Characterization of CP-122,721; a nonpeptide antagonist of the neurokinin NK1 receptor

Journal of Pharmacology and Experimental Therapeutics

Volumn 277, Issue 2, 1996, Pages 900-908

  McLean, S ^a   Ganong, A ^a   Seymour, P A ^a   Bryce, D K ^a   Crawford, R T ^a   Morrone, J ^a   Reynolds, L S ^a   Schmidt, A W ^a   Zorn, S ^a   Watson, J ^a   Fossa, A ^a   Depasquale, M ^a   Rosen, T ^a,b   Nagahisa, A ^a   Tsuchiya, M ^a   Heym, J ^a  

^a PFIZER INC   (United States)

^b AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (DIPHENYLMETHYL) O [(3,5 BIS TRIFLUOROMETHYLPHENYL)METHYL] 1 AZABICYCLO[2.2.2]OCTAN 3 OL; 2 [1 IMINO 2 (2 METHOXYPHENYL)ETHYL] 7,7 DIPHENYLPERHYDROISOINDOL 4 ONE; 2 BENZHYDRYL 3 (2 METHOXYBENZYLAMINO) 1 AZABICYCLO[2.2.2]OCTANE; 3 (2 METHOXY 5 TRIFLUOROMETHOXYBENZYL)AMINO 2 PHENYLPIPERIDINE; 3 (2 METHOXY 5 TRIFLUOROMETHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; 3 (2 METHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; CAPSAICIN; CP 132687; L 709210; NEUROKININ 1 RECEPTOR ANTAGONIST; NOLPITANTIUM; SUBSTANCE P; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CENTRAL NERVOUS SYSTEM; DOSE RESPONSE; DRUG RECEPTOR BINDING; FEMALE; GUINEA PIG; INTRAVENOUS DRUG ADMINISTRATION; LOCOMOTION; LOCUS CERULEUS; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT;

ANIMALS; BLOOD PRESSURE; CAPILLARY PERMEABILITY; DOGS; FEMALE; GUINEA PIGS; HUMANS; LOCUS COERULEUS; MALE; MOTOR ACTIVITY; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NEUROKININ-1; SALIVATION; SUBSTANCE P;

EID: 12644255691     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (57)

1. AHARONY, D., LITTLE, J., POWELL, S., HOPKINS, B., BUNDELL, K. R., MCPHEAT, R. D., GORDON, R. D., HASSALL, G., HOCKNEY, R., GRIFFIN, R. AND GRAHAM, A.: Pharmacological characterization of a cloned NK-2 (neurokinin A) receptor expressed in a baculovirus/Sf-21 insect cell system. Mol. Pharmacol. 44: 356-363, 1993.
2. APPELL, K. C., FRAGALE, B. J., LOSCIG, J., SINGH, S. AND TOMCZUK, B. E.: Antagonists that demonstrate species differences in neurokinin-1 receptors. Mol. Pharmacol. 41: 772-778, 1992.
3. BARNES, P. J.: Neurogenic inflammation in airways. Int. Arch Allergy. Appl. Immunol. 94: 303-309, 1991.
4. BARUCH, P., ARTAUD, F., GODEHEU, G., BARBEITO, L., GLOWINSKI, J. AND CHERAMY, A.: Substance P and neurokinin A regulate by different mechanisms dopamine release from dendrites and nerve terminals of the nigrostriatal dopaminergic neurons. Neuroscience 25: 889-898, 1988.
5. BOIX, F., MATTIOLI, R., ADAMS, F., HUSTON, J. P. AND SCHWARTING, R. K.: Effects of substance P on extracellular dopamine in neostriatum and nucleus accumbens. Eur. J. Pharmacol. 216: 103-107, 1992.
6. BURNS, L. H. AND KELLEY, A. E.: Neurokinin-alpha injected into the ventral tegmental area elicits a dopamine-dependent behavioral activation in the rat. Pharmacol. Biochem. Behav. 31: 255-263, 1988.
7. CADOR, M., RIVET, J. M., KELLEY, A. E., L. E. MOAL, M. AND STINUS, L.: Substance P, neurotensin and enkephalin injections into the ventral tegmental area: Comparative study on dopamine turnover in several forebrain structures. Brain Res. 486: 357-363, 1989.
8. CASTAIRS, J. R. AND BARNES, P. J.: Autoradiographic mapping of substance P receptors in lung. Eur. J. Pharmacol. 127: 295-296, 1986.
9. CHANG, M. M., LEEMAN, S. E. AND NIALL, H. D.: Amino-acid sequence of substance P. Nature 232: 86-87, 1971.
10. CONSTANTINE, J. W., LEBEL, W. S. AND WOODY, H. A.: Inhibition of tachykinin-induced hypotension in dogs by CP-96,345, a selective blocker of NK-1 receptors. Naunyn Schmiedeberg Arch. Pharmacol. 344: 471-477, 1991
11. CUELLO, A. C. AND KANAZAWA, I.: The distribution of substance P immunoreactive fibers in the rat central nervous system. J. Comp. Neurol. 178: 129-156, 1978.
12. 11]-substance P. Brain Res. 531: 333-337, 1990.
13. DEUTCH, A. Y., MAGGIO, J. E., BANNON, M. J., KALIVAS, P. W., TAM, S. Y., GOLDSTEIN, M. AND ROTH, R. H.: Substance K and substance P differentially modulate mesolimbic and mesocortical systems. Peptides 6: (Suppl. 2), 113-122, 1985.
14. ELLIOTT, P. J., MASON, G. S., STEPHENS-SMITH, M. AND HAGAN, R. M.: Behavioural and biochemical responses following activation of midbrain dopamine pathways by receptor selective neurokinin agonists. Neuropeptides 19: 119-126, 1991.
15. 1 receptor antagonist. Eur. J Pharmacol. 250: 403-413, 1993.
16. 2) receptor. Life Sci. 50: PL101-PL106, 1992.
17. FOSTER, A. C. AND TRIDGETT, R.: Comparison of the binding of radiolabelled neurokinin A and eledoisin in rat cortex synaptic membranes. Br. J. Pharmacol. 94: 602-608, 1988.
18. GARRET, C., CARRUETTE, A., FARDIN, V., MOUSSAOUI, S., PEYRONEL, J. F., BLANCHARD, J. C. AND LADURON, P. M.: Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc. Natl. Acad. Sci. U.S.A. 88: 10208-10212, 1991.
19. GEPPETTI, P., BERTRAND, C., BACCI, E., HUBER, O., AND NADEL, J.: Characterization of tachykinin receptors in ferret trachea by peptide agonists and non-peptide antagonists. Am. J. Physiol. 265: L164-L169, 1993.
20. GLOWINSKI, J., KEMEL, M. L., DESBAN, M., GAUCHY, C., LAVIELLE, S., CHASSAING, G., BEAUJOUAN, J. C. AND TREMBLAY, L.: Distinct presynaptic control of dopamine release in striosomal-enriched and matrix-enriched areas of the rat striatum by selective agonists of NK1, NK2 and NK3 tachykinin receptors. Reg. Peptides 46: 124-128, 1993.
21. GUARD, S., BOYLE, S. J., TANG, K. W., WATLING, K. J., MCKNIGHT, A. T. AND WOODRUFF, G. N.: The interaction of the NK1 receptor antagonist CP-96,345 with L-type calcium channels and its functional consequences. Br. J. Pharmacol. 110: 385-391, 1993.
22. GUARD, S. AND WATSON, S. P.: Tachykinin receptor types: Classification and membrane signalling mechanisms. Neurochem. Int. 18: 149-165, 1993.
23. HELKE, C. J., KRAUSE, J. E., MANTYH, P. W., COUTURE, R. AND BANNON, M. J.: Diversity in mammalian tachykinin peptidergic neurons: Multiple peptides, receptors and regulatory mechanisms. FASEB J. 4: 1606-1615, 1990.
24. KAGE, R., MCGREGOR, G. P., THIM, L. AND CONLON, J. M.: Neuropeptide-γ: A peptide isolated from rabbit intestine that is derived from γ-preprotachykinin. J. Neurochem 50: 1412-1417, 1988.
25. KELLEY, A. E., CADOR, M., STINUS, L. AND L. E. MOAL, M.: Neurotensin, substance P, neurokinin-alpha, and enkephalin: Injection into ventral tegmental area in the rat produces differential effects on operant responding. Psychopharmacol. (Berl). 97: 243-252, 1989
26. KIMURA, S., OKADA, M., SUGITA, Y., KANAZAWA, I. AND MUNEKATA, E.: Novel neuropeptides, neurokinin A and neurokinin B, isolated from porcine spinal cord. Proc. Jpn. Acad. 59B: 101-104, 1983.
27. LOWE, J. A. AND MCLEAN, S.: Tachykinin antagonists. Curr. Pharmaceutical Design, 1: 269-278, 1995.
28. LJUNGDAHL, A., HOKFELT, T. AND NILSSON, G.: Distribution of substance P-like immunoreactivity in the central nervous system of the rat-I. Cell bodies and nerve terminals. Neuroscience 3: 861-943, 1978.
29. LUNDBERG, J. M., SARIA, A., BRODIN, E , MARTLING, C. -L., HOKFELT, T. AND ROSELL, S.: Mucosal oedema and bronchoconstriction induced by irritation of capsaicin-sensitive substance P afferents. In Substance P, ed. by P. Skrabanek and D. Powell, pp. 86-87, Boole Press, Dublin, 1983.
30. MANTYH, P. W.: Substance P and the inflammatory and immune response. Ann. N.Y. Acad. Sci. 632: 263-271, 1991.
31. MCLEAN, S., GANONG, A. H., SEEGER, T. F., BRYCE, D. K. PRATT, K. G., REYNOLDS, L. S., SIOK, C. J., LOWE, J. A. AND HEYM, J.: Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist. Science 251: 437-139, 1991.
32. 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. AND E. T. A. L.,: Pharmacology of CF-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J. Pharmacol. Exp. Ther. 267: 472-479, 1993.
33. MCLEAN, S. AND LOWE, J. A.: Agonist and antagonist receptor binding. In The Tachykinin Receptors, ed. by S. H. Buck, pp. 67-99, Humana Press, Totowa, NJ, 1994.
34. MEINI, S., MAK, J. C. W., ROHDE, J. A. L. AND ROGERS, D. F.: Tachykinin control of ferret airways: Mucus secretion, bronchoconstriction and receptor mapping. Neuropeptides 24: 81-89, 1993.
35. MUSSAP, C. J., GERAGHTY, D. P. AND BURCHER, E.: Tachykinin receptors: a radioligand binding perspective. J. Neurochem. 60: 1987-2009, 1993.
36. Nagahisa, A., Asai, R., Kanai, Y., Murase, A., Tsuchiya-Nakagaki, M., Nakagaki, T., Shieh, T. C. and Taniguchi, K.: Non-specific activity of (±) CP-96,345 in models of pain and inflammation. Regul. Pept. 46: 433-436, 1993.
37. NAKANISHI, S.: Mammalian tachykinin receptors. Ann. Rev. Neurosci. 14: 123-136, 1991.
38. NARANJO, J R. AND DEL RIO, J.: Locomotor activation induced in rodent by substance P and analogues. Blockade of the effect of substance P by metenkephalin antiserum. Neuropharmacology 23: 1167-1171, 1984.
39. OTSUKA, M. AND YOSHIOKA, K.: Neurotransmitter functions of mammalian tachykinins. Physiol. Rev. 73: 230-308, 1993.
40. 2 tachykinin receptor subtypes. Br. J. Pharmacol. 104: 91-96, 1991.
41. PAYAN, D. G., BREWSTER, D. R. AND GOETZL, E. J.: Stereospecific receptors for substance P on cultured human IM-9 lymphoblasts. J. Immunol. 133: 3260-3265, 1984.
42. PAYAN, D. G.: Neuropeptides and inflammation: the role of substance P. Ann. Rev. Med. 40: 341-352, 1989.
43. PERNOW, B.: Role of tachykinins in neurogenic inflammation. J. Immunol. 135: 812s-815s, 1985.
44. RAMNARINE, S. I., HIRAYAMA, Y., BARNES, P. J. AND ROGERS, D. F.: 'Sensory-efferent' neural control of mucus secretion. Characterization using tachykinin receptor antagonists in ferret trachea in vitro. Br. J. Pharmacol. 113: 1183-1190, 1994.
45. REGOLI, D., BOUDON, A. AND FAUCHERE, J. -L.: Receptors and antagonists for substance P and related peptides. Pharmacol. Rev. 46: 551-599, 1994.
46. 2+ channel modulator receptors in brain and skeletal muscle membranes: Differentiation by temperature and dihydropyridines. J. Pharmacol. Exp. Ther 237: 731-738, 1986.
47. RUPNIAK, N. M., BOYCE, S., WILLLAMS, A. R., COOK, G., LONGMORE, J., SEABROOK, G. R., CAESER, M., IVERSEN, S. D. AND HILL, R. G.: Antinociceptive activity of NK1 receptor antagonists: Non-specific effects of racemic RP67580. Br. J. Pharmacol. 110: 1607-1613, 1993.
48. RUPNIAK, N. M. AND JACKSON, A.: Non-specific inhibition of dopamine receptor agonist-induced behaviour by the tachykinin NK1 receptor antagonist CP-99,994 in guinea-pigs. Eur. J. Pharmacol. 262: 171-175, 1994.
49. SAFFROY, M., BEAUJOUAN, J. C., TORRENS, Y., BESSEYRE, J., BERGSTROM, L. AND GLOWINSKI, J.: Localization of tachykinin binding sites (NK1, NK2, NK3 ligands) in the rat brain. Peptides 9: 227-241, 1988.
50. 2+ channels. Eur. J. Pharmacol. 215: 351-352, 1992.
51. SEABROOK, G. R., MAIN, M. J., RAZZAQUE, Z. AND LONGMORE, J.: Differences in the effects of tachykinin NK(1) receptor antagonists- neuronal versus smooth muscle tissues. Eur. J. Pharmacol. 250: 125-131, 1993.
52. 1) receptor. Science 251: 435-437, 1991a.
53. SNIDER, R. M., LONGO, K. P., DROZDA, S. E., LOWE, J. A. AND LEEMAN, S. E.: Effect of CP-96,345, a nonpeptide substance P receptor antagonist, on salivation in rats. Proc. Natl. Acad. Sci. U.S.A. 88: 10042-10044, 1991b.
54. SWAIN, C. J., SEWARD, E. M., SABIN, V., OWEN, S., BAKER, E., CASCIERI, M. A., SADOWSKI, S., STRADER, C. AND BALL, R. G.: Quinuclidine based NK-1 antagonists 2: Determination of the absolute stereochemical requirements. Bio. Org. Chem. Lett. 3: 1703-1706, 1993.
55. TABART, M. AND PEYRONEL, J. -F.: Synthesis of RPR 100893, prototype of a new series of potent and selective nonpeptide NK1 antagonists: The triarylperhydroisoindolols. Bioorg. Med. Chem. Lett. 4: 673-676, 1994.
56. VON EULER, U. S. AND GADDUM, J. H.: An unidentified depressor substance in certain tissue extracts. J. Physiol. (Lond.) 72: 74-86, 1931.
57. WEIHE, E., NOHR, D., MULLER, S., BUCHLER, M., FRIESS, H. AND ZENTEL, H. J.: The tachykinin neuroimmune connection in inflammatory pain. Ann. N.Y. Acad. Sci. 632: 283-295, 1991.