2-Acylamino-4, 6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats

…, A Kiba, M Kusaka, S Matsumoto, M Yamaguchi…

Index: Kobayashi, Toshitake; Sasaki, Satoshi; Tomita, Naoki; Fukui, Seiji; Nakayama, Masaharu; Kiba, Atsushi; Kusaka, Masami; Matsumoto, Shin-Ichi; Yamaguchi, Masashi; Itoh, Fumio; Baba, Atsuo Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 5157 - 5171

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Citation Number: 18

Abstract

GPR54 is a G protein-coupled receptor (GPCR) which was formerly an orphan receptor. Recent functional study of GPR54 revealed that the receptor plays an essential role to modulate sex-hormones including GnRH. Thus, antagonists of GPR54 are expected to be novel drugs for sex-hormone dependent diseases such as prostate cancer or endometriosis. We recently reported 2-acylamino-4, 6-diphenylpyridines as the first small molecule ...