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Characterization of Orally Active Nonpeptide Vasopressin V<INF>2</INF> 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
- Source :
- Journal of Medicinal Chemistry; August 2002, Vol. 45 Issue: 17 p3805-3808, 4p
- Publication Year :
- 2002
-
Abstract
- 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 (<BO>10</BO>) was determined by X-ray crystallographic analysis. After evaluation of both enantiomers (compounds R-<BO>2</BO>, S-<BO>2</BO>) for binding affinity, cAMP accumulation, and an in vivo study using Brattleboro rats, R-<BO>2</BO> showed more potent activity as a V<INF>2</INF> receptor agonist than S-<BO>2</BO>.
Details
- Language :
- English
- ISSN :
- 00222623 and 15204804
- Volume :
- 45
- Issue :
- 17
- Database :
- Supplemental Index
- Journal :
- Journal of Medicinal Chemistry
- Publication Type :
- Periodical
- Accession number :
- ejs2356384
- Full Text :
- https://doi.org/10.1021/jm020133q