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'''FG-7142''' ('''ZK-31906''') is a drug which acts as a partial ] at the ] ] site of the ].<ref name="pmid17503486">{{cite journal |vauthors=Stevenson CW, Halliday DM, Marsden CA, Mason R |title=Systemic administration of the benzodiazepine receptor partial inverse agonist FG-7142 disrupts corticolimbic network interactions |journal=Synapse |volume=61 |issue=8 |pages=646–63 |year=2007 |pmid=17503486 |doi=10.1002/syn.20414|citeseerx=10.1.1.323.5370 }}</ref> It has ],<ref>{{cite journal | vauthors = Cottone P, Sabino V, Steardo L, Zorrilla EP | date = May 2007 | title = FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability | journal = Neuropsychopharmacology | volume = 32 | issue = 5| pages = 1069–81 | pmid = 17077811 | doi = 10.1038/sj.npp.1301229 | doi-access = free }}</ref> ] and pro-] effects.<ref>{{cite journal | vauthors = Evans AK, Lowry CA | date = Winter 2007 | title = Pharmacology of the β-carboline FG-7142, a partial inverse agonist at the benzodiazepine allosteric site of the GABA<sub>A</sub> receptor: neurochemical, neurophysiological, and behavioral effects | journal = CNS Drug Reviews | volume = 13 | issue = 4 | pages = 475–501 | pmid = 18078430 | doi = 10.1111/j.1527-3458.2007.00025.x | doi-access = free | pmc = 6494137 }}</ref> It also increases release of ] and ],<ref>{{cite journal | vauthors = Claustre Y, Rouquier L, Desvignes C, Leonetti M, Montégut J, Aubin N, Allouard N, Bougault I, Oury-Donat F, Steinberg R | year = 2006 | title = Effects of the vasopressin (V1b) receptor antagonist, SSR149415, and the corticotropin-releasing factor 1 receptor antagonist, SSR125543, on FG 7142-induced increase in acetylcholine and norepinephrine release in the rat | journal = Neuroscience | volume = 141 | issue = 3| pages = 1481–8 | pmid = 16781820 | doi = 10.1016/j.neuroscience.2006.05.006 }}</ref> and improves memory retention in animal studies.<ref>{{cite journal | vauthors = McNally GP, Augustyn KA, Richardson R | year = 2008 | title = GABA<sub>A</sub> receptors determine the temporal dynamics of memory retention | journal = Learning and Memory | volume = 15 | issue = 3 | pages = 106–11 | pmid = 18285469 | doi = 10.1101/lm.806008 | doi-access = free | pmc = 2275652 }}</ref> '''FG-7142''' ('''ZK-31906''') is a drug which acts as a partial ] at the ] ] site of the ].<ref name="pmid17503486">{{cite journal |vauthors=Stevenson CW, Halliday DM, Marsden CA, Mason R |title=Systemic administration of the benzodiazepine receptor partial inverse agonist FG-7142 disrupts corticolimbic network interactions |journal=Synapse |volume=61 |issue=8 |pages=646–63 |year=2007 |pmid=17503486 |doi=10.1002/syn.20414|citeseerx=10.1.1.323.5370 |s2cid=13415418 }}</ref> It has ],<ref>{{cite journal | vauthors = Cottone P, Sabino V, Steardo L, Zorrilla EP | date = May 2007 | title = FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability | journal = Neuropsychopharmacology | volume = 32 | issue = 5| pages = 1069–81 | pmid = 17077811 | doi = 10.1038/sj.npp.1301229 | doi-access = free }}</ref> ] and pro-] effects.<ref>{{cite journal | vauthors = Evans AK, Lowry CA | date = Winter 2007 | title = Pharmacology of the β-carboline FG-7142, a partial inverse agonist at the benzodiazepine allosteric site of the GABA<sub>A</sub> receptor: neurochemical, neurophysiological, and behavioral effects | journal = CNS Drug Reviews | volume = 13 | issue = 4 | pages = 475–501 | pmid = 18078430 | doi = 10.1111/j.1527-3458.2007.00025.x | doi-access = free | pmc = 6494137 }}</ref> It also increases release of ] and ],<ref>{{cite journal | vauthors = Claustre Y, Rouquier L, Desvignes C, Leonetti M, Montégut J, Aubin N, Allouard N, Bougault I, Oury-Donat F, Steinberg R | year = 2006 | title = Effects of the vasopressin (V1b) receptor antagonist, SSR149415, and the corticotropin-releasing factor 1 receptor antagonist, SSR125543, on FG 7142-induced increase in acetylcholine and norepinephrine release in the rat | journal = Neuroscience | volume = 141 | issue = 3| pages = 1481–8 | pmid = 16781820 | doi = 10.1016/j.neuroscience.2006.05.006 | s2cid = 24944657 }}</ref> and improves memory retention in animal studies.<ref>{{cite journal | vauthors = McNally GP, Augustyn KA, Richardson R | year = 2008 | title = GABA<sub>A</sub> receptors determine the temporal dynamics of memory retention | journal = Learning and Memory | volume = 15 | issue = 3 | pages = 106–11 | pmid = 18285469 | doi = 10.1101/lm.806008 | doi-access = free | pmc = 2275652 }}</ref>


==References== ==References==

Latest revision as of 07:53, 24 September 2021

FG-7142
Names
Preferred IUPAC name N-Methyl-5H-pyridoindole-2-carboxamide
Other names ZK-31906
Identifiers
CAS Number
3D model (JSmol)
ChemSpider
MeSH C526324
PubChem CID
UNII
CompTox Dashboard (EPA)
InChI
  • 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)Key: QMCOPDWHWYSJSA-UHFFFAOYSA-N
SMILES
  • CNC(=O)C1=NC=C2C(=C1)C3=CC=CC=C3N2
Properties
Chemical formula C13H11N3O
Molar mass 225.24594
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). ☒verify (what is  ?) Infobox references
Chemical compound

FG-7142 (ZK-31906) is a drug which acts as a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor. It has anorectic, anxiogenic and pro-convulsant effects. It also increases release of acetylcholine and noradrenaline, and improves memory retention in animal studies.

References

  1. Stevenson CW, Halliday DM, Marsden CA, Mason R (2007). "Systemic administration of the benzodiazepine receptor partial inverse agonist FG-7142 disrupts corticolimbic network interactions". Synapse. 61 (8): 646–63. CiteSeerX 10.1.1.323.5370. doi:10.1002/syn.20414. PMID 17503486. S2CID 13415418.
  2. Cottone P, Sabino V, Steardo L, Zorrilla EP (May 2007). "FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability". Neuropsychopharmacology. 32 (5): 1069–81. doi:10.1038/sj.npp.1301229. PMID 17077811.
  3. Evans AK, Lowry CA (Winter 2007). "Pharmacology of the β-carboline FG-7142, a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor: neurochemical, neurophysiological, and behavioral effects". CNS Drug Reviews. 13 (4): 475–501. doi:10.1111/j.1527-3458.2007.00025.x. PMC 6494137. PMID 18078430.
  4. Claustre Y, Rouquier L, Desvignes C, Leonetti M, Montégut J, Aubin N, Allouard N, Bougault I, Oury-Donat F, Steinberg R (2006). "Effects of the vasopressin (V1b) receptor antagonist, SSR149415, and the corticotropin-releasing factor 1 receptor antagonist, SSR125543, on FG 7142-induced increase in acetylcholine and norepinephrine release in the rat". Neuroscience. 141 (3): 1481–8. doi:10.1016/j.neuroscience.2006.05.006. PMID 16781820. S2CID 24944657.
  5. McNally GP, Augustyn KA, Richardson R (2008). "GABAA receptors determine the temporal dynamics of memory retention". Learning and Memory. 15 (3): 106–11. doi:10.1101/lm.806008. PMC 2275652. PMID 18285469.
GABA receptor modulators
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAATooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators
Convulsants
GABA receptor antagonists
GABA synthesis inhibitors
Glycine receptor antagonists
Glutamate receptor agonists
Convulsant barbiturates
Other


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