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| 25mg |
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| Targets |
GET73 targets the metabotropic glutamate receptor 5 (mGluR5). It acts as a negative allosteric modulator, meaning it binds to a site other than the glutamate binding site and reduces the receptor's response to glutamate. It is also an analog of the natural neurotransmitter gamma-hydroxybutyrate (GHB).
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| ln Vitro |
One hour before and after chronic ethanol exposure, GET73 (1 µM, 10 µM; 1 hour) guards against ethanol-induced reductions in cell viability, cytoskeletal changes, lower extracellular glutamate levels, and enhanced reactive oxygen species formation [1].
In vitro, GET73 (1 μM, 10 μM; 1 hour) prevents ethanol-induced decreases in cell activity when administered before and during chronic ethanol exposure. It affects glutamate transmission and modulates mGluR5 activity. It is used to study the effects of ethanol on the nervous system. |
| ln Vivo |
The elevated plus maze (EPM) test in Sprague-Dawley rats exposed to GET73 (5–50 mg/kg; ir) results in anxiolytic effects [3].
In vivo, GET73 has anti-alcohol and anxiolytic properties. It significantly affects glutamate transmission in the hippocampus. Its effects make it a potential therapeutic agent for alcohol use disorders and anxiety. |
| Enzyme Assay |
Non-cellular assays for GET73 involve measuring its binding affinity to mGluR5. This is typically done using radioligand binding assays with membranes from cells expressing mGluR5. Its negative allosteric modulation can be assessed by measuring its effect on agonist-induced signaling in cell-free systems, such as GTPγS binding.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Rat Hippocampal Neurons Tested Concentrations: 0.1 µM, 1 µM, 10 µM Incubation Duration: 1 hour Experimental Results: Prevention of ethanol (75 mM, 4 days)-induced decrease in MTT. In vitro cellular assays for GET73 are conducted in cells expressing mGluR5. Its activity is assessed by measuring its effect on glutamate-induced intracellular calcium release or on the inhibition of forskolin-stimulated cAMP accumulation. Its neuroprotective effects can be studied in neuronal cell cultures exposed to ethanol. |
| Animal Protocol |
Animal/Disease Models: Male SD rat (200-300 g and 300-350 g) [3]
Doses: 5 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg Route of Administration: po (oral gavage) Experimental Results: Exerts anxiolytic effects in rats exposed to the elevated plus maze (EPM) test. In vivo animal experiments with GET73 are conducted in models of alcohol dependence and anxiety. The compound is administered, and its effects on alcohol consumption, withdrawal symptoms, and anxiety-like behaviors are assessed. Its effects on glutamate transmission can be studied using microdialysis in the hippocampus. |
| ADME/Pharmacokinetics |
GET73 has a molecular weight of 275.27 and a molecular formula of C13H16F3NO2. It is soluble in DMSO and is typically stored as a powder at -20°C. Its pharmacokinetic properties, such as oral bioavailability and brain penetration, would need to be characterized for therapeutic use.
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| Toxicity/Toxicokinetics |
GET73 is considered to have low toxicity based on its use as a research compound. However, comprehensive toxicological data are not extensively published. The compound is intended for research use only and is not approved for human therapeutic use.
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| References |
[1]. Tomasini MC, et al. GET73 Prevents Ethanol-Induced Neurotoxicity in Primary Cultures of Rat Hippocampal Neurons. Alcohol Alcohol. 2016 Mar;51(2):128-35.
[2]. Ferraro L, et al. GET73 modulates rat hippocampal glutamate transmission: evidence for a functional interaction with mGluR5. Pharmacol Rep. 2011;63(6):1359-71. [3]. Loche A, et al. Anti-Alcohol and Anxiolytic Properties of a New Chemical Entity, GET73. Front Psychiatry. 2012 Feb 14;3:8. |
| Additional Infomation |
Get 73 has been studied for its potential use in treating alcohol dependence.
GET73 is a gamma-hydroxybutyric acid (GHB) analog and a negative allosteric modulator of mGluR5. It has anti-alcohol and anxiolytic properties and affects glutamate transmission in the hippocampus. It is used in research on alcohol use disorders and anxiety. |
| Molecular Formula |
C₁₃H₁₆F₃NO₂
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|---|---|
| Molecular Weight |
275.27
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| Exact Mass |
275.113
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| CAS # |
202402-01-5
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| PubChem CID |
10221200
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| Appearance |
White to off-white solid powder
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| LogP |
3.588
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
19
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| Complexity |
274
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1C=CC(=CC=1)CNC(CCCOC)=O)(F)F
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| InChi Key |
QLZOWJNFLXSDSH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16F3NO2/c1-19-8-2-3-12(18)17-9-10-4-6-11(7-5-10)13(14,15)16/h4-7H,2-3,8-9H2,1H3,(H,17,18)
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| Chemical Name |
4-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]butanamide
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| Synonyms |
GET-73; GET 73
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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 |
| 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 : ~100 mg/mL (~363.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.08 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 (9.08 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 (9.08 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 | 3.6328 mL | 18.1640 mL | 36.3280 mL | |
| 5 mM | 0.7266 mL | 3.6328 mL | 7.2656 mL | |
| 10 mM | 0.3633 mL | 1.8164 mL | 3.6328 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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