GBR-12935

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GBR 12935 诱导细胞外多巴胺水平增加至基础水平。

GBR 12935 induced increase in the extracellular levels of dopamine to basal levels.

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 dihydrochloride (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens.GBR 12935 dihydrochloride (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 dihydrochloride (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens.Co-perfusion of 100 μM GBR 12935 dihydrochloride with either 100 μM Sulpiride (HY-B1019) or Raclopride (HY-103414) produces a significant reduction in the GBR 12935 dihydrochloride induced increase in the extracellular levels of dopamine to basal levels.

GBR 12935 dihydrochloride (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 dihydrochloride in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.

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GPCR/G Protein

Dopamine Receptor

Dopamine

Neurological Disease

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67469-81-2

487.5

C28H36Cl2N2O

>98% (HPLC)

Soluble in DMSO

Cl.Cl.C(CN1CCN(CCOC(C2=CC=CC=C2)C2=CC=CC=C2)CC1)CC1=CC=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years