Effect of .beta.-alkyl substitution on D-1 dopamine agonist activity: absolute configuration of .beta.-methyldopamine

Autor: Lewis L. Truex, Robert M. Riggs, Foreman Mark Mortensen, Ann T. McKenzie, David E. Nichols, Stephen R. Byrn
Rok vydání: 1987
Předmět:
Zdroj: Journal of Medicinal Chemistry. 30:1914-1918
ISSN: 1520-4804
0022-2623
DOI: 10.1021/jm00393a039
Popis: beta-Methyldopamine and its enantiomers and racemic beta-phenyldopamine were synthesized and evaluated for dopamine D-1 agonist activity. In the dopamine-sensitive adenylate cyclase assay, beta-phenyldopamine had about one-sixth the activity of dopamine. Racemic beta-methyldopamine was less potent. The absolute configuration of beta-methyldopamine was determined to be R-(+) and S-(-). Evaluation of (R)-(+)- and (S)-(-)-beta-methyldopamine revealed no enantioselectivity for stimulation of adenylate cyclase.
Databáze: OpenAIRE