Actions of 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy) benzeneacetamide (KF4317) and labetalol on alpha- and beta-adrenoceptors.
Blocking activities of alpha- and beta-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. In blocking the beta 1-adrenoceptor, KF4317 was almost as active as labetalol. KF4317 was about 1/10th as potent as labetalol in blocking the beta 2-receptor. KF4317 was beta 1-adrenoceptor selective. KF4317 was about 1/50th as potent as labetalol in blocking the alpha 1-receptor. KF4317 did not interact with the alpha 2-adrenoceptor in concentrations up to 10(-5) M. The present results indicate that KF4317 is a selective beta 1- and alpha 1-adrenoceptor blocker, though the alpha 1-adrenoceptor blocking action is weak.
D000818:Animals; D044482:Benzeneacetamides; D006168:Guinea Pigs; D007741:Labetalol / Q000494:pharmacology*; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011412:Propanolamines / Q000494:pharmacology*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*
D044482:Benzeneacetamides; D011412:Propanolamines; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; C039100:KF 4317; D007741:Labetalol