Alfuzosin hydrochloride 是一种 α1 肾上腺素受体拮抗剂,可用于良性前列腺增生(BPH)的研究。
产品描述
Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist. It applies to treat benign prostatic hyperplasia (BPH).
体外活性
Alfuzosin significantly increases whole-cell peak sodium (hNa(v)1.5) current, increases the probability of late hNa(v)1.5 single-channel openings, and significantly shortens the slow time constant for recovery from inactivation. Alfuzosin also increases hNa(v)1.5 burst duration and number of openings per burst between 2- and 3-fold. [1] Alfuzosin shows a concentration-dependent relaxing effect on rabbit corpus cavernosum (CC) pre-contracted by 10 mM phenylephrine. [2]
体内活性
Alfuzosin (300 nM) significantly prolongs action potential duration (APD)(60) in rabbit Purkinje fibers and QT in isolated rabbit hearts. [1] Alfuzosin enhances the number and amplitude of erections induced by apomorphine in spontaneous hypertensive rats (SHR). [3] Alfuzosin behaves as an alpha-adrenergic antagonist blocking the contractions induced by exogenous noradrenaline without altering spikes in both portions of the vas deferens. [4] Alfuzosin (0.03-0.3 mg kg-1, i.v.) markedly inhibits pressor responses produced by the alpha 1-selective agonist, Cirazoline but inhibits only slightly responses to the alpha 2-selective agonist, UK 14,304, in the pithed rat. Alfuzosin (1 mg kg-1, i.v.) has minimal effects against responses mediated by stimulation of prejunctional alpha 2-receptors (UK 14,304-induced inhibition of sympathetic tachycardia). Alfuzosin (0.001-1 mg kg-1, i.v.) and Prazosin (0.001-0.3 mg kg-1, i.v.) produces dose-related inhibition of the increases in urethral pressure caused by stimulation of sympathetic hypogastric nerves in the anaesthetized cat. [5]
Cas No.
81403-68-1
分子式
C19H28ClN5O4
分子量
425.91
别名
SL 77499-10;Alfuzosin HCl;盐酸阿夫唑嗪;Alfuzosin hydrochloride
储存和溶解度
H2O:10.7 mg/mL (25 mM)
DMSO:10.7 mg/mL (25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years