BIM 23127

Ki: 20.9 nM for neuromedin B receptors

Bombesin (BN) belongs to a family of neuropeptides whose members, as well as their respective receptors, are widely distributed throughout the mammalian central nervous system (CNS). BN and its related peptides modulate behaviors such as spontaneous activities and feeding. BIM 23127 (D-Nal-cyclo[Cys-Tyr-D-Trp-Orn-Val-Cys]-Nal-NH2) is a neuromedin B receptor antagonist.

In vitro: BIM 23127 was reported to potenly give antagonist effect on neuromedin B receptor (Ki = 20.9 nM). In addition, BIM 23127 was also found to be a selective neuromedin B receptor antagonist (> 10000 nM for gastrin-releasing peptide receptors) [2].

In vivo: Prior administration of 100 nmol/kg of BIM 23127 completely blocked the glucose intake suppression produced by neuromedin B. BIM 23127 also completely blocked suppression of intake produced by neuromedin B rather than by neuromedin C. These results suggest an independent role for neuromedin B receptors in suppression of food intake by bombesin-like peptides [3].

Clinical trial: Up to now, BIM 23127 is still in the preclinical development stage.

Reference:
[1] Ladenheim EE, Taylor JE, Coy DH, Moran TH.  Blockade of feeding inhibition by neuromedin B using a selective receptor antagonist. Eur J Pharmacol. 1994 Dec 12;271(1):R7-9.