Abstract
In human blood platelet membranes, 5-HT displaced the binding of the putative selective D-1 dopamine receptor antagonist [ 3H]SCH 23390 in a competitive manner with a K i value of 5.7 ± 0.8 nM, which was about 1000-fold lower than the K i value for dopamine (K i = 4400 ± 150 nM. Thus the ‘D-1 dopamine-like’ site in human blood platelet membranes described previously corresponds to a 5-HT 1-type site. [ 3H]SCH 23390 competition experiments with a number of serotonergic drugs disclosed a pharmacological profile that was distinct from the four 5-HT 1 site subtypes reported previously. We therefore propose that this novel 5-HT site be designated the 5-HT 1E site. Binding of [ 3H]SCH 23390 to 5-HT 1-type sites could not be detected in several regions of the human brain. In some regions, however, 5-HT displaced part of the [ 3H]SCH 23390 binding with a K 1 value of 320–380 nM. These sites correspond to 5-HT 2 receptors.
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