PT  - JOURNAL ARTICLE
AU  - A G Zacchei
AU  - T I Wishousky
AU  - B H Arison
AU  - G Hitzenberger
TI  - The metabolism of (2-cyclopentyl-6,7-dichloro-2-methyl-1-oxo-5-indanyloxy)acetic acid in chimpanzee and man.
DP  - 1978 May 01
TA  - Drug Metabolism and Disposition
PG  - 303--312
VI  - 6
IP  - 3
4099  - http://dmd.aspetjournals.org/content/6/3/303.short
4100  - http://dmd.aspetjournals.org/content/6/3/303.full
SO  - Drug Metab Dispos1978 May 01; 6
AB  - The metabolism of the polyvalent saluretic agent (2-cyclopentyl-6,7-dichloro-2-methyl-1-oxo-5-indanyloxy)acetic acid was studied in chimpanzee and man. The drug was well absorbed and extensively metabolized by man. Peak levels of drug (5--8 microgram/ml) occurred within 1.5--4.5 hr of drug administration. The plasma half-life was estimated to be 2 hr; a similar half-life was observed in the chimpanzee. Little unchanged drug (less than 10%) was excreted in the urine of either species. Similar metabolic profiles were obtained for man and chimpanzee. The major urinary metabolites resulted from hydroxylation of the cyclopentyl moiety, giving rise to a number of diastereomers. The alcohol metabolites were subsequently oxidized to the ketone. The excretion of the metabolites coincided with maximal excretion of sodium and chloride ions. The hydroxylated metabolites have intrinsic pharmacological activity.