Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 281, Issue 3, 1997, Pages 1303-1311

  Sarau, Henry M ^a   Griswold, Don E ^a   Potts, William ^a   Foley, James J ^a   Schmidt, Dulcie B ^a   Webb, Edward F ^a   Martin, Lenox D ^a   Brawner, Mary E ^a   Elshourbagy, Nabil A ^a   Medhurst, Andrew D ^a   Giardina, Giuseppe A M ^b   Hay, Douglas W P ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b UNIVERSITY OF MILAN   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

NEUROKININ 3 RECEPTOR; TACHYKININ RECEPTOR; TACHYKININ RECEPTOR ANTAGONIST; TALNETANT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD LEVEL; CALCIUM MOBILIZATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DOSE TIME EFFECT RELATION; DRUG BIOAVAILABILITY; DRUG SELECTIVITY; NONHUMAN; PATHOPHYSIOLOGY; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

ANIMALS; CALCIUM; CHO CELLS; CRICETINAE; DOGS; HUMANS; MICE; PIPERIDINES; QUINOLINES; RABBITS; RADIOLIGAND ASSAY; RATS; RECEPTORS, NEUROKININ-3; RECEPTORS, TACHYKININ;

EID: 15144349599     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (46)

1. 9]neurokinin-A binding to NK-2 receptors on hamster urinary bladder membranes. Neuropeptides 23: 121-130, 1992.
2. AIYAR, N., BAKER, E., WU, H.-L., NAMBI, P., EDWARDS, R. M., TRILL, J. T., ELLIS, C. AND BERGSMA, D. J.: Human ATI receptor is a single copy gene: Characterization in a stable cell line. Mol. Cell Biochem. 131: 75-86, 1994.
3. ARENAS, E., ALBKRCH, J., PEREX-NAVARRO, E., SOLSONA, C. AND MARSAL, J.: Neurokinin receptor differentially mediate endogenous acetylcholine release evoked by tachykinins in the neostriatum. J. Neurosci. 11: 2332-2338, 1991.
4. BODEN, P., EDEN, J. M., HODGSON, J., HORWELL, D. C., HOWSON, W., HUGHES, J., MCKNIGHT, A. T., MEECHAM, K., PRITCHARD, M. C., RAPHY, J., RATCLIFFE, G. S., SUMAN-CHAUHAN, N. AND WOODRUFF, G. N.: The rational development of small molecule tachykinin NK-3 receptor selective antagonists: The utilization of a dipeptide chemical library in drug design. Bioorg. Med. Chem. Lett 4: 1679-1684, 1994.
5. BODEN, P., EDEN, J. M., HODGSON, J., HORWELL, D. C., PRITCHARD, M. C., RAPHY, J. AND SUMAN-CHAUHAN, N.: The development of a novel series of non-peptide tachykinin NK-3 receptor selective antagonists. Bioorg. Med. Chem. Lett. 16: 1773-1778, 1995.
6. BUELL, G., SCHULZ, M. F., ARKINSTALL, S. J., MACRY, K., MISSOTTEN, M., ADAMI, N., TALABOT, F. AND KAWASHIMA, E.: Molecular characterization, expression and localization of human neurokinin-3 receptor. FEBS Lett 299: 90-95, 1992.
7. 50) of an enzymatic reaction. Biochem. Pharmacol. 22: 3099-3108, 1973.
8. CHUNG, F.-Z., WU, L.-H., TIAN, Y., VARTANIAN, M. A., LEE, H., BIKKER. J., HUMBLET, C., PRITCHAHD, M. C., RAPHY, J., SUMAN-CHAUHAN, N., HORWELL, D. C., LALWANI, N. D. AND OXENDER, D. L.: Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin 3 receptor. Mol. Pharmacol. 48: 711-716, 1995.
9. DESAI, M. C., LEFKOWITZ, S. L., THADEIO, P. F., LONGO, K. P. AND SNIDER, R. M.: Discovery of potent substance P antagonists: Recognition of the key molecular determinant. J. Med. Chem. 35: 4911-4913, 1992.
10. EMONDS-ALT, X., VILAIN, P., GOULAOCIC, P., PROIETTO, V., VAN BROECK, D., ADVENIER, C., NALINE, E., NELIAT, G., LE FUR, G. AND BRELIERE, J. C.: A potent and selective non-peptide antagonist of the neurokinin A (NK-2) receptor. Life Sci. 50: 101-106, 1992.
11. EMONDS-ALT, X., BICHON, D., DUCOUX, J. P., HEACLME, M., MILOUX, B., PONCELET, M., PROIETTO, V., VAN BROECK, D., VILAIN, P., NELIAT, G., SOUBRIÉ, P., LE FUR, G. AND BRELIERE, J. C. S. R.: 142801, the first potent non-peptide antagonist of the tachykinin NK-3 receptor. Life Sci. 56: PL 27-32, 1995.
12. FONO, T. M., YU, H. AND STRADER, C. D.: Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP96,345 and RP 67580. J. Biol. Chem. 267: 25668-25671, 1992.
13. GERARD, N. P., EDDY, R. L. JR., SHOWS, T. B. AND GERARD, C.: The human neurokinin A (substance K) receptor: Molecular cloning of the gene, chromosome localization, and isolation of cDNA from tracheal and gastric tissues. J. Biol. Chem. 265: 20455-20462, 1990.
14. GERABD, N. P., GARRAWAY, L. A., EDDY, R. L. JR., SHOWS, T. B., IIJIMA, H., PAQUET, J. L. AND GERARD, C.: Human substance P receptor (NK-1): Organization of thr gene, chromosome localization, and functional expression of cDNA clones. Biochem. 30: 10640-10646, 1991.
15. GIARDINA, G. A. M., SARAU, H. M., FARINA, C., MEDHURST, A. D., GRUGNI, M., FOLEY, J. J., RAVEGLIA, L. F., SCHMIDT, D. B., RIGOLIO, R., VASSALLO, M., VECCHIETTI, V. AND HAY, D. W. P.: 2-Phenyl-4-quinolinecarboxamides: A novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor. J. Med. Chem. 39: 2281-2284, 1996.
16. 2+ indicators with greatly improved fluorescence properties. J. Biol. Chem. 260: 3440-3450, 1985.
17. HALL, J. M., MITCHELL, D. AND MORTON, I. K. M.: Neurokinin receptors in the rabbit iris sphincter characterised by novel agonist ligands. Eur. J. Pharmacol. 199: 9-14, 1993.
18. HOLZER, P.: Local effector functions of capsaicin-sensitive sensory nerve endings: involvement of tachykinins, calcitonin gene-related peptide and other neuropeptides. Neuroscience 24: 739-768, 1988.
19. HUANG, R.-R. C., CHEUNG, A. H., MAZINA, K. E., STRADER, C. D. AND FONG, T. M.: cDNA sequence and heterologous expression of the human neurokinin-3 receptor. Biochem. Biophys. Res. Commun. 184: 966-972, 1992.
20. ISHIZUKA, O., MATTIASSON, A. AND ANDERSSON, K.-E.: Tachykinin effects on bladder activity in conscious normal rats. J. Urol. 154: 257-261, 1995.
21. LOWE, J. A. AND SNIDER, R. M.: The role of tachykinins in pulmonary disease. In Annual Reports in Medicinal Chemistry, ed. by J. A. Bristol, vol 28, pp. 99-107, Academic Press,San Diego, CA, 1993.
22. MAGGI, C. A., PATACCHINI, R., ROVERO, P. AND GIACHETTI, A.: Tachykinin receptors and tachykinin receptor antagonists. J. Auton. Pharmacol. 13: 23-93, 1993.
23. MAGGI, C. A., GIACHETTI, A., DEY, R. D. AND SAID, S. I: Neuropeptide as regulators of airway function: Vasoactive intestinal peptide and the tachykinins. Physiol. Rev. 75: 277-322, 1995.
24. MAGGI, C. A.: Tachykinins in the autonomic nervous system. Pharmacol. Res. 33: 161-170, 1996.
25. MAGGIO, J. E.: Tachykinins. Annu. Rev. Neurosci. 11: 13-28, 1988.
26. MANTYH, P. W., VIGNA, S. R. AND MAGGIO, J. E.: Receptor involvement in pathology and disease. In The Tachykinin Receptors, ed. by S. H. Buck, pp. 581-610, Humana Press, Totowa, NJ. 1994.
27. MCLEAN, S., GANONG, A., SEYMOUR, P. A., SNIDER, R. M., DESAI, M. C., ROSKN, T., BRYCE, D. K., LONGO, K. P., REYNOLDS, L. S., ROBINSON, G., SCHMIDT, A. W., SIOK, C. AND HEYM, J.: Pharmacology of CP-99994,a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J. Pharmacol. Exp. Ther. 267: 472-479, 1993.
28. 3 receptors in rabbit isolated iris sphincter muscle. Br. J. Pharmocol 120: 93-101, 1997.
29. NAKANISHI, S.: Mammalian tachykinin receptors. Annu. Rev. Neurosci. 14: 123-136, 1991.
30. NGUYEN-LE, X. K., NGUYEN, Q. T., GOBEIL, F., PHENG, L. H., EMONDS-ALT, X., BRELIERE, J. C. AND REGOLI, D.: Pharmacological characterization of SR 142801: A new non-peptide antagonist of the neurokinin NK-3 receptor. Pharmacology 52: 283-291, 1996.
31. OTSUKA, M. AND YOSHIOKA, K.: Neurotransmitter functions of mammalian tachykinins. Physiol. Rev. 73: 229-308, 1993.
32. OURY-DONAT, F., CARAYON, P., THURNEYSSEN, O., PAILHON, V., EMONDS-ALT, X., SOUBRIÉ, P. AND LE FUR, G.: Functional characterization of the non-peptide neurokinin-3 (NK-3) receptor antagonist, SR 142801 on the human NK-3 receptor expressed in Chinese hamster ovary cells. J. Pharmacol. Exp. Ther. 274: 148-154, 1995.
33. 2 tachykinin receptor subtypes. Br. J. Pharmacol. 104: 91-96, 1991.
34. PATACCHINI, R., BARTHÒ, L., HOLZER, P. AND MAGGI, C. A.: Activity of SR 142801 at peripheral tachykinin receptors. Eur. J. Pharmacol. 278: 17-25. 1995.
35. PAVAN, D. G., MCGILLIS, J. P. AND ORGANIST, M. L.: Binding characteristics and affinity labeling of protein constituents of the human IM-9 lymphoblast receptor for substance P. J. Biol. Chem. 261: 14321-14329, 1986.
36. PETITET, F., BEAUJOUAN, J.-C., SAFFROY, M., TORRENS, Y. AND GLOWINSKI, J.: The nonpeptide NK-2 antagonist SR 48968 is also a NK-3 antagonist in the guinea pig but not in the rat. Biochem. Biophys. Res. Commun. 191: 180-187, 1993a.
37. PETITET, F., BEAUJOUAN, J. C., SAFFROY, M., TORRENS, Y., FARDIN, V. AND GLOWINSKI, J.: NK1 tachykinin receptor in rat and guinea pig brains: Pharmacological and autoradiographical evidence for a species difference. Peptides 14: 551-559, 1993b.
38. 4 receptors in guinea pig ileum. Br. J. Pharmacol. 111: 419-424, 1994.
39. REGOLI, D., DRAPEAU, G., DION, S. AND COUTURE, R.: New selective agonists for neurokinin receptors: Pharmacological tools for receptor characterization. Trends Pharmacol. Sci. 9: 290-295, 1988.
40. ROWLAND, M. AND TOZER, T. N.: Clinical Pharmacokinetics Concepts and Applications, 3rd Ed., Williams & Wilkins, Baltimore, 1995.
41. 7]neurokinin B to the neurokinin-3 receptor. Neuropeptides 24: 317-319, 1993.
42. SCHEMANN, M. AND KAYSER, H.: Effects of tachykinins on myenteric neurons of the guinea pig gastric corpus: involvement of NK-3 receptors. Pfluegers Arch. 419: 566-571, 1991.
43. SNIDER, R. M., CONSTANTINE, S. J. W., LOWE, J. A., LONGO, K. P., LEBEL, W. S., WOODY, H. A., DROZDA, S. E., DESAI, M. C., VINICK, F. J., SPENCER, R. W. AND HESS, H. J.: A potent nonpeptide antagonist of the substance P (NK-1) receptor. Science 251: 435-437, 1991.
44. STOESSL, A. J., DOURISH, C. T. AND IVERSEN, S. D.: The NK-3 tachykinin receptor agonist senktide elicits 5-HT-mediated behavior following central or peripheral administration in mice and rats. Br. J. Pharmacol. 94: 285-287, 1988.
45. STOESSL, A. J., DOURISH, C. T. AND IVERSEN, S. D.: Pharmacological characterization of the behavioural syndrome induced by the NK-3 tachykinin agonist senktide in rodents: Evidence for mediation by endogenous 5-HT. Brain Res. 517: 111-116, 1990.
46. WALSH, D. M., STRATTON, S. C., HARVEY, F. J., BERESFORD, I. J. M. AND HAGAN, R. M.: The anxiolytic-like activity of GR159897, a non-peptide NK-2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacology 121: 186-191, 1995.