carbamoylcholine Solifenacin-d5 is intended for use as an internal standard for the quantification of solifenacin by GC- or LC-MS. Solifenacin is a competitive antagonist of M1, M2, and M3 muscarinic acetylcholine receptors (Kis = 25, 125, and 10 nM, respectively, for the human receptors).1 It inhibits calcium mobilization induced by carbamoylcholine in isolated guinea pig detrusor muscle cells (Ki = 4 nM).2 Solifenacin inhibits carbachol-induced contraction of isolated guinea pig urinary bladder smooth muscle. In vivo, solifenacin (0.03-1 mg/kg) inhibits carbachol-induced increases in urinary bladder pressure in anesthetized rats. Formulations containing solifenacin have been used in the treatment of overactive bladder.
1.Hegde, S.S.Muscarinic receptors in the bladder: From basic research to therapeuticsBr. J. Pharmacol.147(2)S80-S87(2006) 2.Ikeda, K., Koboyashi, S., Suzuki, M., et al.M3 receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary glandNaunyn Schmiedebergs Arch. Pharmacol.366(2)97-103(2002)