778639-31-9Relevant academic research and scientific papers
Discovery of a new class of ghrelin receptor antagonists
Mihalic, Jeffrey T.,Kim, Yong-Jae,Lizarzaburu, Mike,Deignan, Jeff,Wanska, Malgorzata,Yu, Ming,Fu, Jiasheng,Chen, Xi,Zhang, Alex,Connors, Richard,Liang, Lingming,Lindstrom, Michelle,Ma, Ji,Tang, Liang,Dai, Kang,Li, Leping,Chen, Xiaoqi
, p. 2046 - 2051 (2012/04/17)
A series of benzodiazepine antagonists of the human ghrelin receptor GHSR1a were synthesized and their antagonism and metabolic stability were evaluated. The potency of these analogs was determined using a functional aequorin (Euroscreen) luminescent assay measuring the intracellular Ca2+ concentration, and their metabolic stability was measured using an in vitro rat and human S9 hepatocyte assay. These efforts led to the discovery of a potent ghrelin antagonist with good rat pharmacokinetic properties.
