Disease relevance of KF 4317

• Furthermore, KF-4317 neither showed any sign indicative of orthostatic hypotension in an experimental model nor exhibited any intrinsic sympathomimetic activity, though a very weak local anesthetic effect was observed [1].
• From these results, it could be concluded that KF-4317 possesses some pharmacological properties similar to labetalol, but in contrast to labetalol it is beta 1-selective, and it may be useful in the treatment of patients with hypertension [1].

High impact information on KF 4317

• This suggests that in addition to beta 1-adrenoreceptor antagonism, KF-4317 probably exerts membrane stabilizing activity [2].
• KF-4317 at 1 microM had no effect on the ability of the rat right ventricle to accumulate radioactivity from [3H]-noradrenaline [2].
• The spontaneous outflow of radioactivity, following loading of the ventricle with [3H]-noradrenaline, was increased by KF-4317 at 1 microM by a cocaine-insensitive mechanism [2].
• Extremely long-acting antihypertensive effects of KF-4317, a alpha- and beta 1-adrenoceptor blocker [1].
• The hypotensive effects of 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy)benzeneacetamide hydrochloride (KF-4317, a novel alpha- and beta 1-adrenoceptor blocker) were evaluated in spontaneously hypertensive rats and renal hypertensive dogs as well as in normotensive dogs, cats and rabbits, using various routes of administration [1].

Associations of KF 4317 with other chemical compounds

• In blocking beta 2-adrenoceptors, KF-4317 is 776 times less potent (in vitro) and 83 times less potent (in vivo) than propranolol [3].
• In blocking beta 1-adrenoceptors, KF-4317 is as active as labetalol in both in vitro and in vivo experiments, and 22 times less potent (in vitro) and 2 times less potent (in vivo) than propranolol [3].

References