| Bioactivity | 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]. | ||||||||||||
| Target | Kb: 0.84 nM (mAChR). | ||||||||||||
| Invitro | In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner[1]. In radioligand binding studies carries out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine is not selective for any muscarinic receptor subtype[1]. | ||||||||||||
| In Vivo | Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses[4]. In vivo, Desfesoterodine is significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively) [1]. Animal Model: | ||||||||||||
| Name | Desfesoterodine | ||||||||||||
| CAS | 207679-81-0 | ||||||||||||
| Formula | C22H31NO2 | ||||||||||||
| Molar Mass | 341.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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) [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. |
Desfesoterodine
CAS: 207679-81-0 F: C22H31NO2 W: 341.49
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.8
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