Background:

IC90: 0.0037 nM for rat SSTR5, 3.6 nM for human SSTR5

Somatostatin receptor type 5?is a?protein?that in humans is encoded by the?SSTR5?gene. Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. SSTR5 is a member of the superfamily of receptors having seven transmembrane segments. BIM 23052 is a linear somatostatin agonist, which displays high binding affinity for the cloned rat sst5?receptor

In vitro: BIM 23052 and the CGP 23996-like compounds bind selectively to rat SSTR5 versus human SSTR1, mouse SSTR2, mouse SSTR3, and human SSTR4.The linear compound BIM 23052 displayed approximately 1000-fold lower affinity for human SSTR5 than for rat SSTR5. Compounds that bind potently to human SSTR5, such as L-362, 855 and BIM 23052, are relatively less potent in GH inhibition [1].

In vivo: BIM 23052 (0.4, 0.8, and 1.2 nmol/rat i.c.) stimulated gastric transit; values of gastric emptying were 65.5 +/- 6.5, 77.4 +/- 5.3, and 77.7 +/- 1.9%, respectively, compared with 43.2 +/-3.2% in i.c. saline group. Intravenous injection of BIM 23052 (0.8 nmol/rat) had no effect. BIM 23052 (0.8 nmol/rat i.c.) action was prevented by subdiaphragmatic vagotomy or atropine [2].

Clinical trial: Up to now, BIM-23052 is still in the preclinical development stage.

参考文献:
[1] O'Carroll AM,?Raynor K,?Lolait SJ,?Reisine T.  Characterization of cloned human somatostatin receptor SSTR5. Mol Pharmacol.?1994 Aug;46(2):291-8.
[2] Martínez V,?Rivier J,?Coy D,?Taché Y.  Intracisternal injection of somatostatin receptor 5-preferring agonists induces a vagal cholinergic stimulation of gastric emptying in rats. J Pharmacol Exp Ther.?2000 Jun;293(3):1099-105.
_x000B__x000B_