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 |
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| Rok vydání: | 1987 |
| Předmět: |
Models
Molecular Agonist Stereochemistry Chemistry medicine.drug_class Dopamine Absolute configuration Stereoisomerism Biological activity Benzazepines Cyclase Dopamine agonist Retina Rats Methyldopamine Deoxyepinephrine Drug Discovery medicine Animals Molecular Medicine heterocyclic compounds Enantiomer Adenylyl Cyclases medicine.drug |
| 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 |
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