Sarpogrelate-d3 is intended for use as an internal standard for the quantification of sarpogrelate (hydrochloride) by GC- or LC-MS. Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).1 It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).2 In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT with collagen, and 5-HT with ADP .3 In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.4 Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.5
1.Rashid, M., Manivet, P., Nishio, H., et al.Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modelingLife Sci.73(2)193-207(2003) 2.Maruyama, K., Kinami, J., Sugita, Y., et al.MCI-9042: High affinity for serotonergic receptors as assessed by radioligand binding assayJ. Pharmacobiodyn.14(4)177-181(1991) 3.Kubacka, M., Kazek, G., Kotańska, M., et al.Anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine is due to their 5-HT2A and α2-adrenoceptor antagonistic properties. A comparison with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239Eur. J. Pharmacol.818263-270(2018) 4.Kataoka, H., Ariyama, Y., Deushi, M., et al.Inhibitory effect of serotonin antagonist on leukocyte-endothelial interactions in vivo and in vitroPLoS One11(1)e0147929(2016) 5.Brasil, D., Temsah, R.M., Kumar, K., et al.Blockade of 5-HT2A receptors by sarpogrelate protects the heart against myocardial infarction in ratsJ. Cardiovasc. Pharmacol. Ther.7(1)53-59(2002)