Sarpogrelate hydrochloride
Cat. No.：YN320291
CAS No. ：135159-51-2
| 产品名称: | Sarpogrelate hydrochloride |
| CAS No.: | 135159-51-2 |
| Chemical Name: | butanedioic acid, 1-[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester, monohydrochloride |
| Synonyms: | 盐酸沙格雷酯; MCI-9042 |
| 分子量: | 465.97 |
| 分子式: | C₂₄H₃₂ClNO₆ |
| SMILES: | COC1=CC=CC(CCC2=CC=CC=C2OCC(CN(C)C)OC(CCC(O)=O)=O)=C1.Cl |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Sarpogrelate hydrochloride (MCI-9042) 是一种选择性的5-HT2R拮抗剂，对 5-HT2A，5-HT2B，和 5-HT2C受体的pKi值分别为 8.52、6.57 和 7.43。Sarpogrelate hydrochloride 对 5-HT1，5-HT3，5-HT4，α1-，α2- 和 β-肾上腺素受体，组胺 H1，H2以及毒蕈碱 M3受体缺乏显著的拮抗活性。Sarpogrelate hydrochloride 可用于研究与血栓形成有关的血管疾病。 |
| IC50和靶点: | [{name:"5-HT2A Receptor:8.52 (pKi)"},{name: "5-HT2B Receptor:6.57 (pKi)"},{name: "5-HT2C Receptor:7.43 (pKi)"}] |
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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)
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)
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.818,263-270(2018)
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)
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)
