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SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor.
SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | |
50 mg | ¥ 13,800 | 6-8周 | |
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor. |
体外活性 | D3 receptor antagonist SB269,652 effectively abolished specific binding of [(3)H]nemanopride and [(3)H]spiperone to Chinese hamster ovary-transfected D(3) receptors when radioligands were used at 0.2 and 0.5 nM, respectively. However, SB269,652 only submaximally inhibited the specific binding of these radioligands when they were employed at 10-fold higher concentrations even at high concentrations (5 μM). By analogy, although SB269,652 potently blocked D(3) receptor-mediated activation of Gα(i3) and phosphorylation of extracellular-signal-regulated kinase (ERK)1/2, when concentrations of dopamine were increased by 10-fold, from 1 μM to 10 μM, SB269,652 only submaximally inhibited dopamine-induced stimulation of Gα(i3) [1]. |
分子量 | 426.55 |
分子式 | C27H30N4O |
CAS No. | 215802-15-6 |
密度 | 1.24 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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