1. Neuronal Signaling
  2. Dopamine Transporter
  3. GBR 12935

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (GBR 12935 dihydrochloride) usually boasts enhanced water solubility and stability.

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GBR 12935 Chemical Structure

GBR 12935 Chemical Structure

CAS No. : 76778-22-8

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Description

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[1][2][3][4].

In Vitro

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[1].
GBR 12935 (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens[2].
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[2].
GBR 12935 (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens[2].
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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male DBA/2J and C57BL/6J mice (22-30 g)[3]
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.
Molecular Weight

414.58

Formula

C28H34N2O

CAS No.
SMILES

N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(CCCC4=CC=CC=C4)CC1

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GBR 12935 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GBR 12935
Cat. No.:
HY-12242A
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