Alfuzosin HCl

Synonyms: SL 77499 HCl

Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).

Alfuzosin HCl  Chemical Structure

Alfuzosin HCl Chemical Structure

CAS No. 81403-68-1

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Biological Activity

Description Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Targets
α1-adrenergic receptor [1]
In vitro
In vitro

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]

In Vivo
In vivo

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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06316336 Not yet recruiting
Healthy Vollunteer
Pharma Nueva
June 10 2024 Phase 1
NCT01685658 Withdrawn
Renal Colic|Acute Renal Colic
Centre Hospitalier Universitaire de Nīmes
September 2016 Phase 4
NCT00637715 Completed
Benign Prostatic Hyperplasia
Sanofi
October 2003 Phase 4
NCT00290030 Completed
Prostatic Hyperplasia|Acute Urinary Retention
Sanofi
May 2001 Phase 3

Chemical Information & Solubility

Molecular Weight 425.91 Formula

C19H27N5O4.HCl

CAS No. 81403-68-1 SDF Download Alfuzosin HCl SDF
Smiles CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 85 mg/mL ( (199.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 85 mg/mL

Ethanol : 85 mg/mL


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In vivo
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