Inhibition of rat platelet 5-hydroxytryptamine uptake by chlordimeform.
Chlordimeform, a formamidine insecticide and acaricide, and two of its toxic N-demethyl metabolites inhibited rat blood platelet 5-hydroxytryptamine (5-HT) uptake. A direct relationship existed between formamidine uptake inhibitory potency and N-demethylation. Didemethylchlordimeform, the most potent formamidine inhibitor of 5-HT uptake examined, had a pI50 of 4.2. However, it was appreciably less active than the classical inhibitor imipramine, which yielded 86.4% inhibition of 5-HT uptake at a concentration of 1.10(-5) M.
D000578:Amidines / Q000494:pharmacology*; D000818:Animals; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D002742:Chlorphenamidine / Q000494:pharmacology*; D003864:Depression, Chemical; D007099:Imipramine / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000097:blood*
D000578:Amidines; D012701:Serotonin; D002742:Chlorphenamidine; D007099:Imipramine