GBR-12935

Research use only, not for human use.

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

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