, J. F., RASMUSSEN, K. AND KALLMAN, M. J.: Central nervous system characterization of the new cholecystokinin-B antagonist LY288513. Pharmacol. Biochem. Behav. 53: 493-502, 1996a.
36. HELTON, D. R., ZIMMERMAN, J. L., JONES, T. W., TURK, J. A. AND KALLMAN, M. J.: General pharmacology of [Lys(B28),Pro(B29)] in animals. Drug Res. 46: 91-97, 1996b.
37. HENRY, J. L.: Effects of substance P on functionally identified units in cat spinal cord. Brain Res. 114: 439-451, 1976.
38. HENRY, J. L.: Discussion of nomenclature for tachykinin receptors. In Substance P and Neurokinins, ed. by J. L. Henry, R. Couture, A. C. Cuello, G. Pelletier, R. Quirion and D. Regoli, pp. 17-18, Springer-Verlag, New York, 1987.
39. HENRY, J. L.: Substance P and inflammatory pain: Potential of substance P antagonists as analgesics. In Inflammatory Disease Therapy: Preclinical & Clinical Developments. Ed. by Robert J. Bonney, pp. 75-87. Birkhäuser Verlag, Basel, 1993.
40. HERSHEY, A. D. AND KRAUSE, J. E.: Molecular characterization of a functional cDNA encoding for rat substance P receptor. Science (Wash, DC) 247: 958-962, 1990.
41. HIPSKIND, P. A., HOWBERT, J. J., BRUNS, R. F., FOREMAN, M. M., GEHLERT, D. R., IYENGAR, S., PHEBUS, L. A., REGOLI, D., CHO, S. S. Y., CROWELL, T. A., JOHNSON, K. W., KRUSHINSKI, D. J. H., LI, D. L., LOBB, K. L., MEHL, B. S., NIXON, J. A., SIMMONS, R. M., THRELKELD, P. G., WATERS, D. C. AND GITTER, B. D.: 3-Ary-1,2-diacetaminidopropane derivatives as novel and potent NK-1 receptor antagonists. J. Med. Chem. 39: 736-748, 1996.
42. HÖKFELT, T., KELLERTH, J.-O., NILSSON, G. AND PERNOW, B.: Substance P: Localization in the central nervous system and in some primary sensory neurons. Science (Wash. DC) 190: 889-890, 1975.
43. HYLDEN, J. L., NAHIN, R. L., TRAUB, R. J. AND DUBNER, R.: Expansion of receptive fields of spinal lamina I projection neurons in rats with unilateral adjuvant-induced inflammation: The contribution of dorsal horn mechanisms. Pain 37: 229-243, 1989.
44. HYLDEN, J. L. K. AND WILCOX, G. L.: Intrathecal substance P elicits a caudally directed biting and scratching behavior in mice. Brain Res. 217: 212-215, 1981.
45. IRWIN, S.: Comprehensive observational assessment. Ia. A systematic, quantitative procedure for assessing the behavioral and physiological state of the mouse. Psychopharmacologia 13: 222-257, 1968.
46. JESSELL, T., TSUNOO, A., KANAZAWA, I. AND OTSUKA, M.: Substance P: Depletion in the dorsal horn of rat spinal cord after section of the peripheral processes of primary sensory neurons. Brain Res. 168: 247-259, 1979.
47. KURAISHI, Y., HIROTA, N., SATO, Y., HANASHIMA, N., TAKAGI, H. AND SATOH, M.: Stimulus specificity of peripherally evoked substance P release from the rabbit dorsal horn in situ. Neuroscience 30: 241-250, 1989.
48. KURAISHI, Y., HIROTA, N., SUGIMOTO, M., SATOH, M. AND TAKAGI, H.: Effects of morphine on noxious stimuli-induced release of substance P from rabbit dorsal horn in vivo. Life Sci. 33: suppl. 1, 693-696, 1983.
49. LAMOTTE, R. H., LUNDBERG, L. E. AND TOREBJORK, H. E.: Pain, hyperalgesia and activity in nociceptive C units in humans after intradermal injection of capsaicin. J. Physiol. (Lond.) 448: 749-764, 1992.
50. LANEUVILLE, O., DORAIS, J. AND COUTURE, R.: Characterization of the effects produced by neurokinins and three agonists selective for neurokinin subtypes in a spinal nociceptive reflex of the rat. Life Sci. 42: 1295-1305, 1988.
51. MACLEOD, A. M., MERCHANT, K. J., CASCIERI, M. A., SADOWSKI, S., BER, E., SWAIN, C. J. AND BAKER, R.: N-Acyl-L-tryptophan benzyl esters: Potent substance P receptor antagonists. J. Med. Chem. 36: 2044-2045, 1993.
52. MAGGI, C. A., PATACHINNI, R., ROVERO, P. AND GIACHETTI, A.: Tachykinin receptors and tachykinin receptor antagonists. J. Auton. Pharmacol. 13: 23-93, 1993.
53. MANTYH, P. W., DEMASTER, E., MALHOTRA, A., GHILARDI, J. R., ROGERS, S. D., MANTYH, C. R., LIU, H., BASBAUM, A. I., VIGNA, S. R., MAGGIO, J. E. AND SIMONE, D. A.: Receptor endocytosis and dendrite reshaping in spinal neurons after somatosensory stimulation. Science (Wash. DC) 268: 1629-1632, 1995.
54. MATSUMURA, H., SAKURADA, T., KARA, A., SAKURADA, S. AND KISARA, K.: Characterization of the hyperalgesic effect induced by intrathecal injection of substance P. Neuropharmacology 24: 421-426, 1985.
55. MCCARSON, K. E. AND GOLDSTEIN, B. D.: Time course of the alteration in dorsal horn substance P levels following formalin: Blockade by naloxone. Pain 41: 95-100, 1990.
56. MCCARSON, K. E. AND GOLDSTEIN, B. D.: Release of substance P into the superficial dorsal horn following nociceptive activation of the hindpaw of the rat. Brain Res. 568: 109-115, 1991.
57. MCCARSON, K. E. AND KRAUSE, J. E.: Regulation of tachykinin receptor mRNA expression in rat dorsal horn during nociception. J. Neurosci. 14: 712-720, 1994.
58. MCCARSON, K. E. AND KRAUSE, J. E.: The formalin induced expression of tachykinin peptide and neurokinin receptor messenger RNAs in rat sensory ganglia and spinal cord is modulated by opiate preadministration. Neuroscience 64: 729-739, 1995.
59. MCLEAN, S., GANONG, A., SEYMOUR, P. A., SNIDER, R. M., DESAI, M. C., ROSEN, T., BRYCE, D. K., LONGO, K. P., REYNOLDS, L. S., ROBINSON, G., SCHMIDT, A. W., SIOK, C. AND HEYM, J.: Pharmacology of CP-99,994; A nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J. Pharmacol. Exp. Ther. 267: 472-479, 1993.
60. MILLS, S. G., WU, M. T., MACCOSS, M., BUDHU, R., DORN, C. P., JR., CASCIERI, M. A., SADOWSKI, S., STRADER, C. D. AND GREENLEE, W. J.: 1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists, Bioorg. Med. Chem. Lett. 3: 2707-2712, 1993.
61. MORIMOTO, H., MURAI, M., MAEDA, Y., YAMAOKA, M., NISHIKAWA, M., KIYOTOH, S. AND FUJH, T.: FK224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity. J. Pharmacol. Exp. Ther. 262: 398-402, 1992.
62. MOUSSAOUI, S. M., HERMANS, E., MATHIEU, A. M., BONICI, B., CLERC, F., GUINET, F., GARRET, C. AND LANDURON, P. M.: Polyclonal antibodies against the rat NK-1 receptor: Characterization and localization in the spinal cord. Mol. Neurosci. Neurorep. 3: 1073-1076, 1992.
63. NAGAHISA, A., ASAI, R., KANAL, Y., MURASE, A., TSUCHIYA-NAKAGAKI, M., NAKAGAKI, T., SIEH, T.-C. AND TANIGUCHI, K.: Non-specific activity of (±)-CP 96,345 in models of pain and inflammation. Br. J. Pharmacol. 107: 273-275, 1992.
64. NAKANISHI, S.: Mammalian tachykinin receptors. Annu. Rev. Neurosci. 14: 123-136, 1991.
65. NOGUCHI, K., MORITA, Y., KIYAMA, H., ONO, K. AND TOHYAMA, M.: A noxious stimulus induces the preprotachykinin A gene expression in the dorsal root ganglion: A quantitative study using in situ hybridization histochemistry. Mol. Brain Res. 464: 31-35, 1988.
66. NOGUCHI, K. AND RUDA, M. A.: Gene regulation in an ascending nociceptive pathway: Inflammation-induced increase in preprotachykinin mRNA in rat lamina I spinal projection neurons. J. Neurosci. 12: 2563-2572, 1992.
67. OTSUKA, M. AND YANAGISAWA, M.: Pain and neurotransmitters. Cell. Mol, Neurobiol. 10: 293-302, 1990.
68. OTSUKA, M. AND YOSHIOKA, K.: Neurotransmitter functions of mammalian tachykinins. Physiol. Rev. 73: 229-308, 1993.
69. PAPIR-KIRCHELI, D., FREY, J., LAUFER, R., GILON, C., CHOREV, M., LINGER, Z. AND DEVOR, M.: Behavioural effects of receptor-specific substance P agonists. Pain 31: 263-276, 1987.
70. PICARD, P., BOUCHER, S., REGOLI, D., GITTER, B., HOWBERT, J. J. AND COUTURE, R.: Use of non-peptide tachykinin antagonists to substantiate the involvement of NK1 and NK2 receptors in a spinal nociceptive reflex in rat. Eur. J. Pharmacol. 232: 255-261, 1993.
71. PIERCEY, M. F., DOBRY, P. J. K., SCHROEDBR, L. A. AND EINSPAHR, J.: Behavioral evidence that substance P may be a spinal cord sensory neurotransmitter. Brain Res. 210: 407-412, 1981.
72. RADHAKRISHNAN, V. AND HENRY, J. L.: Novel substance P antagonist, CP-96, 345., blocks responses of cat spinal dorsal horn neuron. Neurosci. Lett. 132: 39-42, 1991.
73. RADHAKRISHNAN, V. AND HENRY, J. L.: Antagonism of nociceptive responses of cat spinal dorsal horn neurons in viro by the NK-1 antagonists CP-96,345 and CP-99,994 but not by CP-96,344. Neuroscience 64: 943-958, 1995.
74. RANDIC, M. AND MILENTIC, V.: Effect of substance P in cat dorsal horn neurons activated by noxious stimuli. Brain Res. 128: 164-167, 1977.
75. RANG, H. P. AND URBAN, L.: New molecules in analgesia. Br. J. Anaesth. 75: 145-156, 1995.
76. REGOLI, D., BOUDON, A. AND FAUCHERE, J. L.: Receptors and antagonists for substance P and related peptides. Pharmacol. Rev. 46: 551-600, 1994.
77. SAFFROY, M., BEAULOUON, J. C., TORRENS, Y., BESSEYRE, J., BERGSTROM, L. AND GLOWINSKI, J.: Localization of tachykinin binding sites (NK-1, NK-2 and NK-3 ligands) in the rat brain. Peptides 9: 227-241, 1988.
78. SAKURADA, T., KATSUMATA, K., YOGO, H., TAN-NO, K., SAKURADA, S., OHBA, M. AND KISARA, K.: Neurokinin-1 receptor antagonist, sendide, exhibits antinociceptive activity in the formalin test. Pain 60: 175-180, 1995.
79. SAKURADA, T., YAMADA, T., TAN-NO, K., MANOME, Y., SAKURADA, S., KISARA, K AND OHBA, M.: Differential effects of substance P analogs on NK-1 receptor agonists in the mouse spinal cord. J. Pharmacol. Exp. Ther. 259: 205-210, 1991.
80. 1 receptor antagonist, and morphine in the capsaicin test. Brain Res. 649: 319-322, 1994.
81. SCHÄFER, M. K., NOHR, D., KRAUSE, J. E. AND WEIHE, E.: Inflammation-induced upregulation of NK1 receptor mRNA in dorsal horn neurons. NeuroReport 4: 1007-1010, 1993.
82. SCHAIBLE, H. G., JARROTT, B., HOPE, P. J. AND DUGGAN, A. W.: Release of immunoreactive substance P in the spinal cord during development of acute arthritis in the knee joint of the cat: A study with antibody microprobes. Brain Res. 529: 214-223, 1990.
83. SEGUIN, L., LE MAROUILLE-GIRARDON, S. AND MILLIAN, M. J.: Antinociceptive profiles of non-peptidergic neurokinin 1 and neurokinin 2 receptor antagonists: A comparison to other classes of antinociceptive agents. Pain 61: 325-343, 1995.
84. SHIBATA, M., OHKUBO, T., TAKAHASHI, H. AND INOKI, R.: Modified formalin test: Characteristic biphasic pain response. Pain 38: 347-352, 1989.
85. SHULTS, C. W., QUIRION, R., CHRONWALL, B., CHASE, T. N. AND O'DONOHUE, T. L.: A comparison of the anatomical distribution of substance P receptors in the rat central nervous system. Peptides 5: 1097-1128, 1984.
86. SLUKA, K. A. AND WESTLUND, K. N.: Spinal cord amino acid release and content in an arthritis model: The effects of pretreatment with non-NMDA, NMDA and NK-1 receptor antagonists. Brain Res. 627: 89-103, 1993.
87. 1 receptor antagonist, CP-99,994, in antinociceptive tests in rat, mouse and gerbil. Eur. J. Pharmacol. 271: 481-487, 1994.
88. 1) receptor. Science (Wash. DC) 251: 435-437, 1991.
89. TABART, M. AND PEYRONEL, J.-F.: Synthesis of RPR-100893, prototype of a new series of potent and selective non-peptide NK1 antagonists: The triarylperhydroisomdolols. Bioorg. Med. Chem. Lett. 4: 673-676, 1994.
90. TAKAHASHI, K., SAKURADA, T., SAKURADA, S., KUWAHARA, H., YONEZAWA, A., ANDO, R. AND KISARA. K.: Behavioural characterization of substance P induced nociceptive response in mice. Neuropharmacology 26: 1289-1293, 1987.
91. TJØLSEN, A., BERGE, O. G., HUNRKAAR, S., ROSLAND, J. H. AND HOLE, K.: The formalin test: An evaluation of the method. Pain 51: 5-17, 1992.
92. TODA, T. AND HAYASHI, S.: The inhibitory effect of substance-P antagonist, CP-96,345, on the late discharges of nociceptive neurons in the rat superficial spinal dorsal horn. Neurosci. Lett. 158: 36-38, 1993.
93. TOHEBJORK, H. E., LUNDERBERG, L. E. AND LAMOTTE, R. H.: Central changes in processing of mechanoreceptive input in capsaicin-induced secondary hyperalgesia in humans. J. Physiol. (Lond.) 448: 765-780, 1992.
94. URBAN, L., THOMPSON, S. W., NAGY, I. AND DRAY, A.: Hyperexcitability in the spinal dorsal horn: Cooperation of neuropeptides and excitatory amino acids. In Cellular Mechanisms of Sensory Processing, ed. by L. Urban, pp. 379-399, Springer-Verlag, Berlin, 1994.
95. VAUGHT, J. L.: Substance P antagonists and analgesia: A review of the hypothesis. Life Sci. 43: 1419-1431, 1988.
96. WATLING, K. J., GUARD, S., HOWSON, W. AND WALTON, L.: Inhibition of binding to tachykinin NK-1 receptor sites in rat, guinea pig and human brain by the nonpeptide substance P antagonist CP-96,345. Br. J. Pharmacol. 104: 27P, 1991.
97. WHEELER-ACETO, H., PORRECA, F. AND COWAN, A.: The rat paw formalin test Comparison of noxious agents. Pain 40: 229-238, 1990.
98. WILCOX, G. L.: Excitatory neurotransmitters and pain. In Pain Research and Clinical Management, vol. 4, Proceedings of the VIth World Congress on Pain, ed. by M. R. Bond, J. E. Charlton and C. J. Woolf, pp. 97-117, Elsevier. Amsterdam, 1991.
99. WOOLF, C. J.: Evidence for a central component of post-injury pain hypersensitivity. Nature (Lond.) 306: 686-688, 1983.
100. XU, X. J., DAALSGARD, C. J. AND WISENFELD-HALLIN, Z.: Intrathecal CP-96,345 blocks reflex facilitation induced in rats by substance P and C-fiber conditioning stimulation. Eur. J. Pharmacol. 216: 337-344, 1992.
101. YAKSH, T. L.: Substance P release from knee joint afferent terminals: Modulation by opioids. Brain Res. 458: 319-324, 1988.
102. YAMAMOTO, T. AND YAKSH, T. L.: Stereospecific effects of a non-peptide NK-1 Selective antagonist, CP-96,345: Antinociception in the absence of motor dysfunction. Life Sci. 49: 1955-1963, 1991.
103. YASHPAL, K., DAM, T. V. AND QUIRION, R.: Quantitative autoradiographic distribution of multiple neurokinin binding sites in rat spinal cord. Brain Res. 506: 259-266, 1990.
104. YASHPAL, K., DAM, T. V. AND QUIRION, R.: Effects of dorsal rhizotomy on neurokinin receptor subtypes in the rat spinal cord: A quantitative autoradiographic study. Brain Res. 552: 240-247, 1991.
105. YASHPAL, K., RADHAKRISHNAN, V., CODERRE, T. J. Q. AND HENRY, J. L.: CP-96,345 but not its stereoisomer, CP-96,344, blocks the nociceptive responses to intrathecally administered substance P and to noxious thermal and chemical stimuli in the rat. Neuroscience 52: 1039-1047, 1993.
106. YASHPAL, K., WRIGHT, D. M. AND HENRY, J. L.: Substance-P reduces tail-flick latency: Implications for chronic pain syndromes. Pain 14: 155-167, 1982.