Solifenacin succinate

SKU: orb1225544

Description

Solifenacin Succinate(YM905; Vesicare) is a muscarinic receptor antagonist.(In Vitro):Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6±0.056, 6.9±0.034 and 8.0±0.021 for M1, M2 and M3 receptors, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin Succinate and oxybutynin on Ca2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin Succinate does not shift the CCh dose-activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pKb values are obtained as 7.4±0.17 for Solifenacin Succinate and 8.8±0.21 for oxybutynin.\n(In Vivo):Solifenacin Succinate (YM905) reduces bladder responses by 40% at a dose of 210 nmol/kg (0.1 mg/kg) and abolishes them at 2100 nmol/kg (1 mg/kg). In contrast, its inhibitory effects on salivary and cardiac responses are only slight at 630 nmol/kg (0.3 mg/kg), and reach 66% and 49%, respectively, at 2100 nmol/kg (1 mg/kg). At doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), Solifenacin Succinate slightly increases saliva secretion. Solifenacin Succinate (0.01 to 0.3 mg/kg i.v.) dose-dependently increases bladder capacity and voided volume at doses of 0.03 mg/kg i.v. or more, but does not affect residual volume or micturition pressure at any dose tested.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 242478-38-2
• MW: 480.56
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₆N₂O₂·C₄H₆O₄
• SMILES: C1CN2CCC1[C@H](C2)OC(=O)N3CCC4=CC=CC=C4[C@@H]3C5=CC=CC=C5.C(CC(=O)O)C(=O)O
• Target: AChR
• Solubility: Ethanol: 5 mg/mL (10.4 mM); Water: 96 mg/mL (199.77 mM); DMSO: 3 mg/mL (6.24 mM)

Bioactivity

• In Vivo:
  Solifenacin Succinate (YM905) reduces bladder responses by 40% at a dose of 210 nmol/kg (0.1 mg/kg) and abolishes them at 2100 nmol/kg (1 mg/kg). In contrast, its inhibitory effects on salivary and cardiac responses are only slight at 630 nmol/kg (0.3 mg/kg), and reach 66% and 49%, respectively, at 2100 nmol/kg (1 mg/kg). At doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), Solifenacin Succinate slightly increases saliva secretion. Solifenacin Succinate (0.01 to 0.3 mg/kg i. v.) dose-dependently increases bladder capacity and voided volume at doses of 0.03 mg/kg i. v. or more, but does not affect residual volume or micturition pressure at any dose tested.
• In Vitro:
  Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6±0.056, 6.9±0.034 and 8.0±0.021 for M1, M2 and M3 receptors, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin Succinate and oxybutynin on Ca2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin Succinate does not shift the CCh dose-activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pKb values are obtained as 7.4±0.17 for Solifenacin Succinate and 8.8±0.21 for oxybutynin.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Isoprenalinoe sulfate | YM-67905

Quick Database Links

Gene Symbol

AChR