New series of cardioselective adrenergic .beta.-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols
| Autor: | A. H. Loveless, J. R. Clark, K. R. H. Wooldridge, E. C. J. Coffee, Berkeley Basil, D. L. Pain, R. Jordan |
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| Rok vydání: | 1976 |
| Předmět: |
Steric effects
CATS Adrenergic receptor Blocking (radio) Stereochemistry Chemistry Adrenergic beta-Antagonists Isoproterenol Molecular Conformation Adrenergic Arrhythmias Cardiac Transport effect Receptors Adrenergic Propanolamines Structure-Activity Relationship Dogs Heart Rate Organ Specificity Drug Discovery Cats Animals Molecular Medicine Anilides Ouabain Receptor |
| Zdroj: | Journal of Medicinal Chemistry. 19:399-402 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | A series of 1-(2-acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols has been synthesized and examined for beta-receptor blocking and antiarrhythmic activity. Several of these compounds are more than 20 times as active in blocking cardiac beta-receptors than vascular beta-receptors when given intravenously to anesthetized cats. The activities have been correlated quantitatively with partition and steric substitution constants. The observed relationships are consistent with a tentative proposal that the vascular receptor is situated in a more lipophilic environment than the cardiac receptor so that there is a differential transport effect between the two types of receptor. |
| Databáze: | OpenAIRE |
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