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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride

Names

[ CAS No. ]:
250214-40-5

[ Name ]:
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride

Biological Activity

[Description]:

(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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Signaling Pathways >> GPCR/G Protein >> mAChR
Research Areas >> Neurological Disease

[Target]

Ki: M1 (2.3 nM), M2 (2 nM), M3 (2.5 nM), M4 (2.8 nM), and M5 (2.9 nM)[1]


[In Vitro]

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].

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H32ClNO2

[ Molecular Weight ]:
377.95

Related Compounds