Naftopidil was launched in Japan for the treatment of dysuria
associated with benign prostatic hypertrophy (BPH). It can be prepared by a two
step route starting with α-naphthol. Naftopidil is a potent postsynaptic-selective
alpha-l-antagonist with a slightly higher affinity for the human prostatic than for
the aortic alpha-adrenoceptor. It also shows a 5-HT1A agonistic effect, as well
as a weak calcium antagonistic activity, but no alpha-2 or beta-adrenoreceptor
affinity. In experiments with rats or rabbits, Naftopidil was shown to be more
potent and selective for the urodynamic effect than the hypotensive effect.
Aromatic or aliphatic hydroxylation are the major routes of metabolism,
producing metabolites with a profile similar to the parent compound.
화학적 성질
Off-White Solid
용도
A α-1-Adrenergic receptor antagonist, antihypertensive.
생물학적 활성
An α 1 -adrenoceptor antagonist with only weak antagonism at post-junctional α 2 receptors; a potent, persistent antihypertensive and vasodilator.
