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| Targets |
FG 7142 targets the GABAA receptor, specifically the benzodiazepine binding site on GABAA receptors containing the α1 subunit. It acts as an inverse agonist, meaning it reduces the effect of GABA at the receptor, leading to decreased chloride influx and neuronal inhibition. It has a Ki of 91 nM for the α1 subunit-containing GABAA receptor and modulates GABA-induced chloride flux with an EC50 of 137 nM. The compound also affects tyrosine hydroxylase and β-adrenoceptors.
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| ln Vitro |
FG-7142 exhibits affinity for α subunit expression, with a Ki value of 91 nM; 330 nm; α1, α2, α3, and α5 subunits, respectively, being 492 nM and 2.150 μM[1]. When it comes to controlling GABA-induced chloride flux at GABAA receptors that express the α1 subunit energy (EC50 = 137 nM) micron), FG-7142 is much more effective than other α subunits (EC50: α2=507 nM, α3=1.021μM, and α5=1.439) [1].
In vitro studies have demonstrated that FG 7142 is a non-selective benzodiazepine inverse agonist with high affinity for the α1 subunit-containing GABAA receptor (Ki = 91 nM). It modulates GABA-induced chloride flux on GABAA receptors expressing the α1 subunit with an EC50 of 137 nM. The compound increases tyrosine hydroxylation and causes upregulation of β-adrenoceptors in the mouse cerebral cortex. It has anxiogenic and proconvulsant properties. |
| ln Vivo |
In rats, FG-7142 (ip; 15–30 mg/kg) increases dopamine in the nucleus accumbens and prefrontal cortex by activating mesolimbic cortical dopaminergic projections [1]. In vivo, FG-7142 (ip; 15 mg/kg) raises dopamine turnover and tyrosine hydroxylase activity in the ventral tegmentum and medial prefrontal cortex, but not in the mesolimbic or nigrostriatal regions [1].
In vivo studies have shown that FG 7142 (intraperitoneal injection; 15 mg/kg) increases tyrosine hydroxylase activity and dopamine turnover in the medial prefrontal cortex and ventral tegmentum, but effects are not detected in mesolimbic or nigrostriatal areas. It causes upregulation of β-adrenoceptors in the mouse cerebral cortex. The compound has anxiogenic and proconvulsant properties. It is used as a research tool for studying anxiety, GABAA receptor function, and the benzodiazepine binding site. |
| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for FG 7142 typically involve radioligand binding studies using membrane preparations from cells expressing recombinant GABAA receptors or from brain tissue. The receptor is incubated with increasing concentrations of FG 7142 (0.01 nM - 10 μM) and a fixed concentration of a radiolabeled benzodiazepine ligand (e.g., ³H-flunitrazepam or ³H-diazepam) in binding buffer at 4°C for 1-2 hours. Bound and free radioligand are separated by rapid filtration through glass fiber filters. Radioactivity is measured by liquid scintillation counting. IC50 values are calculated from dose-response curves by nonlinear regression, and Ki values are derived using the Cheng-Prusoff equation.
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| Cell Assay |
For in vitro cell-based assays, cells expressing recombinant GABAA receptors (e.g., α1β2γ2 subunit combination) are cultured in appropriate media. Cells are treated with FG 7142 at concentrations ranging from 0.01-10 μM for 1-24 hours. Receptor modulation is assessed by measuring chloride flux using fluorescent chloride-sensitive dyes (e.g., MQAE) or by patch-clamp electrophysiology. Cells are typically co-treated with GABA to assess the compound's inverse agonist effects. Cell viability is assessed by MTT or CCK-8 assays. The compound's effects on downstream signaling can be assessed by measuring changes in gene expression.
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| Animal Protocol |
In vivo animal studies with FG 7142 typically use mouse or rat models to study anxiety, seizure susceptibility, and GABAA receptor function. The compound is administered intraperitoneally at doses such as 15 mg/kg. Anxiogenic effects are assessed in behavioral tests such as the elevated plus maze, open field test, or light-dark box. Proconvulsant effects are assessed by measuring seizure thresholds. Tyrosine hydroxylase activity and dopamine turnover are measured in brain regions. β-adrenoceptor levels are measured by radioligand binding. Brain tissues are collected for neurochemical analysis.
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| ADME/Pharmacokinetics |
FG 7142 has a molecular weight of 225.25 g/mol and molecular formula C13H11N3O. Chemical name: N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide. The compound is soluble in DMSO. Storage recommendations: dry, dark place. Pharmacokinetic properties include rapid brain penetration following intraperitoneal administration. The compound is used as a research tool for studying the benzodiazepine binding site and GABAA receptor function.
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| Toxicity/Toxicokinetics |
In preclinical studies, FG 7142 has shown anxiogenic and proconvulsant properties, which are expected pharmacological effects of benzodiazepine inverse agonists. The compound is used as a research tool and is not intended for human therapeutic use. At research doses, the compound is well-tolerated in animal models with appropriate monitoring. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide is a member of the β-carboline class of compounds.
FG 7142 (also known as ZK 39106 or LSU-65) is a non-selective benzodiazepine inverse agonist. It has high affinity for the α1 subunit-containing GABAA receptor with a Ki of 91 nM. FG 7142 modulates GABA-induced chloride flux on GABAA receptors expressing the α1 subunit with an EC50 of 137 nM. It increases tyrosine hydroxylation and causes upregulation of β-adrenoceptors in the mouse cerebral cortex. The compound has anxiogenic and proconvulsant properties. FG 7142 is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C13H11N3O
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| Molecular Weight |
225.24594
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| Exact Mass |
225.09
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| Elemental Analysis |
C, 69.32; H, 4.92; N, 18.66; O, 7.10
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| CAS # |
78538-74-6
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| PubChem CID |
4375
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.328g/cm3
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| Boiling Point |
576.3ºC at 760 mmHg
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| Flash Point |
302.3ºC
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| Index of Refraction |
1.735
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| LogP |
2.466
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC(=O)C1=NC=C2C(=C1)C3=CC=CC=C3N2
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| InChi Key |
QMCOPDWHWYSJSA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H11N3O/c1-14-13(17)11-6-9-8-4-2-3-5-10(8)16-12(9)7-15-11/h2-7,16H,1H3,(H,14,17)
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| Chemical Name |
N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide
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| Synonyms |
FG-7142 FG 7142 FG7142
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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 (~443.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.10 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 (11.10 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 (11.10 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 | 4.4395 mL | 22.1976 mL | 44.3951 mL | |
| 5 mM | 0.8879 mL | 4.4395 mL | 8.8790 mL | |
| 10 mM | 0.4440 mL | 2.2198 mL | 4.4395 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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