The Uptake of 6‐Methoxy‐1,2,3,4‐Tetrahydro‐β‐carboline and its Effect on 5‐Hydroxytryptamine Uptake and Release in Blood Platelets

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Abstract
The uptake of 6‐methoxy‐1,2,3,4‐tetrahydro‐β‐carboline (6‐MeOTHBC, 5‐methoxytryptoline) by rabbit blood platelets was studied by using 3H‐labelled compound. A high rate active uptake (Km 6.6 μM), which was inhibited by 5‐hydroxytryptamine (5‐HT) and cinnanserine, and a slow rate uptake, not inhibited by 5‐HT were observed. The intracellular distribution of 3H‐6‐McOTHBC in platelets clearly differed from that of 14C‐5‐HT. 6‐MeOTHBC also competitively inhibited the high‐rate active (but not the slow passive) uptake of 14C‐5‐HT, being more active than 5‐HT itself. The spontaneous release of the newly taken‐up 14C‐5‐HT from platelets was increased only with high concentrations of 6‐MeOTHBC.