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编 号:F254675
分子式:C22H31NO2
分子量:341.49
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
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.

体内研究:
Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses. 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) . Animal Model:Female Sprague Dawley rats at ages 9 to 11 weeks weighing 180 to 250 g
Dosage:0.1 and 1 mg/kg
Administration:IV; single imidafenacin administration
Result:Significantly increased bladder compliance after moderate and high doses.

体外研究:
In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. 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.
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