250214-40-5

250214-40-5 structure
250214-40-5 structure
  • Name: (Rac)-5-Hydroxymethyl Tolterodine hydrochloride
  • Chemical Name: (Rac)-5-Hydroxymethyl Tolterodine hydrochloride
  • CAS Number: 250214-40-5
  • Molecular Formula: C22H32ClNO2
  • Molecular Weight: 377.95
  • Catalog: Signaling Pathways GPCR/G Protein mAChR
  • Create Date: 2021-12-19 17:23:48
  • Modify Date: 2024-02-04 07:53:06
  • (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].

Name (Rac)-5-Hydroxymethyl Tolterodine hydrochloride
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
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.

Molecular Formula C22H32ClNO2
Molecular Weight 377.95
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