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).

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