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

GBR 12935 dihydrochloride 

Cat. No.: HY-12242 Purity: 99.45%
COA Handling Instructions

GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice.

For research use only. We do not sell to patients.

GBR 12935 dihydrochloride Chemical Structure

GBR 12935 dihydrochloride Chemical Structure

CAS No. : 67469-81-2

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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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50 mg USD 132 In-stock
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100 mg USD 238 In-stock
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Description

GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride 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 dihydrochloride (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 dihydrochloride (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 dihydrochloride (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 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[2].

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

In Vivo

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[3].

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 dihydrochloride in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.
Molecular Weight

487.50

Formula

C28H36Cl2N2O

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (51.28 mM; Need ultrasonic)

H2O : 7.14 mg/mL (14.65 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0513 mL 10.2564 mL 20.5128 mL
5 mM 0.4103 mL 2.0513 mL 4.1026 mL
10 mM 0.2051 mL 1.0256 mL 2.0513 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
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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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Product Name:
GBR 12935 dihydrochloride
Cat. No.:
HY-12242
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