5HT2-receptors and serotonin release: their role in human platelet aggregation.

Involvement of 5HT2 receptors in human platelet aggregation was assessed by studying the effect of ADP, epinephrine and thrombin on 3H-5HT release from platelets. The release experiments were made with a perfusion method to preserve any compound, released or formed by platelet, from interacting with platelet itself. In these conditions, aggregation does not occur, as confirmed by Scanning Electron Microscopy. These release experiments showed that the platelet activation by such agents is coupled with 5-HT release. The aggregation experiments, made on different aliquots of the same platelet-rich plasma (PRP), showed that the released 5-HT, interacting with its own receptors on platelet activated surface, determines aggregation. In fact, although it is known that 5-HT added to PRP was only able to induce a moderate platelet aggregation, the 5-HT2 antagonist ketanserin counteracted the aggregation induced by ADP, epinephrine and thrombin. These results suggest that a 5HT2 antagonist could be therapeutically important in those pathological states in which serotonin, released by activated platelets, may increase aggregation.