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Species differences in the metabolism of α‐1‐ trans ‐4‐dimethylaminotetrahydro‐3‐furylcyclohexanephenylglycolate, an experimental anticholinergic agent
Author(s) -
Sullivan Hugh R.,
Page John G.,
Due Susan L.
Publication year - 1975
Publication title -
biomedical mass spectrometry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 121
eISSN - 1096-9888
pISSN - 0306-042X
DOI - 10.1002/bms.1200020110
Subject(s) - anticholinergic , anticholinergic agents , metabolism , pharmacology , medicine , psychology
Metabolism studies in the rat, dog and cat have demonstrated a definite species difference in biotransformation and elimination of α‐1‐ trans ‐4‐dimethylaminotetrahydro‐3‐furylcyclohexanephenylglycolate (Lilly 82537), an experimental anticholinergic agent. Separation and identification of urinary and biliary metabolites by gas chromatographic mass spectrometric analysis has shown three mechanisms to be involved in the metabolism of Lilly 82537 in these species; N ‐demethylation, aliphatic hydroxylation and ester hydrolysis. A major portion of the drug administered was eliminated unaltered in the cat and dog, while only trace quantities of parent drug were observed in the urine and bile of rats. These metabolic differences may be responsible for observed species differences in the pharmacologic activity of Lilly 82537.

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