5-Hydroxytryptamine and dopamine transport by rat and human blood platelets

British Journal of Pharmacology
J L Gordon, H J Olverman


1 Uptake of 5-hydroxytryptamine (5-HT) by rat platelets in plasma was very rapid and diffusion did not contribute significantly at substrate concentrations that did not saturate the active transport.2 Under conditions which allowed measurement of initial rates of uptake, kinetic analysis revealed a high affinity uptake mechanism for 5-HT (K(m) = 0.7 muM).3 Uptake of dopamine was relatively slow and involved a lower affinity (K(m) = 70 muM) active transport process. Diffusion contributed significantly at concentrations that did not saturate the active transport.4 5-HT competitively inhibited uptake of dopamine, and vice versa; K(i) values for both amines were similar to their respective K(m) values for uptake.5 Chlorimipramine, desmethylimipramine and benztropine were tested as uptake inhibitors. Each was equipotent against 5-HT and dopamine, although the absolute potency of the drugs varied greatly. Chlorimipramine was the most potent (K(i)## 100 nM), and kinetic analysis revealed that the inhibition was competitive against both 5-HT and dopamine.6 Similar results were obtained in studies with human platelets: K(m) values for 5-HT and dopamine were about 1 muM and 100 muM respectively. Activity profiles of inhibitors were also ...Continue Reading


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