BIM-23027

Names

[ CAS No. ]:
78981-49-4

[ Name ]:
BIM-23027

Biological Activity

[Description]:

BIM-23027 is a selective agonist of sst2 receptor (EC50=0.32 nM), with similar effect to somatostatin (SRIF), a cyclic tetradecapeptide. BIM-23027 stimulates dopamine release, which is mediated by a Glu-dependent mechanism[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

EC50: 0.32 nM (sst2)[2]


[In Vitro]

BIM-23027 (10,50 和 100 nM; 90分钟) 显著增加多巴胺水平[1]。 BIM-23027 (50 nM; 100 nM SRIF 处理前 15 分钟孵育) 显著减弱了天然肽的作用[1]。 BIM-23027 (30 nM; 30 分钟) 卡威酚刺激的基底鳞状细胞增加 60-70%，EC50 为 0.29 nM[2]。 BIM-23027 与大鼠结肠粘膜 [125I]Tyr11-SRIF 结合位点的亚群相互作用[2]。

[References]

[1]. Hathway GJ, et al. Evidence that somatostatin sst2 receptors mediate striatal dopamine release. Br J Pharmacol. 1999 Nov;128(6):1346-52.  

[2]. McKeen ES, et al. Somatostatin receptors mediating inhibition of basal and stimulated electrogenic ion transport in rat isolated distal colonic mucosa. Naunyn Schmiedebergs Arch Pharmacol. 1995 Oct;352(4):402-11.  

Chemical & Physical Properties

[ Molecular Formula ]:
C43H54N8O7

[ Molecular Weight ]:
794.94

Related Compounds