rac-Desethyl oxybutynin is an active metabolite of the muscarinic acetylcholine receptor (mAChR) antagonist oxybutynin .1,2,3rac-Desethyl oxybutynin is formed from oxybutynin by the cytochrome P450 (CYP) isoform CYP3A4.2It binds to mAChRs in isolated rat bladder, submaxillary gland, heart, and colon with Kivalues of 5.38, 3.12, 16, and 5.59 nM, respectively.rac-Desethyl oxybutynin (0.4 and 0.8 mg/kg) reduces micturition pressure in rats.3
Oxybutynin R-isomer , also known as Aroxybutynin, is a muscarinic receptor antagonist. Aroxybutynin is the optically avtice inhibitor of proliferation and supresses gene expression in bladder smooth muscle cells. Oxybutynin exerts direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. It exhibits one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects).
(R)-Oxybutynin (Aroxybutynin) is an orally active muscarinic receptor antagonist, which exhibits antimuscarinic, antispasmodic, and anticholinergic activity. This compound, being the (R)-isomer of Oxybutynin, competitively antagonizes Carbachol-induced contractions. It is particularly useful in researching neurogenic bladder dysfunction-related incontinence [1] [2] [3].
Esoxybutynin Chloride is (S)-enantiomer of oxybutynin. Esoxybutynin Chloride exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.
Esoxybutynin Free Base is (S)-enantiomer of oxybutynin. Esoxybutynin Free Base exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.