Bombesin receptor antagonists

Aziridine cleavage based on an Sn2 reaction was used for the synthesis of peptides bearing E alkene dipeptide isosteres, a novel class of potent bombesin receptor antagonists [62]. Treatment of the vinylaziridine 86 (Scheme 9.19) with isobutyl and isopentyl magnesiocyanocuprates in THF at —78 °C for 30 min. stereospecifi-cally gave the desired E alkene isosteres 87 in high isolated yields [63]. 

Moody TW, Jensen RT. Bombesin receptor antagonists. Drugs Future 1998 23 1305-15. 

VI. BOMBESIN RECEPTOR ANTAGONISTS, KUWANONS G (1) AND H (2), ISOLATED FROM MORUS SPECIES... 

Pinski J, Yano T, Schally AV (1992) Inhibitory efffects of the new bombesin receptor antagonist RC-3095 on the luteinizing hormone release in rats. Neuroendocrinology 56 831-837. 

At BB2 (GRP-preferring) receptors, selective antagonists include the peptides [DPhe ]-BB6, 3 ethyl ester, AC-GRP20.26 ethyl ester, the pseudo-peptides [DPhe ,Cpa -t rl3-14]-BB6,4, and l-naphthoyl-[DAIa, DPro ,t f ]GRP2o.27, and recently the nonpeptides kuwanon G and H (isolated from mulberry). Houben, H. er a/. (1991) Bombesin receptor antagonists and their use in the evaluation of paracrine and autocrine intercellular communication. Front. Harm. Res.. 19.176-195. 

Jensen. R.T. etal. (1991) Progress in the development of potent bombesin receptor antagonists. Trends Pharmacol. ScL, 12.13-19. 

Gastrin receptor antagonists and gastrin-releasing peptide antagonists have now been developed for experimental use. but it is not yet clear if either will be useful clinically. See BOMBESIN RECEPTOR ANTAGONISTS) CHOLECYSTOKININ RECEPTOR ANTAGONISTS. 

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