Abstract
The effect of 5-hydroxytryptamine (5-HT), tryptamine (T), 6-hydroxy-1,2,3,4-tetrahydroharmane (6-HTH), and 1,2,3,4-tetrahydroharmane (TH) on the accumulation of radioactive 5-HT and histamine, was studied in rabbit blood platelets. 6-HTH and TH inhibited the uptake of the labelled amine, but they were weaker inhibitors than 5-HT or T. All four compounds inhibited the accumulation of radioactive histamine in the granules as well as in the whole cells, but the latter effect is not the consequence of inhibition of granular accumulation. It is concluded that the methylene bridge, which is the most important structural difference between the harmanes and the tryptamines, does not abolish the affinity of the molecule to the uptake receptor at the platelet membrane. However, since the inhibitory potency was lower than that of the parent amines, one cannot be certain as to whether or not the conformation present in the harmane derivatives offers the best fit for the receptor.
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