Antagonist of neuromedin B receptor,selective
CAS：111857-96-6
分子式：C62H73N11O9S2
分子量：1180.44
纯度：98%
存储：Store at -20°C

Background:

Ki: 49 ±14 nM for neuromedin B-induced endpoint in huNMBR cells

Neuromedin B, a mammalian peptide of the bombesinlike peptide family sharing amino acid homology with its amphibian counterpart ranatensin, elicits a diverse array of biological responses in central and peripheral tissues. BIM 23042 [D-Nal-Cys-Tyr- D-Trp-Lys-Val-Cys-Nal-NH2] is a selective neuromedin B antagonist.

In vitro: BIM 23042 has a l00-fold greater affinity for BB1 receptors than BB2 receptors. The submaximal mobilisation observed with neuromedin B (1 nM) was abolished by BIM 23042 but restored with a subsequently higher concentration of neuromedin B (1 μM). BIM 23042 competitively inhibited neuromedin B-induced endpoint in huNMBR cells with a Ki of 49 ±14 nM [1].

In vivo: In cat upper GI tract, SSocta, at concentrations of 10 mM, did not influence the smooth muscle tone but shifted NMB concentration response to the right yielding (Ki=1.7±0.8 mM). Ssocta inhibited both NMB- and GRP-induced contractions on the esophagus. the NMB-receptor antagonist SSocta had no effect on circular fundic muscle indicating the absence of this receptor subtype on fundus. [2].

Clinical trial: Up to now, BIM 23042 is still in the preclinical development stage.

参考文献:
[1] Ryan RR, Taylor JE, Daniel JL, Cowan A.  Pharmacological profiles of two bombesin analogues in cells transfected with human neuromedin B receptors. Eur J Pharmacol. 1996 Jun 13;306(1-3):307-14.
[2] Milusheva EA,?Kortezova NI,?Mizhorkova ZN,?Papasova M,?Coy DH,?Bálint A,?Vizi ES,?Varga G.  Role of different bombesin receptor subtypes mediating contractile activity in cat upper gastrointestinal tract. Peptides.?1998;19(3):549-56.