RS-127445 hydrochloride
Cat. No.：YN320982
| 产品名称: | RS-127445 hydrochloride |
| CAS No.: | 199864-86-3 |
| Chemical Name: | 4-(4-fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine, monohydrochloride |
| Synonyms: | 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐,RS 127445,MT 500 |
| 分子量: | 317.79 |
| 分子式: | C₁₇H₁₇ClFN₃ |
| SMILES: | NC1=NC(C(C)C)=CC(C2=C3C=CC=CC3=C(F)C=C2)=N1.[H]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: | RS-127445 hydrochloride 是一种有效的，具有口服活性的，高亲和力选择性5-HT2B受体拮抗剂，pKi为 9.5，比作用于其他受体和离子通道的选择性高 1000 倍。 |
| IC50和靶点: | [{name:"sPLA2:5.5 (pKi)"},{name: "5-HT3 Receptor:<6 (pKi)"},{name: "5-HT5 Receptor:<6 (pKi)"},{name: "5-HT6 Receptor:<6 (pKi)"},{name: "5-HT2A Receptor:6.3 (pKi)"},{name: "5-HT2C Receptor:6.4 (pKi)"},{name: "5-HT2B Receptor:9.5 (pKi)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Bonhaus, D.W., Flippin, L.A., Greenhouse, R.J., et al.RS-127445: A selective, high affinity, orally bioavailable 5-HT2B receptor antagonistBr. J. Pharmacol.127(5),1075-1082(1999)
Bassil, A.K., Taylor, C.M., Bolton, V.J., et al.Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiologyBr. J. Pharmacol.158(1),252-258(2009)
Devroye, C., Cathala, A., Di Marco, B., et al.Central serotonin2B receptor blockade inhibits cocaine-induced hyperlocomotion independently of changes of subcortical dopamine outflowNeuropharmacology97,329-337(2015)
