FG-8205

FG-8205[1] (L-663,581) is an imidazobenzodiazepine derivative related to bretazenil, which acts as a partial agonist at GABAA receptors, with slight selectivity for the α1-containing subtype. In animal tests it has anxiolytic and anticonvulsant effects but with little sedation or ataxia produced.[2][3][4][5]

FG-8205
Identifiers
  • 7-chloro-5-methyl-3-(5-propan-2-yl-1,2,4-oxadiazol-3-yl)-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H16ClN5O2
Molar mass357.80 g·mol−1
3D model (JSmol)
  • Clc4cccc3n2cnc(c1nc(on1)C(C)C)c2CN(C(=O)c34)C
  • InChI=1S/C17H16ClN5O2/c1-9(2)16-20-15(21-25-16)14-12-7-22(3)17(24)13-10(18)5-4-6-11(13)23(12)8-19-14/h4-6,8-9H,7H2,1-3H3 checkY
  • Key:SEWXZWMBVGJJPG-UHFFFAOYSA-N checkY
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See also

References
  1. Watjen F, Baker R, Engelstoff M, Herbert R, MacLeod A, Knight A, Merchant K, Moseley J, Saunders J, Swain CJ (October 1989). "Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines". J. Med. Chem. 32 (10): 2282–91. doi:10.1021/jm00130a010. PMID 2552115.
  2. Tricklebank MD, Honoré T, Iversen SD, Kemp JA, Knight AR, Marshall GR, Rupniak NM, Singh L, Tye S, Watjen F (November 1990). "The pharmacological properties of the imidazobenzodiazepine, FG 8205, a novel partial agonist at the benzodiazepine receptor". Br. J. Pharmacol. 101 (3): 753–61. doi:10.1111/j.1476-5381.1990.tb14152.x. PMC 1917729. PMID 1963808.
  3. Lin JH, Chen IW, Lin TH (December 1994). "Blood–brain barrier permeability and in vivo activity of partial agonists of benzodiazepine receptor: a study of L-663,581 and its metabolites in rats". J. Pharmacol. Exp. Ther. 271 (3): 1197–202. PMID 7996426.
  4. Guscott MR, Cook GP, Bristow LJ (September 2000). "Contextual fear conditioning and baseline startle responses in the rat fear-potentiated startle test: a comparison of benzodiazepine/gamma-aminobutyric acid-A receptor agonists". Behav Pharmacol. 11 (6): 495–504. doi:10.1097/00008877-200009000-00006. PMID 11103915. S2CID 33999227.
  5. Atack JR (August 2003). "Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site". Curr Drug Targets CNS Neurol Disord. 2 (4): 213–32. doi:10.2174/1568007033482841. PMID 12871032.
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