ssr-149415 and Disease-Models--Animal

ssr-149415 has been researched along with Disease-Models--Animal* in 1 studies

Other Studies

1 other study(ies) available for ssr-149415 and Disease-Models--Animal

Article	Year
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. Bioorganic & medicinal chemistry letters, 2011, Jun-15, Volume: 21, Issue:12 Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity. Topics: Animals; Antidepressive Agents; Antidiuretic Hormone Receptor Antagonists; Disease Models, Animal; Indoles; Molecular Structure; Oxindoles; Protein Binding; Rats	2011

Article

Year

Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.

Bioorganic & medicinal chemistry letters, 2011, Jun-15, Volume: 21, Issue:12

Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity.

Topics: Animals; Antidepressive Agents; Antidiuretic Hormone Receptor Antagonists; Disease Models, Animal; Indoles; Molecular Structure; Oxindoles; Protein Binding; Rats

2011