An α1-adrenergic receptor antagonist
Naftopidil is an α1-adrenergic receptor antagonist that competitively inhibits α-adrenoceptor-mediated contractions induced by noradrenaline with pA2 values of 6.73-8.15 in various blood vessels from dog, rabbit, guinea pig, and rat. It binds to the cloned human α1-adrenergic receptors with Ki values of 3.7, 20, and 1.2 nM for α1A, α1B and α1D, respectively. Clinical formulations of naftopidil are used in the treatment of benign prostatic hyperplasia in Japan. Naftopidil also exhibits antiproliferative activity, inhibiting the growth of androgen-sensitive LNcaP cells and androgen-insensitive PC-3 cancer cell lines with IC50 values of 22.2 and 33.2 µM, respectively.
动态评分
0.0