Effects of imipramine and some tryptamine derivatives on the efflux of 3H-5-hydroxytryptamine from rabbit platelets.
The efflux of 3H-5-hydroxytryptamine (3H-5-HT) from rabbit platelets (monoamine oxidase inhibited; pretreatment with reserpine) was measured in the absence and presence of various concentrations of imipramine or a number of tryptamine derivatives. The maximum efflux-accelerating effect (Emax) of 5-HT and some other tryptamines (e.g., N-methyl-5-HT, 5-methoxytryptamine) far exceeded that of imipramine, whereas the Emax for 2-methyl-5-HT did not. It is concluded that tryptamines that are more effective in releasing 3H-5-HT than imipramine have the property of being substrates of the 5-HT transporter.
Wölfel
R
R
Department of Pharmacology and Toxicology, University of Würzburg, Federal Republic of Germany.
Graefe
K H
KH
D000704:Analysis of Variance; D000818:Animals; D001692:Biological Transport; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D007099:Imipramine / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D011817:Rabbits; D012701:Serotonin / Q000097:blood*; D013329:Structure-Activity Relationship; D014316:Tritium; D014363:Tryptamines / Q000494:pharmacology*
D014363:Tryptamines; D014316:Tritium; D012701:Serotonin; D007099:Imipramine