Chemistry:Sarpogrelate

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Sarpogrelate (INN, JAN), sold under the brand names Anplag and Sapodifil, is a serotonin 5-HT2 receptor antagonist which is used in the treatment of arterial occlusive disorders such as peripheral artery disease in Japan, South Korea, and China.[1][2][3][4] Development in the United States and the European Union was discontinued and it is not available in these regions.[1][3]

The drug acts as an antagonist at the serotonin 5-HT2A,[5][6] 5-HT2B, and 5-HT2C receptors.[7][8] 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.[7] The drug blocks serotonin-induced platelet aggregation, and has potential applications in the treatment of many diseases including diabetes mellitus,[9][10] Buerger's disease,[11] Raynaud's disease,[12] coronary artery disease,[13] angina pectoris,[14] and atherosclerosis.[15]

The predicted log P (XLogP3) of sarpogrelate is 1.2.[16] A 2004 review stated that it was unknown whether sarpogrelate crosses the blood–brain barrier.[17] However, other papers have stated that sarpogrelate minimally crosses into the brain and hence is peripherally selective.[18][19][20] Accordingly, a rat study found that peak sarpogrelate levels were 50-fold lower in the brain and spinal cord than in the circulation.[20][21]

See also

References

  1. ↑ 1.0 1.1 "Sarpogrelate". 12 December 2025. https://adisinsight.springer.com/drugs/800002129. 
  2. ↑ Index Nominum: International Drug Directory. CRC Press. 2004. ISBN 978-3-88763-101-7. https://books.google.com/books?id=EgeuA47Ocm4C&pg=PA1086. Retrieved 16 January 2026. 
  3. ↑ 3.0 3.1 Pilowsky, Paul M. (21 September 2018). Serotonin: The Mediator that Spans Evolution. Academic Press. ISBN 978-0-12-800584-2. https://books.google.com/books?id=jtycBAAAQBAJ&pg=PA111. Retrieved 16 January 2026. "Sarpogrelate hydrochloride remains on market, albeit limited to circulation in Japan, China, and Korea, with development in the United States and EU discontinued. Sarpogrelate hydrochloride (brand name Anplag) is structurally different from Ketanserin, a feature presumably contributing to its improved receptor subtype selectivity. Although Anplag demonstrated lower bleeding rates compared to those induced with aspirin, trials for use in stroke were discontinued, and Anplag remains contraindicated for patients at increased bleeding risk. Anplag is currently only available for chronic arterial occlusion and has been demonstrated to be particularly effective on the collateral circulation, with its main utility for the treatment of peripheral arterial disease (PAD) [169]. A sustained-release formulation of Sarpogrelate hydrochloride (DP-R202 or Sapodifil SR, once daily) was launched in Korea in May of 2015, again for use in PAD." 
  4. ↑ "Sarpogrelate controlled release". 31 October 2021. https://adisinsight.springer.com/drugs/800045361. 
  5. ↑ "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. doi:10.1111/j.2042-7158.1995.tb05801.x. PMID 7791029. 
  6. ↑ "Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes". Archives Internationales de Pharmacodynamie et de Therapie 331 (2): 189–202. 1996. PMID 8937629. 
  7. ↑ 7.0 7.1 "Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling". Life Sci 73 (2): 193–207. May 2003. doi:10.1016/s0024-3205(03)00227-3. PMID 12738034. 
  8. ↑ "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. doi:10.1254/jphs.sc0060241. PMID 17609583. 
  9. ↑ "The effect of MCI-9042 on serotonin-induced platelet aggregation in type 2 diabetes mellitus". Thrombosis Research 70 (2): 131–8. April 1993. doi:10.1016/0049-3848(93)90154-g. PMID 8322284. 
  10. ↑ "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 26 (5–6): 461–4. 1999. doi:10.1111/j.1440-1681.1999.03056.x. PMID 10386239. 
  11. ↑ "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. doi:10.1016/s0049-3848(96)00212-5. PMID 8987165. 
  12. ↑ "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. doi:10.1111/j.1346-8138.2000.tb02246.x. PMID 11092268. 
  13. ↑ "Sarpogrelate, a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease". Clinical Cardiology 25 (1): 28–32. January 2002. doi:10.1002/clc.4950250108. PMID 11808836. 
  14. ↑ "Effectiveness of a novel serotonin blocker, sarpogrelate, for patients with angina pectoris". American Heart Journal 144 (2): A1–A6. August 2002. doi:10.1067/mhj.2002.124056. PMID 12177659. 
  15. ↑ "Sarpogrelate HCl, a selective 5-HT2A antagonist, retards the progression of atherosclerosis through a novel mechanism". Atherosclerosis 168 (1): 23–31. May 2003. doi:10.1016/s0021-9150(03)00054-6. PMID 12732383. 
  16. ↑ "Sarpogrelate". https://pubchem.ncbi.nlm.nih.gov/compound/5160. 
  17. ↑ "Therapeutic potentials of sarpogrelate in cardiovascular disease". Cardiovasc Drug Rev 22 (1): 27–54. 2004. doi:10.1111/j.1527-3466.2004.tb00130.x. PMID 14978517. 
  18. ↑ "Sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, attenuates neurogenic pain induced by nucleus pulposus in rats". Spine (Phila Pa 1976) 32 (3): 315–320. February 2007. doi:10.1097/01.brs.0000253601.35732.c1. PMID 17268262. 
  19. ↑ "Antinociception in rat by sarpogrelate, a selective 5-HT(2A) receptor antagonist, is peripheral". Eur J Pharmacol 404 (1–2): 95–102. September 2000. doi:10.1016/s0014-2999(00)00522-7. PMID 10980267. 
  20. ↑ 20.0 20.1 "Effects of a 5-HT2A receptor antagonist, sarpogrelate on thermal or inflammatory pain". Eur J Pharmacol 516 (1): 18–22. May 2005. doi:10.1016/j.ejphar.2005.04.026. PMID 15916757. "After oral administration of sarpogrelate to rats, the peak sarpogrelate concentration in the brain and spinal cord was about 2% of the plasma concentration (Komatsu et al., 1991). Thus, sarpogrelate has very low permeability of the blood–brain barrier.". 
  21. ↑ "Studies on the Metabolic Fate of (.+-.)-2-(Dimethylamino)-1-((o-(m-methoxyphenethyl)-phenoxy)methyl)ethyl hydrogen siccinate hydrochloride (MCI-9042). (II). Absorption, Distribution, Metabolism and Excretion after a Single Administration to Rats.". Drug Metabolism and Pharmacokinetics 6 (3): 377–398. 1991. doi:10.2133/dmpk.6.377. ISSN 0916-1139. 



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