General paperActions of 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy)benzeneacetamide (KF4317) and labetalol on α- and β-adrenoceptors

Add time:08/14/2019    Source:sciencedirect.com

1.1. Blocking activities of α- and β-adrenoceptors by 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy)benzeneacetamide (KF4317) were tested on the isolated muscles, compared with the action of labetalol.2.2. In blocking the β1-adrenoceptor, KF4317 was almost as active as labetalol.3.3. KF4317 was about 1/10th as potent as labetalol in blocking the β2-receptor.4.4. KF4317 was β1-adrenoceptor selective.5.5. KF4317 was about 1/50th as potent as labetalol in blocking the α1-receptor.6.6. KF4317 did not interact with the α2-adrenoceptor in concentrations up to 10−5 M.7.7. The present results indicate that KF4317 is a selective β1- and α1-adrenoceptor blocker, though the α1-adrenoceptor blocking action is weak.

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