Sarpogrelate hydrochloride

A potent, specific 5HT2 receptor antagonist with Ki of 8.39 nM for 5-HT2A; also shows binding affinity for 5-HT2B; displays selectivity over 5-HT1-like, 5-HT3, beta, H1, H2 and M3; blocks serotonin-induced platelet aggregation.Heart Failure Approved (In Vitro) :Sarpogrelate is selective for 5-HT2 (pKi=7.54) over 5-HT1 (pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39) .Sarpogrelate (10 μM) significantly reduces the number of platelet-rich plasma (PRP) -induced THP-1 cell that adheres to human umbilical vein endothelial cells (HUVECs) .Sarpogrelate (10 μM) significantly reduces the expression of PRP-induced E-selectin in HUVECs. (In Vivo) :Sarpogrelate (5 mg/kg; i.p. daily for 4 weeks) inhibits HFFD-induced obesity and decreases leukocyte-endothelial interactions in mice.