product name Silodosin
Description: Silodosin (also known as KAD 3213, KMD 3213) 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.
References: Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16; Yakugaku Zasshi. 2006 Mar;126 Spec no.:231-6.
495.53
Formula
C25H32F3N3O4
CAS No.
160970-54-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 99 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 99 mg/mL (199.8 mM)
Solubility (In vivo)
Synonyms
KAD 3213, KMD 3213
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397926
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16; Yakugaku Zasshi. 2006 Mar;126 Spec no.:231-6. |
Related Posts
product name Silodosin
Description: Silodosin (also known as KAD 3213, KMD 3213) 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.
References: Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16; Yakugaku Zasshi. 2006 Mar;126 Spec no.:231-6.
495.53
Formula
C25H32F3N3O4
CAS No.
160970-54-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 99 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 99 mg/mL (199.8 mM)
Solubility (In vivo)
Synonyms
KAD 3213, KMD 3213
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397926
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16; Yakugaku Zasshi. 2006 Mar;126 Spec no.:231-6. |