Molecular Weight(MW): 357.49
Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.
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|Description||Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.|
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. 
|In vivo||Oxybutynin decreases significantly binding potential (BP) of (+)N-[(11)C]methyl-3-piperidyl benzilate ([(11)C](+)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. |
-  Lukkari E, et al. Pharmacol Toxicol, 1998, 82(4), 161-166.
-  Tonini M, et al. J Pharm Pharmacol, 1987, 39(2), 103-107.
-  Comar JF, et al. Pharmacol Toxicol, 2003, 93(3), 147-152.
|In vitro||DMSO||71 mg/mL (198.6 mM)|
|Ethanol||71 mg/mL (198.6 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02961790||Recruiting||Bothered by Hot Flashes|Breast Carcinoma|Ductal Breast Carcinoma In Situ|Lobular Breast Carcinoma In Situ||Academic and Community Cancer Research United|National Cancer Institute (NCI)||December 2016||Phase 3|
|NCT02908529||Recruiting||Obstructive Sleep Apnea (OSA)||Brigham and Womens Hospital||September 2016||Phase 1|Phase 2|
|NCT02240459||Recruiting||Overactive Bladder|Mild Cognitive Impairment||University of Alberta|Pfizer||August 2016||Phase 2|
|NCT02704013||Not yet recruiting||Overactive Bladder||Childrens Hospital Zagreb|University Hospital for Infectious Diseases, Croatia||April 2016||--|
|NCT02633371||Active, not recruiting||Hyperhidrosis||University of Colorado, Denver|Society for Pediatric Dermatology||February 2016||--|
|NCT02099695||Withdrawn||Hyperhidrosis||Cristália Produtos Químicos Farmacêuticos Ltda.|Hospital Israelita Albert Einstein|University of Sao Paulo||December 2015||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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