Sarpogrelate
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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[1][2] 5-HT2B, and 5-HT2C receptors.[3][4] 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.[3] The drug blocks serotonin-induced platelet aggregation, and has potential applications in the treatment of many diseases including diabetes mellitus,[5][6] Buerger's disease,[7] Raynaud's disease,[8] coronary artery disease,[9] angina pectoris,[10] and atherosclerosis.[11]
The predicted log P (XLogP3) of sarpogrelate is 1.2.[12] A 2004 review stated that it was unknown whether sarpogrelate crosses the blood–brain barrier.[13] However, other papers have stated that sarpogrelate minimally crosses into the brain and hence is peripherally selective.[14][15][16] Accordingly, a rat study found that peak sarpogrelate levels were 50-fold lower in the brain and spinal cord than in the circulation.[16][17]
See also
References
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