FG-7142 (ZK-31906) is a drug which acts as a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor.[1] It has anorectic,[2] anxiogenic and pro-convulsant effects.[3] It also increases release of acetylcholine and noradrenaline,[4] and improves memory retention in animal studies.[5]

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.