Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.
Kazumi Kondo, Keizo Kan, Yoshihisa Tanada, Masahiko Bando, Tomoichi Shinohara, Muneaki Kurimura, Hidenori Ogawa, Shigeki Nakamura, Takahiro Hirano, Yoshitaka Yamamura, Masaru Kido, Toyoki Mori, Michiaki Tominaga
文献索引：J. Med. Chem. 45 , 3805, (2002)
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摘要
The synthesis and evaluation of both the (R)- and (S)-enantioisomers about the 5-position on a tetrahydro-1H-1-benzazepine derivative were described. The absolute configuration of the (R,R)-isomer (10) was determined by X-ray crystallographic analysis. After evaluation of both enantiomers (compounds R-2, S-2) for binding affinity, cAMP accumulation, and an in vivo study using Brattleboro rats, R-2 showed more potent activity as a V(2) receptor agonist than S-2.