Chemistry:Sarpogrelate

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Short description: Chemical compound
Sarpogrelate
Sarpogrelate structure.png
Clinical data
Other namesSarpogrelate, (−)-4-[1-dimethylamino-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]propan-2-yl]oxy-4-oxobutanoic acid
AHFS/Drugs.comInternational Drug Names
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC24H31NO6
Molar mass429.513 g·mol−1
3D model (JSmol)
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Sarpogrelate (former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the 5HT2A[1][2] and 5-HT2B[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

References

  1. ↑ "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. 
  2. ↑ "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. 
  3. ↑ "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. 
  4. ↑ "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. 
  5. ↑ "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. 
  6. ↑ "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. 
  7. ↑ "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. 
  8. ↑ "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. 
  9. ↑ "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. 
  10. ↑ "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. 



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