research use only
Cat.No.S1409
| Related Targets | AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR |
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| Other Adrenergic Receptor Inhibitors | Zenidolol (ICI-118551) Hydrochloride L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide |
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In vitro |
DMSO
: 85 mg/mL
(199.57 mM)
Water : 85 mg/mL Ethanol : 85 mg/mL |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 425.91 | Formula | C19H27N5O4.HCl |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 81403-68-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | SL 77499 HCl | Smiles | CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC.Cl | ||
| Targets/IC50/Ki |
α1-adrenergic receptor
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|---|---|
| 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. 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. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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