| Identification | Back Directory | [Name]
2-(3-(diisopropylaMino)-1-phenylpropyl)-4-(hydroxyMethyl)phenol (hydrochloride) | [CAS]
250214-40-5 | [Synonyms]
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride
2-(3-(diisopropylaMino)-1-phenylpropyl)-4-(hydroxyMethyl)phenol (hydrochloride) | [Molecular Formula]
C22H32ClNO2 | [MOL File]
250214-40-5.mol | [Molecular Weight]
377.95 |
| Hazard Information | Back Directory | [Uses]
(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]. | [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]. | [IC 50]
mAChR1; mAChR3; mAChR4; mAChR5 | [References]
[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. DOI:10.1111/j.1600-0773.1997.tb02064.x
[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. DOI:10.2174/092986709789712835
[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. DOI:10.1016/j.jphs.2019.05.001 |
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