Description
Cas:78538-74-6
Product Information:
FG-7142 is a benzodiazepine receptor ligand with anxiogenic and proconvulsant properties.
Chemical Formula: C13H11N3O
Exact Mass: 225.0902
Molecular Weight: 225.251
Elemental Analysis: C, 69.32; H, 4.92; N, 18.66; O, 7.10
Synonym:
FG-7142
FG 7142
FG7142
Chemical Name:
N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide
InChi Key:
QMCOPDWHWYSJSA-UHFFFAOYSA-N
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)
Smiles Code:
O=C(C1=CC2=C(C=N1)NC3=C2C=CC=C3)NC
Technical Data:
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
In Vitro:
FG-7142 has affinity for those expressing the α subunit, the Ki values are 91 nM; 330 nM; 492 nM and 2.150 μM for α1, α2,α3 and α5 subunits, respectively.
FG-7142 has a high efficacy in modulating GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50 = 137 nM) as compared to the other α subunits (EC50: α2= 507 nM,α3=1.021μM , α5=1.439 μM).
In Vivo:
FG-7142 (intraperitoneal injection; 15-30 mg/kg) activates mesolimbocortical dopaminergic projections, leading to increases in dopamine in the prefrontal cortex and the nucleus accumbens in rats.
FG-7142 (intraperitoneal injection; 15 mg/kg) increases tyrosine hydroxylase activity and dopamine turnover in the medial prefrontal cortex and ventral tegmentum in vivo, but effects are not detected in mesolimbic or nigrostriatal areas.
References:
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Horowski R. FG 7142: is this validated tool to study anxiety now forgotten? J Neural Transm (Vienna). 2020 Feb;127(2):287-289. doi: 10.1007/s00702-019-02136-3. Epub 2020 Jan 11. PMID: 31927622.
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Kurumaji A, Nishikawa T. An anxiogenic drug, FG 7142, induced an increase in mRNA of Btg2 and Adamts1 in the hippocampus of adult mice. Behav Brain Funct. 2012 Aug 22;8:43. doi: 10.1186/1744-9081-8-43. PMID: 22913326; PMCID: PMC3541064.
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Waters RP, See RE. Chronic cocaine self-administration attenuates the anxiogenic-like and stress potentiating effects of the benzodiazepine inverse agonist, FG 7142. Pharmacol Biochem Behav. 2011 Sep;99(3):408-13. doi: 10.1016/j.pbb.2011.05.021. Epub 2011 May 24. PMID: 21635914; PMCID: PMC3129491.
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Martire SI, Parkes SL, Westbrook RF. The effects of FG 7142 on sensory- specific satiety in rats. Behav Brain Res. 2010 May 1;209(1):131-6. doi: 10.1016/j.bbr.2010.01.034. Epub 2010 Jan 29. PMID: 20117147.
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Sink KS, Segovia KN, Sink J, Randall PA, Collins LE, Correa M, Markus EJ, Vemuri VK, Makriyannis A, Salamone JD. Potential anxiogenic effects of cannabinoid CB1 receptor antagonists/inverse agonists in rats: comparisons between AM4113, AM251, and the benzodiazepine inverse agonist FG-7142. Eur Neuropsychopharmacol. 2010 Feb;20(2):112-22. doi: 10.1016/j.euroneuro.2009.11.002. Epub 2009 Dec 16. PMID: 20015619; PMCID: PMC2817975.
Products are for research use only. Not for human use.
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