Bombesin receptor

IC5Q — 3.4 pM gastrin-releasing peptide/bombesin receptor... 

S., Beglinger, C., and Eberle, A.N. A combinatorial peptoid library for the identification of novel MSH and GRP/ Bombesin receptor ligands. J. Receptor Signal Transduct. Res. 1999, 19, 449-466. 

Millar, J.B., and Rozengur, E. (1990) Chronic desensitization to bombesin by progressive down-regulation of bombesin receptors in Swiss 3T3 cells./. Biol. Chem. 265, 12052-12058. 

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]. 

Semi-rational approaches Four subt)rpes of the bombesin receptor have been identified (gastrin-releasing peptide [GRP] receptor, neuromedin B receptor, the orphan receptor bombesin receptor subtype 3 and bombesin receptor subtype 4). The roles of individual receptor... 

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... 

Varga et al. (1995) determined gastric emptying in rats 5 min after a 3 ml intragastric load of 0.9 % NaCl using phenol red as marker in order to define which bombesin receptors are involved in the delay of gastric emptying by bombesin-like peptides. 

Kroog GS, Jensen RT, Battey JF (1995) Mammalian bombesin receptors. Medicinal Res Rev 75 389 117. 

Ladenheim EE, Jensen RT, Mantey SA, Moran TH (1992) Distinct distributions of two bombesin receptor subtypes in the rat central nervous system. Brain Res 595 168-178. 

Pinnock RD, Reynolds T, Woodruff GN (1994) Different types of bombesin receptors on neurons in the dorsal raphe nucleus and the rostral hypothalamus in rat brain slices in vitro. Brain Res 653 119-124. 

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. 

BBB, blood brain barrier BBI, Bowman-Birk serine protease inhibitor BB-R, bombesin receptor BChE, butyryl cholinesterase BDNF, brain-derived neurotrophic factor BDNF-RTK, brain-derived neurotrophic factor receptor tyrosine kinase aBgTX, a-bungarotoxin BKAS, (3-ketoacyl-ACP synthase BK-R, bradykinin receptor BZ-R, benzodiazepine receptor... 

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