Sarpogrelate Explained

Sarpogrelate (former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the 5HT_2A^{[1] [2]} and 5-HT_2B^[3] receptors. It blocks serotonin-induced platelet aggregation, and has applications in the treatment of many diseases including diabetes mellitus,^{[4] [5]} Buerger's disease,^[6] Raynaud's disease,^[7] coronary artery disease,^[8] angina pectoris,^[9] and atherosclerosis.^[10]

See also

• Cinanserin
• Naftidrofuryl

Notes and References

1. Pertz H, Elz S . In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery . The Journal of Pharmacy and Pharmacology . 47 . 4 . 310–6 . April 1995 . 7791029 . 10.1111/j.2042-7158.1995.tb05801.x . 25311518 .
2. Nishio H, Inoue A, Nakata Y . Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes . Archives Internationales de Pharmacodynamie et de Therapie . 1996 . 331 . 2 . 189–202 . 8937629 .
3. Muntasir HA, Hossain M, Bhuiyan MA, Komiyama T, Nakamura T, Ozaki M, Nagatomo T . Identification of a key amino acid of the human 5-HT(2B) serotonin receptor important for sarpogrelate binding . Journal of Pharmacological Sciences . 104 . 3 . 274–7 . July 2007 . 17609583 . 10.1254/jphs.sc0060241 . free .
4. Pietraszek MH, Takada Y, Taminato A, Yoshimi T, Watanabe I, Takada A . The effect of MCI-9042 on serotonin-induced platelet aggregation in type 2 diabetes mellitus . Thrombosis Research . 70 . 2 . 131–8 . April 1993 . 8322284 . 10.1016/0049-3848(93)90154-g .
5. Ogawa S, Takeuchi K, Sugimura K, Sato C, Fukuda M, Lee R, Ito S, Sato T . 6 . The 5-HT2 receptor antagonist sarpogrelate reduces urinary and plasma levels of thromboxane A2 and urinary albumin excretion in non-insulin-dependent diabetes mellitus patients . Clinical and Experimental Pharmacology & Physiology . 1999 . 26 . 5–6 . 461–4 . 10.1111/j.1440-1681.1999.03056.x . 10386239 . 31041268 .
6. Rydzewski A, Urano T, Hachiya T, Kaneko H, Baba S, Takada Y, Takada A . The effect of a 5HT2 receptor antagonist sarpogrelate (MCI-9042) treatment on platelet function in Buerger's disease . Thrombosis Research . 84 . 6 . 445–52 . December 1996 . 8987165 . 10.1016/s0049-3848(96)00212-5 .
7. Igarashi M, Okuda T, Oh-i T, Koga M . Changes in plasma serotonin concentration and acceleration plethysmograms in patients with Raynaud's phenomenon after long-term treatment with a 5-HT2 receptor antagonist . The Journal of Dermatology . 27 . 10 . 643–50 . October 2000 . 11092268 . 10.1111/j.1346-8138.2000.tb02246.x . 24884976 .
8. Satomura K, Takase B, Hamabe A, Ashida K, Hosaka H, Ohsuzu F, Kurita A . Sarpogrelate, a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease . Clinical Cardiology . 25 . 1 . 28–32 . January 2002 . 11808836 . 10.1002/clc.4950250108 . 6654074 .
9. Kinugawa T, Fujita M, Lee JD, Nakajima H, Hanada H, Miyamoto S . Effectiveness of a novel serotonin blocker, sarpogrelate, for patients with angina pectoris . American Heart Journal . 144 . 2 . A1–A6 . August 2002 . 12177659 . 10.1067/mhj.2002.124056 .
10. Hayashi T, Sumi D, Matsui-Hirai H, Fukatsu A, Arockia Rani PJ, Kano H, Tsunekawa T, Iguchi A . 6 . Sarpogrelate HCl, a selective 5-HT2A antagonist, retards the progression of atherosclerosis through a novel mechanism . Atherosclerosis . 168 . 1 . 23–31 . May 2003 . 12732383 . 10.1016/s0021-9150(03)00054-6 .