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Sarpogrelate is a small molecule drug that acts as an antagonist at serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors. It has the highest affinity for the 5-HT2A receptor and much lower affinities for the other subtypes. By blocking these receptors—especially 5-HT2A—sarpogrelate inhibits serotonin-induced platelet aggregation and vasoconstriction. This mechanism underlies its use in improving vascular function and treating conditions such as peripheral arterial disease (PAD), diabetes mellitus (including diabetic nephropathy), coronary artery disease, chronic renal insufficiency, Buerger's disease, Raynaud's disease, angina pectoris, and atherosclerosis. Sarpogrelate is peripherally selective with minimal penetration into the central nervous system[1][3][4][5][6].
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