Home Neuronal Signaling AChR antagonist Oxybutynin For research use only.

Oxybutynin

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

Oxybutynin Chemical Structure

CAS No. 5633-20-5

Purity & Quality Control

Oxybutynin Related Products

Signaling Pathway

AChR Signaling Pathways

AChR Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05637671 Recruiting
Vasomotor Symptoms
Cairo University
 February 10 2022 Phase 3
NCT04526353 Unknown status
Male Urogenital Diseases
University Hospital Bordeaux
 September 10 2020 Phase 2
NCT02522936 Withdrawn
Overactive Bladder|Xerostomia|Compliance
University of Southern California
 August 1 2018 Phase 4
NCT02099695 Withdrawn
Hyperhidrosis
Cristália Produtos Químicos Farmacêuticos Ltda.|Hospital Israelita Albert Einstein|University of Sao Paulo
 December 2015 Phase 3

Chemical Information & Solubility

Molecular Weight 357.49 Formula

C22H31NO3
CAS No. 5633-20-5 SDF Download Oxybutynin SDF
Smiles CCN(CC)CC#CCOC(=O)C(C1CCCCC1)(C2=CC=CC=C2)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (198.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble


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In vivo
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