product name Alfuzosin HCl
Description: Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). As an antagonist of the alpha-1 adrenergic receptor, Alfuzosin works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate. It is thus used to treat benign prostatic hyperplasia (BPH).
References: J Pharmacol Exp Ther. 2008 Feb;324(2):427-33; Eur Urol. 2004 Jan;45(1):110-6.
425.91
Formula
C19H27N5O4.HCl
CAS No.
81403-68-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 85 mg/mL (199.6 mM)
Water: 85 mg/mL (199.6 mM)
Ethanol: 85 mg/mL (199.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397724
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2008 Feb;324(2):427-33; Eur Urol. 2004 Jan;45(1):110-6 |
Related Posts
product name Alfuzosin HCl
Description: Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). As an antagonist of the alpha-1 adrenergic receptor, Alfuzosin works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate. It is thus used to treat benign prostatic hyperplasia (BPH).
References: J Pharmacol Exp Ther. 2008 Feb;324(2):427-33; Eur Urol. 2004 Jan;45(1):110-6.
425.91
Formula
C19H27N5O4.HCl
CAS No.
81403-68-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 85 mg/mL (199.6 mM)
Water: 85 mg/mL (199.6 mM)
Ethanol: 85 mg/mL (199.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397724
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2008 Feb;324(2):427-33; Eur Urol. 2004 Jan;45(1):110-6 |