[CAS NO. 57149-08-3]  Naftopidil DiHCl

Naftopidil diHCl possesses 5-HT1A agonistic properties in addition to being an α1-adrenoceptor antagonist. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil inhibits the growth of androgen-sensitive LNCaP cells and androgen-insensitive PC-3 cells with IC50 of 22.2 μM and 33.2 μM, respectively. Cell growth inhibition by Naftopidil is due to the arrest of the G1 cell cycle. Expressions of p27 and p21 are significantly increased in LNCaP cells treated with Naftopidil. In PC-3 cells, Naftopidil induces p21 but not p27. Naftopidil produces a concentration-dependent inhibition of collagen-induced Ca mobilization, maximum inhibition (22.9%) occurring with 40 μM Naftopidil. The adrenaline-induced rise in [Ca] is inhibited dose dependently by Naftopidil. Naftopidil is significantly more effective than tamsulosin in relieving nocturia. Naftopidil induces G(1) cell-cycle arrest in both PCa cells and PrSC. In Naftopidil-treated PrSC, total interleukin-6 protein is significantly reduced with increased suppression of cell proliferation.