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SB 277011A dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB 277011A dihydrochloride图片
CAS NO:1226917-67-4
规格:98%
分子量:511.49
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
dopamine D3 receptor antagonist
CAS:1226917-67-4
分子式:C28H30N4O.2HCl
分子量:511.49
纯度:98%
存储:Store at -20°C

Background:

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0,<5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.


SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors, with pKis of 8.0, 6.0,<5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1].


SB-277011 dihydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats[1].


参考文献:
[1]. Stemp G, 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. 2000 May 4;43(9):1878-85.