Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat

Autor:	Sajad Mohammed, George Hynd, Nicholas C. Ray, Hazel Hunt, Shahadat Ahmed, Steve Daly, Peter Lockey, Gerry Buckley, Robert Roe, Jon Sutton, Robin D. Clark, Christine Blasey, Joe Belanoff, Elizabeth O'connor
Rok vydání:	2012
Předmět:	Olanzapine medicine.medical_specialty Clinical Biochemistry Administration Oral Pharmaceutical Science Pharmacology Weight Gain Biochemistry Rats Sprague-Dawley Benzodiazepines Structure-Activity Relationship chemistry.chemical_compound Receptors Glucocorticoid In vivo Internal medicine Drug Discovery medicine Animals Structure–activity relationship Receptor Molecular Biology Dose-Response Relationship Drug Molecular Structure Chemistry Antiglucocorticoid Organic Chemistry Antagonist Rats Dose–response relationship Endocrinology Models Animal Molecular Medicine medicine.symptom Weight gain Thymine medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 22:7376-7380
ISSN:	0960-894X
Popis:	We report the optimization of a series of non-steroidal GR antagonists that led to the identification of compound 7. This compound is efficacious when dosed orally in an olanzapine-induced weight gain model in rats.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::541110052c7b57a2ea48db89fe09a186 https://doi.org/10.1016/j.bmcl.2012.10.074 Zobrazit plný text záznamu Full Text from ScienceDirect