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抑制剂描述:

产品名称:Oxybutynin

产品别名:见爱必信官网

英文别名:Oxybutynin

靶点:AChR

CAS:5633-20-5

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Oxybutynin (Ditropan) is an anticholinergic medication used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination (urge incontinence), by decreasing muscle spasms of the bladder.Oxybutynin contains one stereocenter. The (R)-enantiomer is a more potent anticholinergic than either the racemate or the (S)-enantiomer, which is essentially without anticholinergic activity at the doses used in clinical practice. The other actions (calcium antagonism, local anesthesia) of oxybutynin are not stereospecific. (S)-Oxybutynin has not been clinically tested for its spasmolytic effects, but may be clinically useful for the same indications as the racemate, without the unpleasant anticholinergic side effects.

溶解性:Ethanol :66 mg/mL (184.6 mM)
DMSO :66 mg/mL (184.6 mM)

体外研究:

Oxybutynin N-deethylation in human liver microsomes in vitro is potently inhibited by ketoconazole (IC50 4.5 mM), less and variably by itraconazole and not by quinidine or several other reference inhibitors, suggesting that CYP3A enzymes are predominant catalysts of the reaction. Oxybutynin inhibits CYP3A4- and CYP2D6- associated activities (testosterone 6 beta-hydroxylase and dextromethorphan O- demethylase, respectively) in human liver microsomes. Oxybutynin is predominantly metabolized by CYP3A4 and CYP3A5 but not by CYP2D6. Oxybutynin (30, 100 nM) competitively antagonizes acetylcholine-induced contractions but does not alter those induced by histamine. Oxybutynin (up to 10 mM) induces a non-competitive depression of responses to both agonists and causes a parallel shift to the right of the Ca2+-induced contractions in taenia caeci strips bathed in a Ca2+-free, high-K+ medium. Oxybutynin (1-10 mM) impairs rhythmic muscular contractions in normal medium and after CaCl2 addition in Ca2+-free medium. Oxybutynin increases the perfusion pressure starting at 100 mM in perfused rat liver. Oxybutynin also increases the perfusion pressure in the hepatic artery.

体内研究:Oxybutynin decreases significantly binding potential (BP) of (+)N-methyl-3-piperidyl benzilate ((+)3-MPB) in the rat cerebral cortex and corpus striatum in a dose-dependent manner. Oxybutynin induces a significant decrease in micturition pressure without changes in BVC in obstructed rats.

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