Antihypertensive 1-Acyl-4-[2-(1,4-benzodioxan-2-yl)-2-hydroxyethylamino]piperidines

Several 1-acyl-4-[2-(1,4-benzodioxan-2-yl)-2-hydroxy-ethylamino]piperidines were prepared and a number of the compounds showed antihypertensive activity in the spontaneously hypertensive rat (SHR). This activity was specific for the (2S, 2R) enantiomers. General pharmacological evaluation and ligand...

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Veröffentlicht in:Journal of pharmaceutical sciences 1987-01, Vol.76 (1), p.32-34
Hauptverfasser: Caroon, Joan M., Clark, Robin D., Repke, David B., Kluge, Arthur F., Strosberg, Arthur M., Whiting, Roger L., Okada, Marlys D., Hedley, Linda R., van Antwerp, Donna, Brown, Christine M.
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Sprache:eng
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Zusammenfassung:Several 1-acyl-4-[2-(1,4-benzodioxan-2-yl)-2-hydroxy-ethylamino]piperidines were prepared and a number of the compounds showed antihypertensive activity in the spontaneously hypertensive rat (SHR). This activity was specific for the (2S, 2R) enantiomers. General pharmacological evaluation and ligand binding data on selected compounds indicated a moderate degree of α1- and β-antagonistic activity. The α1 antagonism was probably not of sufficient magnitude to explain the blood pressure lowering activity in the SHR.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600760110