Sarpogrelate

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IUPAC_name = (-)-4- [1-dimethylamino-3- [2- [2-(3-methoxyphenyl)ethyl] phenoxy] propan-2-yl] oxy-4-oxobutanoic acid

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CAS_number = 125926-17-2
synonyms = Sarpogrelate
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PubChem = 5160
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C = 24 | H = 31 | N = 1 | O = 6
molecular_weight = 429.506 g/mol
smiles = CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O
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Sarpogrelate (Anplag, MCI-9042, LS-187,118) is a drug which acts as an antagonist at the 5HT_2A receptor. [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 Therapie". 1996 Mar-Apr;331(2):189-202. PMID 8937629] It blocks serotonin-induced platelet aggregation, and has applications in the treatment of many diseases including diabetes mellitus, [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] Buerger's disease, [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] Raynaud's disease, [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] coronary artery disease, [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] angina pectoris, [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] and atherosclerosis. [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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