5-hydroxymethyl Tolterodine is an active metabolite of the muscarinic acetylcholine receptor antagonists tolterodine and fesoterodine.
CAS:380636-49-7
分子式:C22H31NO2.CH2O2
分子量:387.5
纯度:98%
存储:Store at -20°C
Background:
5-hydroxymethyl Tolterodine is an active metabolite of the muscarinic acetylcholine receptor antagonists tolterodine and fesoterodine . It is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases. 5-hydroxymethyl Tolterodine inhibits M1-5 muscarinic receptors with Ki values of 2.3, 2, 2.5, 2.8, and 2.9 nM, respectively, for the human receptors expressed in CHO cells. It selectively inhibits acetylcholine-induced bladder contraction over electrically induced salivation in anesthetized cats (ID50s = 15 and 40 nmol/kg, respectively).