product name Solifenacin succinate
Description: Solifenacin succinate is a urinary antispasmodic of the antimuscarinic class. Solifenacin succinate is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The affinity constants (pKi) of solifenacin for recombinant human muscarinic M1, M2 and M3 receptors are 7.6, 6.9 and 8.0, respectively. Hence, the muscarinic M3 receptor subtype selectivity of solifenacin over the muscarinic M2 receptor subtype is readily apparent, but is only marginal over the muscarinic M1 receptor subtype.
References: Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):97-103; J Urol. 2004 Nov;172(5 Pt 1):1919-24.
480.55
Formula
C23H26N2O.C4H6O4
CAS No.
242478-38-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 3 mg/mL (6.2 mM)
Water: 96 mg/mL (199.7 mM)
Ethanol: 5 mg/mL (10.4 mM)
Solubility (In vivo)
Synonyms
YM905
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19390641
| In Vitro |
In vitro activity: Solifenacin succinate is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The affinity constants (pKi) of solifenacin for recombinant human muscarinic M1, M2 and M3 receptors are 7.6, 6.9 and 8.0, respectively. Hence, the muscarinic M3 receptor subtype selectivity of solifenacin over the muscarinic M2 receptor subtype is readily apparent, but is only marginal over the muscarinic M1 receptor subtype. In the same study, solifenacin and oxybutynin inhibit muscarinic M3 receptor-mediated intracellular Ca2+ mobilization in bladder smooth muscle cells isolated from guinea pigs and in submandibular gland cells isolated from mice. Kinase Assay: Cell Assay: In radioligand receptor binding assay, the Ki values of solifenacin for human muscarinic M1, M2, M3, M4and M5receptors were 26, 170, 12, 110 and 31 nM, respectively. In isolated rat urinary bladder, solifenacin competitively antagonized carbachol-induced contractions, with a pA2value of 7.44±0.09.In bladder smooth muscle cells and salivary gland cells isolated from rats, solifenacin and the other antimuscarinic drugs inhibited carbachol-induced increases in intracellular Ca2+levels in a concentration-dependent manner. ThepKi was 8.12 for bladder smooth muscle cells, 3.6-fold more potent than that for salivary gland cells (pKi=7.57). |
|---|---|
| In Vivo | In anesthetized rats, solifenacin dose-dependently inhibited carbachol-induced intravesical pressure elevation and salivary secretion, and exhibited selectivity (3.7- to 6.5-fold) for urinary bladder over salivary gland. In anesthetized rats, solifenacin and oxybutynin increased the maximum bladder capacity in a dose-dependent manner and also decreased the maximum intravesical pressure.In healthy young men, multidose study evaluated doses. In the single-dose of solifenacin succinate (5-, 10-, 20-, and 30-mg), mean time to maximal concentration and elimination half-life ranged from 3.3 to 4.8 and from 40.2 to 57.6 hours, respectively.In the multidose study, the ranges were 2.9 to 5.8 and 45.0 to 64.8, respectively. The single-dose administration was well tolerated. The common adverse events were dry mouth, blurred vision, and headache. |
| Animal model | |
| Formulation & Dosage | |
| References | Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):97-103; J Urol. 2004 Nov;172(5 Pt 1):1919-24; Eur J Pharmacol. 2004 May 25;492(2-3):243-50; Biol Pharm Bull. 2007 Jan;30(1):54-8. |
Related Posts
product name Solifenacin succinate
Description: Solifenacin succinate is a urinary antispasmodic of the antimuscarinic class. Solifenacin succinate is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The affinity constants (pKi) of solifenacin for recombinant human muscarinic M1, M2 and M3 receptors are 7.6, 6.9 and 8.0, respectively. Hence, the muscarinic M3 receptor subtype selectivity of solifenacin over the muscarinic M2 receptor subtype is readily apparent, but is only marginal over the muscarinic M1 receptor subtype.
References: Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):97-103; J Urol. 2004 Nov;172(5 Pt 1):1919-24.
480.55
Formula
C23H26N2O.C4H6O4
CAS No.
242478-38-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 3 mg/mL (6.2 mM)
Water: 96 mg/mL (199.7 mM)
Ethanol: 5 mg/mL (10.4 mM)
Solubility (In vivo)
Synonyms
YM905
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19390641
| In Vitro |
In vitro activity: Solifenacin succinate is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The affinity constants (pKi) of solifenacin for recombinant human muscarinic M1, M2 and M3 receptors are 7.6, 6.9 and 8.0, respectively. Hence, the muscarinic M3 receptor subtype selectivity of solifenacin over the muscarinic M2 receptor subtype is readily apparent, but is only marginal over the muscarinic M1 receptor subtype. In the same study, solifenacin and oxybutynin inhibit muscarinic M3 receptor-mediated intracellular Ca2+ mobilization in bladder smooth muscle cells isolated from guinea pigs and in submandibular gland cells isolated from mice. Kinase Assay: Cell Assay: In radioligand receptor binding assay, the Ki values of solifenacin for human muscarinic M1, M2, M3, M4and M5receptors were 26, 170, 12, 110 and 31 nM, respectively. In isolated rat urinary bladder, solifenacin competitively antagonized carbachol-induced contractions, with a pA2value of 7.44±0.09.In bladder smooth muscle cells and salivary gland cells isolated from rats, solifenacin and the other antimuscarinic drugs inhibited carbachol-induced increases in intracellular Ca2+levels in a concentration-dependent manner. ThepKi was 8.12 for bladder smooth muscle cells, 3.6-fold more potent than that for salivary gland cells (pKi=7.57). |
|---|---|
| In Vivo | In anesthetized rats, solifenacin dose-dependently inhibited carbachol-induced intravesical pressure elevation and salivary secretion, and exhibited selectivity (3.7- to 6.5-fold) for urinary bladder over salivary gland. In anesthetized rats, solifenacin and oxybutynin increased the maximum bladder capacity in a dose-dependent manner and also decreased the maximum intravesical pressure.In healthy young men, multidose study evaluated doses. In the single-dose of solifenacin succinate (5-, 10-, 20-, and 30-mg), mean time to maximal concentration and elimination half-life ranged from 3.3 to 4.8 and from 40.2 to 57.6 hours, respectively.In the multidose study, the ranges were 2.9 to 5.8 and 45.0 to 64.8, respectively. The single-dose administration was well tolerated. The common adverse events were dry mouth, blurred vision, and headache. |
| Animal model | |
| Formulation & Dosage | |
| References | Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):97-103; J Urol. 2004 Nov;172(5 Pt 1):1919-24; Eur J Pharmacol. 2004 May 25;492(2-3):243-50; Biol Pharm Bull. 2007 Jan;30(1):54-8. |