GBR 12935 HCl
| CAS号 | 67469-81-2 | 货号 | BCP09762 |
| 中文名 | GBR 12935 HCl | ||
| 英文名 | GBR 12935 HCl | ||
| 中文别名 | |||
| 英文别名 | GBR12935;GBR-12935; | ||
| 分子式 | C28H36Cl2N2O | 分子量 | 487.5 |
| 生物活性 | in vitro: The calculated Kd of [3H]GBR-12935 binding to CYP2D6 was 42.2 nM, indicating that GBR-12935 has a high affinity for CYP2D6. The binding of [3H]GBR-12935 to CYP2D6 was decreased partially by substrates or inhibitors of CYP2D isoforms (quinine, quinidine, propranolol, bufuralol, imipramine, and desipramine) . Co-perfusion of 100 microM GBR 12909 or GBR 12935 with either 100 microM sulpiride or raclopride produced a significant reduction in the GBR 12909 or GBR 12935 induced increase in the extracellular levels of dopamine to basal levels. In vitro, GBR 12909 (1-9 nM) dose-dependently inhibited active uptake of [3H]dopamine in homogenates of the nucleus accumbens . in vivo: GBR 12935 elevated locomotion to a greater extent in C57BL/6J mice at the maximally active dose of 10 mg/kg. Locomotor stimulation by GBR 12935 remained consistent in both strains with repeated injections. DBA/2J mice became sensitized to cocaine-induced stereotypy with repeated injections. Cocaine induced no | ||
| 信号通路 | Neuro Signaling Pathway | ||
| 靶 点 | Dopamine Transporter | ||
结构式
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