5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM,Desfesoterodine) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
5-hydroxymethyl tolterodine is a major pharmacologically active metabolite of tolterodine. 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 5-hydroxymethyl tolterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. [1] 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. [2] Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. [3]
5-hydroxymethyl tolterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. 5-hydroxymethyl tolterodine is three times more potent at the urinary bladder compared to the salivary gland. [1]
[1] Nilvebrant L, et al. Pharmacol Toxicol, 1997, 81(4), 169-172. [2] Nilvebrant L, et al. Life Sci, 1997, 60(13-14), 1129-1136. [3] Modiri AR, et al. Urology, 2002, 59(6), 963-968.