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]
^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.
PMID7996426.
^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.
PMID11103915.
S2CID33999227.
^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.
PMID12871032.
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]
^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.
PMID7996426.
^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.
PMID11103915.
S2CID33999227.
^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.
PMID12871032.