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| Targets |
GBR 12783 dihydrochloride targets the dopamine transporter (DAT). By inhibiting DAT, it blocks the reuptake of dopamine from the synaptic cleft, leading to increased extracellular dopamine levels. This mechanism makes it a valuable tool for studying the role of dopamine in various physiological and pathological processes.
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| ln Vitro |
In cell-free systems, GBR 12783 dihydrochloride inhibits [³H]dopamine uptake with high potency. It has an IC50 of 1.8 nM in rat striatal synaptosomes and 1.2 nM in mouse striatal synaptosomes. These assays confirm its potent and selective inhibition of the dopamine transporter. Cellular uptake assays demonstrate that GBR 12783 dihydrochloride potently inhibits dopamine uptake in neuronal cells. The compound blocks DAT-mediated dopamine transport, leading to increased extracellular dopamine levels. Its high potency and selectivity make it a useful tool for studying dopaminergic function in cell culture models.
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| ln Vivo |
GBR 12783 (10 mg/kg; intraperitoneal injection; 100 minutes; male Sprague-Dawley rats) therapy increases hippocampus ACh release, enhances dopamine transmission only at synapses instantly active, and enhances memory performance in a passive avoidance task[1].
In vivo, GBR 12783 dihydrochloride is used to study the behavioral and neurochemical effects of increased dopaminergic signaling. By inhibiting dopamine reuptake, it enhances dopaminergic transmission. It is used in animal models to investigate the role of dopamine in reward, locomotion, and neuropsychiatric disorders. |
| Enzyme Assay |
Dopamine uptake inhibition assays for GBR 12783 dihydrochloride are performed using synaptosomal preparations from rat or mouse striatum. [³H]Dopamine is used as the substrate, and uptake is measured in the presence of varying concentrations of the compound. IC50 values are determined from inhibition curves.
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| Cell Assay |
Cellular assays for GBR 12783 dihydrochloride are conducted using neuronal cell cultures or cells expressing the dopamine transporter. Cells are pre-incubated with the compound at various concentrations, then [³H]dopamine is added. Uptake is terminated after a defined period, and accumulated radioactivity is measured. IC50 values are calculated from concentration-response data.
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (180-200 g)[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; for 100 minutes Experimental Results: For a moderate electric shock intensity (0.4 mA), improved retention performance, increased hippocampal acetylcholine release in vivo. In vivo studies using GBR 12783 dihydrochloride are conducted in animal models, such as rodents. The compound is administered systemically, and its effects on behavior, such as locomotor activity, and neurochemistry, such as dopamine levels, are assessed. These studies help to elucidate the role of DAT in vivo. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GBR 12783 dihydrochloride are not extensively reported in the available literature. As a potent DAT inhibitor, it is expected to be capable of crossing the blood-brain barrier. Its lipophilic nature likely contributes to its central nervous system activity.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for GBR 12783 dihydrochloride are limited. It is used in research settings at concentrations that inhibit dopamine uptake. Standard laboratory safety practices should be followed when handling the compound.
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| References |
[1]. Nail-Boucherie K, et al. The specific dopamine uptake inhibitor GBR 12783 improves learning of inhibitory avoidance and increases hippocampal acetylcholine release. Brain Res Cogn Brain Res. 1998 Oct;7(2):203-5.
[2]. Bonnet JJ, et al. GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo. Eur J Pharmacol. 1986 Feb 18;121(2):199-209. |
| Additional Infomation |
GBR 12783 dihydrochloride is a research tool for studying the dopamine transporter and dopaminergic neurotransmission. Its high potency and selectivity make it a valuable compound for investigating the role of dopamine in neuropsychiatric disorders and for the development of potential therapeutic agents. It is not approved for clinical use.
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| Molecular Formula |
C28H34CL2N2O
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| Molecular Weight |
485.49
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| Exact Mass |
484.205
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| CAS # |
67469-75-4
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| Related CAS # |
GBR 12783;67469-57-2
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| PubChem CID |
24744862
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
6.603
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
477
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)/C=C/CN2CCN(CC2)CCOC(C3=CC=CC=C3)C4=CC=CC=C4.Cl.Cl
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| InChi Key |
HJDXBLLTRMCYNC-JFXLULTRSA-N
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| InChi Code |
InChI=1S/C28H32N2O.2ClH/c1-4-11-25(12-5-1)13-10-18-29-19-21-30(22-20-29)23-24-31-28(26-14-6-2-7-15-26)27-16-8-3-9-17-27;;/h1-17,28H,18-24H2;2*1H/b13-10+;;
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| Chemical Name |
1-(2-benzhydryloxyethyl)-4-[(E)-3-phenylprop-2-enyl]piperazine;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0598 mL | 10.2989 mL | 20.5977 mL | |
| 5 mM | 0.4120 mL | 2.0598 mL | 4.1195 mL | |
| 10 mM | 0.2060 mL | 1.0299 mL | 2.0598 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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