Abstract
In the past 25 years, a large number of biologically active peptides has been identified in both brain and peripheral tissues. However, our understanding of their role in physiology and disease has been often undermined by the lack of potent and selective antagonists.
This review represents a summary of the work presented during the IUPHAR 94 in the symposium on “Peptide receptor antagonists”. The section on cholecystokinin antagonists was presented by L.L. Iverson (Merck Sharp and Dohme, Harlow, UK) and J.D. Gardner (St. Louis University, MO, USA). The section on tachykinin antagonists was presented by R.M. Snider (Pfizer, Groton, CT, USA and Burroughs Wellcome Company Research Triangle Park, NC, USA) and J.M. Lundberg (Karolinska Institute, Stockholm, Sweden). The section on neurotensin antagonists was presented by D. Gully (Sanofi Recherche, Toulouse, France) and P. Kitabgi (IPMC CNRS, Sophia-Antipolis, Valbonne, France).
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References
Chang RS, Lotti VJ, Monaghan J, Birnbaum J, Stapley EO, Goetz MA et al A potent non-peptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus. Science 1985; 230: 177–179.
Patel S, Smith AJ, Chapman KL, Fletcher AE, Kemp JA, Marshall GR et al. Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B gastrin receptor antagonist with high affinity in vitro and high potency in vivo, Mol. Pharmacol. 1994; 46: 943–948.
Talkad VD, Fortune KP, Pollo DA, Shah GN, Wank SA, Gardner JD. Direct demonstration of three different states of the pancreatic cholecystokinin receptor. Proc. Natl. Acad. Sci. USA 1994; 91: 1868–1872.
Delay-Goyet P, Franco-Cereceda A, Golsalves SF, Clingan CA, Lowe III JA, Lundberg JM. CP 96345 antagonism of NK1 receptors and smoke-induced protein extravasation is unrelated to its cardiovascular effects. Eur. J. Pharmacol. 1992; 222: 213–218.
Delay-Goyet P, Satoh H, Lundberg JM. Differences in the potency of CP 96345 and RP 67580, two new non-peptide antagonists selective for NK1 receptors in inhibiting responses evoked by stimulation of sensory nerves. Regul. Pept. 1993; 46: 304–306.
Satoh H, Lou YP, Lundberg JM. Inhibitory effects of capsazepine and SR 48968 on citric acid-induced bronchoconstriction in guinea-pigs. Eur. J. Pharmacol. 1993; 236: 367–372.
Kitabgi P, Nemeroff CB, editors. The neurobiology of neurotensin. Ann. New York Acad. Sci. Vol. 668, 1992, pp. 1–374.
Gully D, Canton M, Boigegrain R, Jeanjean F, Molimard JC, Poncelet M et al. Biochemical and pharmacological profile of a potent and selective non-peptide antagonist of neurotensin receptor. Proc. Natl. Acad. Sci. USA 1993; 90: 65–69.
Dubuc I, Costentin J, Terranova JP, Barnouin MC, Soubrié P, Le Fur G et al. Br. J. Pharmacol. 1994; 112: 352–354.
Kitabgi P. Effects of neurotensin on intestinal smooth muscle: application to the study of structure-activity relationships. Ann. N.Y. Acad. Sci. 1982; 400: 37–52.
Labbé-Jullié C, Deschaintres S, Gully D, Le Fur G, Kitabgi P. Effect of the non-peptide neurotensin antagonist, SR 48692, and two enantiomeric analogs, SR 48527 and SR 49711, on neurotensin binding and contractile responses in guinea-pig ileum and colon. J. Pharmacol, exp. Ther. 1994; 271: 267–276.
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© 1995 Birkhäuser Verlag Basel/Switzerland
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Rostene, W., Le Fur, G. (1995). Peptide Receptor Antagonists. In: Cuello, A.C., Collier, B. (eds) Pharmacological Sciences: Perspectives for Research and Therapy in the Late 1990s. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7218-8_4
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DOI: https://doi.org/10.1007/978-3-0348-7218-8_4
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