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(R)-Oxybutynin

Cat. No. M41000
(R)-Oxybutynin Structure
Synonym:

Aroxybutynin

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Biological Activity

(R)-Oxybutynin is a racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. It has antitussive and anticholinergic activity, competitively antagonizes carbachol-induced contractions, and can be used in studies related to obstructive sleep apnea (OSA).

Chemical Information
Molecular Weight 357.49
Formula C22H31NO3
CAS Number 119618-21-2
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Melanie Kretschmar et al. J Clin Pharmacol. A Population Pharmacokinetic Model of (R)- and (S-) Oxybutynin and Its Active Metabolites After Oral and Intravesical Administration to Healthy Volunteers

[2] Primal Sharma et al. J Pharm Biomed Anal. Parallel achiral-chiral determination of oxybutynin, N-desethyl oxybutynin and their enantiomers in human plasma by LC-MS/MS to support a bioequivalence trial

[3] Haruhi Mizushima et al. Biol Pharm Bull. Pharmacokinetics/pharmacodynamics analysis of the relationship between the in vivo micturition pressure and receptor occupancy of (R)-oxybutynin and its metabolite in rats

[4] G Sathyan et al. Br J Clin Pharmacol. Effect of OROS controlled-release delivery on the pharmacokinetics and pharmacodynamics of oxybutynin chloride

[5] M M Goldenberg. Clin Ther. An extended-release formulation of oxybutynin chloride for the treatment of overactive urinary bladder

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