[Effect of reserpine on monoamine uptake by rat brain synaptosomes].
With regard to the inhibition of monoamine-uptake the concentration response curve of reserpine shows a biphasice turn. The first phase produces a maximum dopamin-uptake inhibition of 55% (EC50:8 X 10(-9) mol X 1(-1)) which is of a competitive manner only in the presence of a very low reserpine concentration (1 X 10(-9) mol X 1(-1)). Higher concentrations of reserpine inhibit the dopamine-uptake non competitively. This specific irreversible vesicular reserpine effect used therapeutically forms a plateau within a concentration rank from 10(-7) mol X 1(-1) to 10(-5) mol X 1(-1). A second mode of action of reserpine affects obviously the carrier mechanism located at the synaptosomal membrane (EC50: 5 X 10(-5) mol X 1(-1)). This second phase differs both from the first vesicular reserpine effect and from the synaptosomal action of tricyclic antidepressant drugs by its kinetic behavior (Km, Vmax).
D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism*; D007700:Kinetics; D051381:Rats; D012110:Reserpine / Q000494:pharmacology*; D012701:Serotonin / Q000378:metabolism*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism*
D012701:Serotonin; D012110:Reserpine; D004298:Dopamine
Beeinflussung der Monaminaufnahme in Synaptosomen des Rattenhirns durch Reserpin.