Catalog No.S1754

For research use only.

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  Chemical Structure

CAS No. 5633-20-5

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Biological Activity

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.
AChR [1]
In vitro

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. [1] 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. [2] Oxybutynin increases the perfusion pressure starting at 100 mM in perfused rat liver. Oxybutynin also increases the perfusion pressure in the hepatic artery. [3]

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. [4] Oxybutynin induces a significant decrease in micturition pressure without changes in BVC in obstructed rats. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 357.49


CAS No. 5633-20-5
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04526353 Not yet recruiting Drug: Oxybutynin 1 mg/ml Syrup Male Urogenital Diseases University Hospital Bordeaux September 10 2020 Phase 2
NCT02522936 Withdrawn Drug: Biotene oral spray Overactive Bladder|Xerostomia|Compliance University of Southern California August 1 2018 Phase 4
NCT02099695 Withdrawn Drug: Oxybutynin|Drug: Placebo Hyperhidrosis Cristália Produtos Químicos Farmacêuticos Ltda.|Hospital Israelita Albert Einstein|University of Sao Paulo December 2015 Phase 3
NCT02327936 Completed Drug: Fesoterodine|Drug: Oxybutynin XL Overactive Bladder Stéphane Bolduc|Pfizer|CHU de Quebec-Universite Laval December 2014 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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