| Bioactivity | (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research[1]. | ||||||||||||
| Target | Ki: M1 (2.3 nM), M2 (2 nM), M3 (2.5 nM), M4 (2.8 nM), and M5 (2.9 nM) | ||||||||||||
| Invitro | In vitro, (Rac)-5-Hydroxymethyl Tolterodine (PNU-200577) hydrochloride produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips (KB of 0.84 nM; pA2 of 9.14)[2]. | ||||||||||||
| In Vivo | (Rac)-5-Hydroxymethyl Tolterodine (5-HMT; 0.88 μmol/kg; i.v.) hydrochloride treatment shows the binding activity of (Rac)-5-Hydroxymethyl Tolterodine hydrochloride to muscarinic receptors is significantly observed in all tissues, except cerebral cortex, with a longer duration in bladder[3]. | ||||||||||||
| Name | (Rac)-5-Hydroxymethyl Tolterodine hydrochloride | ||||||||||||
| CAS | 250214-40-5 | ||||||||||||
| Formula | C22H32ClNO2 | ||||||||||||
| Molar Mass | 377.95 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. L Nilvebrant, et al. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72. [2]. B Malhotra, et al. The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9. [3]. Shizuo Yamada, et al. Muscarinic receptor binding of fesoterodine, 5-hydroxymethyl tolterodine, and tolterodine in rat tissues after the oral, intravenous, or intravesical administration. J Pharmacol Sci. 2019 May;140(1):73-78. |
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride
CAS: 250214-40-5 F: C22H32ClNO2 W: 377.95
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR
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