| Name | Desfesoterodine |
| Description | Desfesoterodine (5-HMT) is a new muscarinic receptor antagonist with Kb of 0.84 nM. |
| 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. [1] Desfesoterodine has a similar pharmacological profile with tolterodine. [2] Intravenous infusion of Desfesoterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. [3] |
| 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. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.86 mM), Sonication is recommended.
Ethanol : 63 mg/mL (184.49 mM), Sonication is recommended.
DMSO : 65 mg/mL (190.34 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Tolterodine | receptor | PNU-200583 | PNU200577 | PNU 200577 | pA2 | Muscarinic acetylcholine receptor | muscarinic | metabolite | mAChR | Inhibitor | inhibit | Fesoterodine | Desfesoterodine | 5-Hydroxymethyl Tolterodine |
| Inhibitors Related | Adiphenine hydrochloride | Levamisole hydrochloride | Ethyl (triphenylphosphoranylidene) acetate | Urethane | Hexamethonium Bromide | Ribavirin | Adenine | Mitotane | Choline chloride | Propoxur | N,N-Dicyclohexylcarbodiimide | Arecoline |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Anti-Alzheimer's Disease Compound Library | Approved Drug Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Preclinical Compound Library | Human Metabolite Library |
United States
