Autor: |
Kondo K; Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Company, 463-10 Kagasuno Kawauchi-cho, Tokushima 771-0192, Japan. k_kondo@research.otsuka.co.jp, Kan K, Tanada Y, Bando M, Shinohara T, Kurimura M, Ogawa H, Nakamura S, Hirano T, Yamamura Y, Kido M, Mori T, Tominaga M |
Jazyk: |
angličtina |
Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2002 Aug 15; Vol. 45 (17), pp. 3805-8. |
DOI: |
10.1021/jm020133q |
Abstrakt: |
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. |
Databáze: |
MEDLINE |
Externí odkaz: |
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