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]
^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.
^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. PMC1917729. PMID 1963808.
^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.
^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.
^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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8205, imidazobenzodiazepine, derivative, related, bretazenil, which, acts, partial, agonist, gabaa, receptors, with, slight, selectivity, containing, subtype, animal, tests, anxiolytic, anticonvulsant, effects, with, little, sedation, ataxia, produced, identif. 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 a1 containing subtype In animal tests it has anxiolytic and anticonvulsant effects but with little sedation or ataxia produced 2 3 4 5 FG 8205IdentifiersIUPAC name 7 chloro 5 methyl 3 5 propan 2 yl 1 2 4 oxadiazol 3 yl 4H imidazo 1 5 a 1 4 benzodiazepin 6 oneCAS Number122384 14 9 YPubChem CID129710ChemSpider114837 YUNII7V0I080855ChEMBLChEMBL307202 YCompTox Dashboard EPA DTXSID40153589Chemical and physical dataFormulaC 17H 16Cl N 5O 2Molar mass357 80 g mol 13D model JSmol Interactive imageSMILES Clc4cccc3n2cnc c1nc on1 C C C c2CN C O c34 CInChI 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 YKey SEWXZWMBVGJJPG UHFFFAOYSA N Y N Y what is this verify See also EditBenzodiazepineReferences Edit 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 Tricklebank MD Honore 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 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 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 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 This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title FG 8205 amp oldid 1120043607, wikipedia, wiki, book, books, library,
