产品描述:
PF-05190457 is an inverse agonist of the growth hormone secretagogue receptor (GHS-R), which is also known as the ghrelin receptor.{51642} It selectively binds to GHS-R (Ki = 4.37 nM) over M2 muscarinic acetylcholine receptors (mAChRs; Ki = 1,950 nM) and the serotonin (5-HT) receptor subtype 5-HT2B (IC50 = 3,700 nM). PF-05190457 (1 µM) increases glucose-induced insulin secretion in primary human pancreatic islets. It potentiates intracellular calcium levels induced by glucagon-like peptide 1 (GLP-1) in isolated dispersed rat islets when used at a concentration of 100 nM.{51643} Intragastric administration of PF-05190457 increases ex vivo vagal nerve firing rate in rats (EC50 = 10.7 nM).