Sarpogrelate
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| AHFS/Drugs.com | International Drug Names |
| ATC code | none |
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| Synonyms | Sarpogrelate, (−)-4-[1-dimethylamino-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]propan-2-yl]oxy-4-oxobutanoic acid |
| CAS Number | 125926-17-2  |
| PubChem (CID) | 5160 |
| IUPHAR/BPS | 210 |
| ChemSpider | 4976  |
| UNII | 19P708E787 |
| ChEMBL | CHEMBL52939 |
| Chemical and physical data | |
| Formula | C24H31NO6 |
| Molar mass | 429.506 g/mol |
| 3D model (Jmol) | Interactive image |
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Sarpogrelate (brand name Anplag; 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[edit]
References[edit]
- ^ 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. Journal of Pharmacy and Pharmacology. 1995 Apr;47(4):310-6. PMID 7791029
- ^ 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 Thérapie. 1996 Mar-Apr;331(2):189-202. PMID 8937629
- ^ 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. 2007 Jul;104(3):274-7. PMID 17609583
- ^ 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. 1993 Apr 15;70(2):131-8. PMID 8322284
- ^ Ogawa S, Takeuchi K, Sugimura K, Sato C, Fukuda M, Lee R, Ito S, Sato T. 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 and Physiology. 1999 May-Jun;26(5-6):461-4. PMID 10386239
- ^ 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. 1996 Dec 15;84(6):445-52. PMID 8987165
- ^ 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. Journal of Dermatology. 2000 Oct;27(10):643-50. PMID 11092268
- ^ 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. 2002 Jan;25(1):28-32. PMID 11808836
- ^ 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. 2002 Aug;144(2):E1. PMID 12177659
- ^ Hayashi T, Sumi D, Matsui-Hirai H, Fukatsu A, Arockia Rani P J, Kano H, Tsunekawa T, Iguchi A. Sarpogrelate HCl, a selective 5-HT2A antagonist, retards the progression of atherosclerosis through a novel mechanism. Atherosclerosis. 2003 May;168(1):23-31. PMID 12732383
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