货号 | 11982-1mg |
描述 | SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and <5.2 for D2, 5-HT1D and 5-HT1Brespectively).1,2,3 It has high oral bioavailability and enters the central nervous system of the rat.1 SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.2,4 |
供应商 | Cayman |
应用文献 | |
1.Stemp, G.,Ashmeade, T.,Branch, C.L., et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J.Med.Chem. 43(9), 1878-1885 (2000). 2.Reavill, C.,Taylor, S.G.,Wood, M.D., et al. Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A. J.Pharmacol.Exp.Ther. 294(3), 1154-1165 (2000). 3.Heidbreder, C.A.,Gardner, E.L.,Xi, Z.-X., et al. The role of central dopamine D3 receptors in drug addiction: a review of pharmacological evidence. Brain Res.Rev. 49(1), 77-105 (2005). 4.Carcinella, S.,Drui, G.,Boulet, S., et al. Implication of dopamine D3 receptor activation in the reversion of Parkinson’s disease-related motivational deficits. Transl.Psychiatry 4(e401), (2014). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 511.5 |
分子式 | C28H30N4O • 2HCl |
CAS号 | 1226917-67-4 |
稳定性 | ≥ 2 years |
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