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SB-277011 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-277011 dihydrochloride图片
CAS NO:1226917-67-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
SB-277011A dihydrochloride
产品介绍
SB-277011 dihydrochloride (SB-277011A dihydrochloride) 是一种有效的,选择性的,可口服的,可透过血脑屏障的dopamine D3受体拮抗剂,对 D3,D2,5-HT1B和 5-HT1D受体的pKi值分别为 8.0,6.0,<5.2 和 5.9。
生物活性

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetratedopamineD3receptorantagonist, withpKis of 8.0, 6.0,<5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1Dreceptors, respectively.

IC50& Target

pKi: 8.0 (D3receptor), 6.0 (D2receptor),<5.2 (5-HT1Breceptor), 5.9 (5-HT1Dreceptor)[1]

体外研究
(In Vitro)

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1Dreceptors, with pKis of 8.0, 6.0,<5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1Dreceptors, respectively[1].

体内研究
(In Vivo)

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].
SB-277011A (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011A can significantly inhibit basal and cocaine-enhanced locomotion in rats[2].

分子量

511.49

Formula

C28H32Cl2N4O

CAS 号

1226917-67-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.