2934185-00-7

Sarpogrelate-d3 is intended for use as an internal standard for the quantification of sarpogrelate (hydrochloride) (Item No. 24194) 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 (Item No. 14332) with collagen, and 5-HT with ADP (Item No. 16778; IC50s = 57.7, 0.56, and 22.7 μM, respectively).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.5WARNING This product is not for human or veterinary use.

[1] MAMUNUR RASHID . 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 modeling[J]. Life sciences, 2003, 73 2: Pages 193-207. DOI: 10.1016/s0024-3205(03)00227-3
[2] K MARUYAMA. MCI-9042: high affinity for serotonergic receptors as assessed by radioligand binding assay.[J]. Journal of pharmacobio-dynamics, 1991, 14 4: 177-181. DOI: 10.1248/bpb1978.14.177
[3] MONIKA KUBACKA . 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 ARC239[J]. European journal of pharmacology, 2018, 818: Pages 263-270. DOI: 10.1016/j.ejphar.2017.10.053
[4] H. KATAOKA. Inhibitory Effect of Serotonin Antagonist on Leukocyte-Endothelial Interactions In Vivo and In Vitro[J]. PLoS ONE, 2016, 11 1. DOI: 10.1371/journal.pone.0147929
[5] D. BRASIL. Blockade of 5-HT2A Receptors by Sarpogrelate Protects the Heart Against Myocardial Infarction in Rats[J]. Journal of Cardiovascular Pharmacology and Therapeutics, 2002, 7 1: 53-59. DOI: 10.1177/107424840200700i108