Sarpogrelate

Sarpogrelate (former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the serotonin 5-HT_2A^[1][2] 5-HT_2B, and 5-HT_2C receptors.^[3][4] However, its affinities for the human 5-HT_2C and 5-HT_2B receptors are about one and two orders of magnitude lower than for the human 5-HT_2A receptor, respectively.^[3] The drug blocks serotonin-induced platelet aggregation, and has potential applications in the treatment of many diseases including diabetes mellitus,^[5][6] Buerger's disease,^[7] Raynaud's disease,^[8] coronary artery disease,^[9] angina pectoris,^[10] and atherosclerosis.^[11]

Sarpogrelate

Clinical data
Other names	MCI-9042; LS-187,118
AHFS/Drugs.com	International Drug Names
ATC code	None
Identifiers
IUPAC name 4-[2-(dimethylamino)-1-({2-[2-(3-methoxyphenyl)ethyl]phenoxy}methyl)ethoxy]-4-oxobutanoic acid
CAS Number	125926-17-2 Y
PubChem CID	5160
IUPHAR/BPS	210
ChemSpider	4976 Y
UNII	19P708E787
ChEMBL	ChEMBL52939 Y
CompTox Dashboard (EPA)	DTXSID7048328
Chemical and physical data
Formula	C24H31NO6
Molar mass	429.513 g·mol−1
3D model (JSmol)	Interactive image
SMILES CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O
InChI InChI=1S/C24H31NO6/c1-25(2)16-21(31-24(28)14-13-23(26)27)17-30-22-10-5-4-8-19(22)12-11-18-7-6-9-20(15-18)29-3/h4-10,15,21H,11-14,16-17H2,1-3H3,(H,26,27) N Key:FFYNAVGJSYHHFO-UHFFFAOYSA-N N
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The predicted log P (XLogP3) of sarpogrelate is 1.2.^[12] A 2004 review stated that it was unknown whether sarpogrelate crosses the blood–brain barrier.^[13] However, other papers have stated that sarpogrelate minimally crosses into the brain and hence is peripherally selective.^[14][15][16] Accordingly, a rat study found that peak sarpogrelate levels were 50-fold lower in the brain and spinal cord than in the circulation.^[16][17]

See also

• Cinanserin
• Naftidrofuryl