1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Desfesoterodine

Desfesoterodine (Synonyms: PNU-200577; 5-Hydroxymethyl Tolterodine)

Cat. No.: HY-76569 Purity: 99.58% ee.: 99.81%
Handling Instructions

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. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.

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Desfesoterodine Chemical Structure

Desfesoterodine Chemical Structure

CAS No. : 207679-81-0

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Description

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].

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].

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: 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.
Molecular Weight

341.49

Formula

C₂₂H₃₁NO₂

CAS No.

207679-81-0

SMILES

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

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
In Vitro: 

DMSO : ≥ 100 mg/mL (292.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.58% ee.: 99.81%

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Keywords:

DesfesoterodinePNU-2005775-Hydroxymethyl TolterodinePNU200577PNU 200577mAChRMuscarinic acetylcholine receptormuscarinicreceptorKBpA2metaboliteTolterodinePNU-200583FesoterodineInhibitorinhibitorinhibit

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Desfesoterodine
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