Platelet uptake of serotonin following repeated administration of 3-cyano-imipramine to healthy volunteers.
In a double blind, placebo-controlled study the effects of daily oral administration of 3-cyano-imipramine on the 3H-serotonin uptake capacity of platelets were investigated in healthy volunteers. The initial dose was 1 mg, rising to 3 mg daily for 7 days. A rapid and profound inhibition of 3H-serotonin uptake was observed in platelets isolated from the treated subjects. During repeated administration, uptake was reduced to less than 10% of pre-drug values. Five days after the final dose uptake had only partially recovered, to 53% of pre-drug values. A similar inhibition profile was observed when serum from the treated subjects was incubated with normal platelets and 3H-serotonin. The results establish 3-cyano-imipramine as a potent inhibitor of platelet serotonin uptake in humans.
D000293:Adolescent; D000328:Adult; D001792:Blood Platelets / Q000378:metabolism*; D004311:Double-Blind Method; D006801:Humans; D007099:Imipramine / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D012701:Serotonin / Q000097:blood*; D012702:Serotonin Antagonists / Q000494:pharmacology*
D012702:Serotonin Antagonists; C024316:cianopramine; D012701:Serotonin; D007099:Imipramine