In Vitro and In Vivo Characterization of Alpha-1A Selective Agonists and Their Utility for Stress Incontience

Autor:	Michael E. Brune, Teodozyj Kolasa, Michael Meyer, Jorge D. Brioni, James P. Sullivan, William A. Carroll, Robert J. Altenbach, Steven A. Buckner
Rok vydání:	2004
Předmět:	Ring size Mean arterial pressure In vivo Chemistry Organic Chemistry Alpha (ethology) Subtype selectivity General Pharmacology Toxicology and Pharmaceutics Electrophilic aromatic substitution Pharmacology Selectivity In vitro
Zdroj:	Medicinal Chemistry Research. 13:134-148
ISSN:	1554-8120 1054-2523
DOI:	10.1007/s00044-004-0020-z
Popis:	SAR studies were conducted around a series of arylalkylimidazoles and arylalkylimidazolines based upon the core structure of A-61603. Changes in ring size, the heterocyclic appendage, aromatic substitution and absolute stereochemistry were examined. Compounds were evaluated for subtype selectivity in vitro using radioligand binding and functional tissue strip assays. In vivo, selectivity for effects on intraurethral pressure (IUP) versus mean arterial pressure (MAP) was determined in anesthetized dogs. Compounds were identified that displayed selectivity in vitro for the α 1 A subtype and that also showed enhanced urethral selectivity relative to non-subtype selective agents.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::22b543f291985eb10434aae7d5a43b4f https://doi.org/10.1007/s00044-004-0020-z Zobrazit plný text záznamu Full text from SpringerLink