Naftopidil

57149-07-2

C24H28N2O3

H2O : < 0.1 mg/mL (insoluble); DMSO : 33.33 mg/mL (84.92 mM; Need ultrasonic)

GPCR/G Protein; Neuronal Signaling

Naftopidil (Flivas), a selective alpha1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug. Target: alpha1-Adrenergic Receptor Naftopidil significantly improved the overall international prostatic symptom score ; from 19.2+/-7.9 to 11.7+/-5.8 in the M group and from 19.4+/-6.4 to 12.3+/-6.8 in the E group (p<0.0001), QOL score from 4.9+/-0.8 to 3.2+/-1.4 in the M group and from 5.0+/-0.8 to 3.6+/-1.3 in the E group (p<0.0001), and OAB symptom score from 7.8+/-2.6 to 5.0+/-2.5 in the M group (p<0.0001) and from 8.6+/-2.9 to 5.8+/- 3.3 in the E group (p<0.0001). naftopidil improves storage symptoms as well as voiding symptoms regardless of timing of administration [1]. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human alpha1-adrenoceptor subtypes, naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for alpha1a- and alpha1d-adrenoceptor subtypes [2].