Antihypertensive aminotetralins related to labetalol and medroxalol

A series of compounds was prepared in which the 1-methyl-3-phenylpropylamino moieties of the antihypertensive agents labetalol and medroxalol were replaced by 2-aminotetralins. Compounds containing a 6-methoxy and 6,7-methylenedioxy group in the aminotetralin were at least as active as labetalol in...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1986, Vol.75 (1), p.80-82
Main Authors: CLARK, R. D, CAROON, J. M, REPKE, D. B, STROSBERG, A. M, WHITING, R. L, BROWN, C. M
Format: Article
Language:English
Subjects:
Animals
Antihypertensive Agents - chemical synthesis
Biological and medical sciences
Cerebral Cortex - metabolism
Chemical Phenomena
Chemistry
Ethanolamines - pharmacology
General pharmacology
Labetalol - analogs & derivatives
Labetalol - pharmacology
Male
Medical sciences
Naphthalenes - chemical synthesis
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Rats
Rats, Inbred SHR
Receptors, Adrenergic, alpha - metabolism
Tetrahydronaphthalenes - chemical synthesis
Tetrahydronaphthalenes - pharmacology
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Summary:A series of compounds was prepared in which the 1-methyl-3-phenylpropylamino moieties of the antihypertensive agents labetalol and medroxalol were replaced by 2-aminotetralins. Compounds containing a 6-methoxy and 6,7-methylenedioxy group in the aminotetralin were at least as active as labetalol in lowering the blood pressure of the spontaneously hypertensive rat (SHR). As determined by ligand binding, these compounds were comparable to labetalol as alpha 1-antagonists but were substantially weaker beta 1-antagonists.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600750119