Desfesoterodine

Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively[1]. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) [2][3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats[4].

Product Specifications

CAS Number

[207679-81-0]

Product Name Alternative

PNU-200577; 5-Hydroxymethyl Tolterodine

UNSPSC

12352005

Hazard Statement

H302-H319-H360

Target

MAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/_R_-5-Hydroxymethyl-Tolterodine.html

Concentration

10mM

Purity

99.88

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C

Molecular Formula

C22H31NO2

Molecular Weight

341.50

Precautions

P264-P270-P280-P305+P351+P338-P330-P405-P501

References & Citations

[1]Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81 (4) :169-72.|[2]Fullhase, Claudius; Soler, Roberto; Gratzke, Christian et al. Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction. Journal of Urology (New York, NY, United States) (2010), 184 (2), 783-789.|[3]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.|[4]Naoki Aizawa, et al. Selective Inhibitory Effect of Imidafenacin and 5-hydroxymethyl Tolterodine on Capsaicin Sensitive C Fibers of the Primary Bladder Mechanosensitive Afferent Nerves in the Rat. J Urol. 2015 Apr;193 (4) :1423-32.