[CAS NO. 207679-81-0] Desfesoterodine
PRODUCTS SPECIFICATIONS [207679-81-0]
DESCRIPTION [207679-81-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 341.49 |
| Molecular Formula | C22H31NO2 |
| SMILES | OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C |
Summary
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a K B and a pA 2 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] .
IC50 & Target
Kb: 0.84 nM (mAChR) [1] .
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female Sprague Dawley rats at ages 9 to 11 weeks weighing 180 to 250 g [4] |
| Dosage: | 0.1 and 1 mg/kg |
| Administration: | IV; single imidafenacin administration |
| Result: | Significantly increased bladder compliance after moderate and high doses. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
H 2 O : 100 mg/mL ( 292.83 mM ; Need ultrasonic)
DMSO : 50 mg/mL ( 146.42 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9283 mL | 14.6417 mL | 29.2834 mL |
| 5 mM | 0.5857 mL | 2.9283 mL | 5.8567 mL |
| 10 mM | 0.2928 mL | 1.4642 mL | 2.9283 mL |
References
- [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.
Synonyms