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
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)
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
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).
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.
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.
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.
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.
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.
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.
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