Desfesoterodine

SKU: orb1686400

Description

Desfesoterodine

Research Area

Neuroscience

Key Properties

• CAS Number: 207679-81-0
• MW: 341.49
• Purity: 99.77% (May vary between batches)
• Formula: C₂₂H₃₁NO₂
• SMILES: CC(C)N(CC[C@H](c1ccccc1)c1cc(CO)ccc1O)C(C)C
• Target: AChR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.86 mM);DMSO:65 mg/mL (190.34 mM);Ethanol:63 mg/mL (184.49 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  mAChR:0.84 nM(Kb)
• In Vivo:
  Desfesoterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. Desfesoterodine is three times more potent at the urinary bladder compared to the salivary gland.
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• In Vitro:
  Desfesoterodine is a major pharmacologically active metabolite of tolterodine. Desfesoterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. Desfesoterodine antagotizes muscarinic receptors with a pA2 of 9.1. Desfesoterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. Desfesoterodine has a similar pharmacological profile with tolterodine. Intravenous infusion of Desfesoterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Fesoterodine, inhibit, muscarinic, Muscarinic acetylcholine receptor, metabolite, pA2, mAChR, Desfesoterodine, (R)-5-Hydroxymethyl Tolterodine, 5-HM, 5-HMT, 5-hydroxymethyl Tolterodine, 5-Hydroxymethyl Tolterodine, PNU-200583, PNU200577, PNU-200577, PNU 200577, receptor, Tolterodine

Compound Identifiers

PubChem CID

9819382