Oxybutynin

Catalog No.S1754

Oxybutynin  Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 970 In stock
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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.
Targets
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

Solubility (25°C)

In vitro DMSO 71 mg/mL (198.6 mM)
Ethanol 71 mg/mL (198.6 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 357.49
Formula

C22H31NO3

CAS No. 5633-20-5
Storage powder
Synonyms N/A

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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

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AChR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID