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CAS No. 81403-68-1
Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
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PC-3 and LNCaP cell viability following treatment with a1-adrenoceptor antagonists. (A) Cells were treated with drug (0.01-100 μM) for 72 hr and cell viability determined using the resazurin reduction assay. (B) Effect of treatment duration on PC-3 and LNCap cell survival following treatment with doxazosin (30 μM) or prazosin (30 μM). Survival is expressed as the percentage values of untreated vehicle control and values are the mean ( sem) of six independent determinations each conducted in triplicate. *P<0.05, ***P<0.001 compared to corresponding values for LNCap cells.
Prostate, 2016, 76(8):757-66.. Alfuzosin HCl purchased from Selleck.
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|Description||Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).|
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.  Alfuzosin shows a concentration-dependent relaxing effect on rabbit corpus cavernosum (CC) pre-contracted by 10 mM phenylephrine. 
|In vivo||Alfuzosin (300 nM) significantly prolongs action potential duration (APD)(60) in rabbit Purkinje fibers and QT in isolated rabbit hearts.  Alfuzosin enhances the number and amplitude of erections induced by apomorphine in spontaneous hypertensive rats (SHR).  Alfuzosin behaves as an alpha-adrenergic antagonist blocking the contractions induced by exogenous noradrenaline without altering spikes in both portions of the vas deferens.  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. |
-  Lacerda AE, et al. J Pharmacol Exp Ther,?008, 324(2), 427-433.
-  Palea S, et al. BJU Int,?003, 91(9), 873-877.
-  Mayoux E, et al. Eur Urol,?004, 45(1), 110-116.
|In vitro||DMSO||85 mg/mL warmed (199.57 mM)|
|Water||85 mg/mL (199.57 mM)|
|Ethanol||85 mg/mL (199.57 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01685658||Withdrawn||Drug: Intravenous ketoprofen|Drug: Intravenous paracetamol||Renal Colic|Acute Renal Colic||Centre Hospitalier Universitaire de Nīmes||September 2016||Phase 4|
|NCT00637715||Completed||Drug: Alfuzosin||Benign Prostatic Hyperplasia||Sanofi||October 2003||Phase 4|
|NCT00290030||Completed||Drug: Alfuzosin||Prostatic Hyperplasia|Acute Urinary Retention||Sanofi||May 2001||Phase 3|
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