产品
编 号：F453571
分子式：C28H34N2O
分子量：414.58
分子式：C28H34N2O
分子量：414.58
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CAS No: 76778-22-8
产品详情
生物活性：
GBR 12935 is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice.
体内研究：
GBR 12935 (1-32 mg/kg; repeat injection; 7 d) elevates locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice, and (10 mg/kg; injection; 7 d) results few mice sensitized to cocaine-induced stereotypy with repeated injections.Animal Model:Adult male DBA/2J and C57BL/6J mice (22-30 g)
Dosage:1.0, 3.2, 10, 32 mg/kg
Administration:Repeat injection; for 7 days
Result:Elevated locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice.No stereotypy was induced by an eighth day challenge of 10 mg/kg GBR 12935 in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.
体外研究：
GBR 12909 (10-100 nM) also shows a high affinity for CYP2D6 with the Kd value of 42.2 nM, lower than the affinity for dopamine transporter. The binding effect can be reduced by Quinidine (HY-B1751) and Quinine (HY-D0143), which are the specific and potent inhibitors of CYPZD enzymatic activities.GBR 12935 (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens.GBR 12935 (100 μM; 60 min) increases extracellular levels of dopamine compared with levels for artificial cerebrospinal fluid (ACSF) by local perfusion for 60 min.GBR 12935 (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens.Co-perfusion of 100 μM GBR 12935 with either 100 μM Sulpiride (HY-B1019) or Raclopride (HY-103414) produces a significant reduction in the GBR 12935 induced increase in the extracellular levels of dopamine to basal levels.
GBR 12935 is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice.
体内研究：
GBR 12935 (1-32 mg/kg; repeat injection; 7 d) elevates locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice, and (10 mg/kg; injection; 7 d) results few mice sensitized to cocaine-induced stereotypy with repeated injections.Animal Model:Adult male DBA/2J and C57BL/6J mice (22-30 g)
Dosage:1.0, 3.2, 10, 32 mg/kg
Administration:Repeat injection; for 7 days
Result:Elevated locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice.No stereotypy was induced by an eighth day challenge of 10 mg/kg GBR 12935 in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.
体外研究：
GBR 12909 (10-100 nM) also shows a high affinity for CYP2D6 with the Kd value of 42.2 nM, lower than the affinity for dopamine transporter. The binding effect can be reduced by Quinidine (HY-B1751) and Quinine (HY-D0143), which are the specific and potent inhibitors of CYPZD enzymatic activities.GBR 12935 (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens.GBR 12935 (100 μM; 60 min) increases extracellular levels of dopamine compared with levels for artificial cerebrospinal fluid (ACSF) by local perfusion for 60 min.GBR 12935 (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens.Co-perfusion of 100 μM GBR 12935 with either 100 μM Sulpiride (HY-B1019) or Raclopride (HY-103414) produces a significant reduction in the GBR 12935 induced increase in the extracellular levels of dopamine to basal levels.
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