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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
GBR-12935 is a novel, potent and selective dopamine reuptake inhibitor and a piperazine derivative. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain.
| ln Vitro |
GBR 12909 (10-100 nM) demonstrates a strong affinity for CYP2D6, demonstrating a Kd value of 42.2 nM, a value that is less than that of the dopamine transporter. In addition to being strong and selective inhibitors of CYPZD enzyme activity, quinidine and quinine can lessen the binding impact [1]. Extracellular dopamine levels rise to almost 400% of basal values in the nucleus accumbens when GBR 12935 diHCl (10 nM; 2 minutes) is given [2]. Extracellular dopamine levels are higher with GBR 12935 diHClide (100 μM; 60 min) than with locally perfused artificial cerebrospinal fluid (ACSF) [2]. In nucleus accumbens homogenates, GBR 12935 diHClide (1-9 nM) dose-dependently inhibits [3H]dopamine's active absorption [2]. The extracellular dopamine levels created by GBR 12935 dihydrochloride were dramatically lowered to basal levels by co-infusion of 100 μM GBR 12935 dihydrochloride with 100 μM sulpiride or raclopride [2].
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| ln Vivo |
More locomotor activity was seen in C57BL/6J mice after repeated injections of GBR 12935 dihydrochloride (1–32 mg/kg; injection; 7 days) than in DBA/2J mice (10 mg/kg; injection; 7 days). In mice susceptible to stereotypy brought on by repeated cocaine injections, there were minimal effects [3].
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| Animal Protocol |
Animal/Disease Models: Adult male DBA/2J and C57BL/6J mice (22-30 g) [3]
Doses: 1.0, 3.2, 10, 32 mg/kg Route of Administration: Repeat injection; continued for 7 days Experimental Results: C57BL/6J The locomotor activity of mice was increased to a greater extent than that of DBA/2J mice. Challenge with 10 mg/kg GBR 12935 dihydrochloride on day eight did not induce stereotypy in mice pretreated with seven consecutive injections of 32 mg/kg cocaine or saline. |
| References |
[1]. Hiroi T, et al. Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9.
[2]. Rahman S, et al. Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 dopamine uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44. [3]. Tolliver BK, et al. Comparison of cocaine and GBR 12935: effects on locomotor activity and stereotypy in two inbred mouse strains. Pharmacol Biochem Behav. 1994 Jul;48(3):733-9. |
| Molecular Formula |
C28H36CL2N2O
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|---|---|
| Molecular Weight |
487.5042
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| CAS # |
67469-81-2
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| Related CAS # |
GBR 12935;76778-22-8
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| SMILES |
Cl[H].Cl[H].O(C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C([H])([H])C1([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~51.28 mM)
H2O : ~7.14 mg/mL (~14.65 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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