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Functional distinction between serotonin uptake and serotonin-induced shape change receptors in rat platelets
Authors:Maria Grazia Lampugnani  Giovanni de Gaetano  Ennio C. Rossi
Affiliation:1. Laboratory of Cardiovascular Clinical Pharmacology, Mario Negri Institute for Pharmacological Research, Via Eritrea 62, 20157 Milan Italy;2. Section of Hematology, Department of Medicine, Northwestern University School of Medicine, Chicago, IL U.S.A.
Abstract:Tyramine and dopamine are taken up by rat platelets through the serotonin uptake mechanism while phenethylamine is not taken up. This indicates that an aromatic hydroxyl group is a structural requirement for the uptake of phenethylamine derivatives by rat platelets. Although none of these phenethylamine derivatives induce platelet shape change, they inhibit serotonin-induced shape change and serotonin uptake with the same relative potency (tyramine >phenethylamine ? dopamine). This suggests that the receptors controlling serotonin uptake and serotonin-induced shape change have a common structural component that binds phenethylamine derivatives. However, the fact that phenethylamine derivatives activate the serotonin uptake mechanism but do not induce platelet shape change suggests that serotonin uptake and serotonin-induced shape change are mediated by two distinct activation sites of serotonin receptors.
Keywords:Amine uptake  Phenethylamine derivative  Platelet shape change  Serotonin receptor  (Rat platelet)
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