Sex difference of the metabolic disposition of clioquinol in rats.
The order of plasma levels of clioquinol and its conjugates in male rats after intraduodenal administration of 32.7 mumol/kg dose of clioquinol was clioquinol sulfate (C-Sul) greater than glucuronide (C-Glu) much greater than clioquinol, whereas that in female rats was C-Glu greater than C-Sul much greater than clioquinol. Total (urine + bile) recovery was almost the same among male and female rats. The percentage of excretion amounts of C-Sul (urine + bile) to the total excretion amounts for 24 h in male rats after intravenous administration of clioquinol was about twice that in female rats, while the percentage of excretion amounts of C-Glu to the total excretion amounts in male rats was smaller than that in female rats. In intravenous administration of 16.4 mumol/kg dose of C-Glu, C-Sul and clioquinol other than C-Glu were found in bile and urine of male and female rats. The percentage of excretion amounts of C-Sul and C-Glu (urine + bile) to the total excretion amounts was similar among male and female rats, respectively. In intravenous administration of 16.4 mumol/kg dose of C-Sul, C-Glu and clioquinol other than C-Sul were found in bile and urine of male and female rats, and the percentage of excretion amounts of C-Sul (urine + bile) to the total excretion amounts in male rats was 1.3 fold that in female rats.(ABSTRACT TRUNCATED AT 250 WORDS)
Ohshima
N
N
Hospital Pharmacy, Faculty of Medicine, University of Tokyo, Japan.
Kotaki
H
H
Saitoh
Y
Y
Nakagawa
F
F
Tamura
Z
Z
D000818:Animals; D001646:Bile / Q000378:metabolism; D007464:Clioquinol / Q000031:analogs & derivatives / Q000378:metabolism* / Q000652:urine; D005260:Female; D006912:Hydroxyquinolines / Q000378:metabolism*; D007262:Infusions, Intravenous; D007263:Infusions, Parenteral; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012727:Sex Characteristics
D006912:Hydroxyquinolines; C062045:clioquinol glucuronide; D007464:Clioquinol