Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors

Autor:	Eun Kyung Lee, Ralf Roetz, Clara Jeou Jen Lin, Jason Choy, Amy Geraldine Moore, Sandra Steiner, Kerem Erol Ozboya, Yansheng Zhai, Robert James Weikert, Karin Ann Stein, David S. Carter, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Pravin Iyer, Hai-Ying Cai, Saul Jaime-Figueroa, Robert Greenhouse, Lubica Raptova, Ryan Craig Schoenfeld, Linda M. Bannwart, Marzia Villa
Rok vydání:	2008
Předmět:	Tail Serotonin Pyrrolidines Clinical Biochemistry Pharmaceutical Science Pharmacology Motor Activity Biochemistry chemistry.chemical_compound Mice Norepinephrine Dopamine Uptake Inhibitors Dopamine In vivo Drug Discovery medicine Animals Humans Neurotransmitter Molecular Biology Monoamine transporter biology Dose-Response Relationship Drug Molecular Structure Organic Chemistry Antidepressive Agents Monoamine neurotransmitter chemistry Drug Design Catecholamine biology.protein Molecular Medicine Reuptake inhibitor medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 18(23)
ISSN:	1464-3405
Popis:	A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug interaction potential are described. One example showed in vivo anti-depressant-like effects in the mouse tail suspension assay with a minimum effective dose of 30 mg/kg i.p.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a84114b6169c0bc75e13b7bfee4fda1f https://pubmed.ncbi.nlm.nih.gov/18954985 Zobrazit plný text záznamu Full Text from ScienceDirect