Chemical compound
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Sarpogrelate (former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the serotonin 5-HT2A 5-HT2B, and 5-HT2C receptors. However, its affinities for the human 5-HT2C and 5-HT2B receptors are about one and two orders of magnitude lower than for the human 5-HT2A receptor, respectively. The drug blocks serotonin-induced platelet aggregation, and has potential applications in the treatment of many diseases including diabetes mellitus, Buerger's disease, Raynaud's disease, coronary artery disease, angina pectoris, and atherosclerosis.
The predicted log P (XLogP3) of sarpogrelate is 1.2. A 2004 review stated that it was unknown whether sarpogrelate crosses the blood–brain barrier. However, other papers have stated that sarpogrelate minimally crosses into the brain and hence is peripherally selective. Accordingly, a rat study found that peak sarpogrelate levels were 50-fold lower in the brain and spinal cord than in the circulation.
References.
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