Catalog No.S1613 Synonyms: KAD 3213, KMD 3213
Molecular Weight(MW): 495.53
Silodosin is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.
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Choose Selective Adrenergic Receptor Inhibitors
|Description||Silodosin is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.|
Silodosin shows higher selectivity for the alpha(1A)-AR subtype than tamsulosin hydrochloride, naftopidil or prazosin hydrochloride (affinity is highest for tamsulosin hydrochloride, followed by silodosin, prazosin hydrochloride and naftopidil in that order).  Silodosin and tadalafil have synergistic inhibitor effects on nerve-mediated contractions of human and rat isolated prostates in rats. 
|In vivo||Silodosin strongly antagonizes noradrenaline-induced contractions in rabbit lower urinary tract tissues (including prostate, urethra and bladder trigone, with pA(2) or pKb values of 9.60, 8.71 and 9.35, respectively).  Silodosin significantly inhibits the phenylephrine-induced increase in intraurethral pressure (versus the vehicle-treated group) at 12 hours, 18 hours, and 24 hours after its oral administration in rats.  Silodosin (0.1-0.3 mg/kg) or prazosin (0.03-0.1 mg/kg) reduces obstruction-induced increases in intraluminal ureter pressures by 21-37% or 18-40% respectively. Silodosin inhibits contractions of the rat and human isolated ureters and has excellent functional selectivity in vivo to relieve pressure-load of the rat obstructed ureter.  Silodosin (0.3-300 mg/kg) dose-dependently inhibits the hypogastric nerve stimulation-induced increase in intraurethral pressure (without significant hypotensive effects) in both young and old dogs with benign prostatic hyperplasia. |
-  Tatemichi S, et al. Yakugaku Zasshi,?006, 126, 209-216.
-  Buono R, et al. Eur J Pharmacol,?014, 744, 42-51.
-  Kobayashi M, et al. Yakugaku Zasshi,?006, 126, 231-236.
|In vitro||DMSO||99 mg/mL (199.78 mM)|
|Ethanol||99 mg/mL (199.78 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||KAD 3213, KMD 3213|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02090439||Terminated||Kidney Stone|Expulsive Medical Therapy||Centre Hospitalier Departemental Vendee||July 2014||Phase 3|
|NCT02106182||Unknown status||Nocturia|Benign Prostatic Hyperplasia||JW Pharmaceutical||December 2013||Phase 4|
|NCT02581826||Recruiting||Premature Ejaculation||Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation||October 2013||Phase 2|
|NCT02369744||Terminated||Ureteral Calculus|Ureterolithiasis|Ureteral Stone||Albert Einstein Healthcare Network||March 2013||Phase 4|
|NCT01560091||Unknown status||Kidney Stones||Albert Einstein Healthcare Network||March 2012||--|
|NCT01533389||Completed||Ureteral Stone||JW Pharmaceutical||October 2011||Phase 4|
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