Peer-reviewed veterinary case report
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2011
- Authors:
- Oost, Thorsten et al.
- Affiliation:
- Abbott · Germany
- Species:
- rodent
Abstract
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.
Find similar cases for your pet
PetCaseFinder finds other peer-reviewed reports of pets with the same symptoms, plus a plain-English summary of what was tried across them.
Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/21605973/