Chemical Name:N,N-Dihexyl-2-(4-fluorophenyl)indole-3-acetamide
Biological Activity:
Binds specifically and with high
affinity to the peptide DBI receptor (benzodiazepine receptor) on mitochondrial
membranes, inducing production of neurosteroids, which modulate GABA receptors
(EC50 = 3 nM for increase in production of pregnenolone in glial
cells). Thus it reduces anxiety without causing sedation.
Romeoet al (1992) 2-Aryl-3-indoleacetamides (FGIN-1): a new
class of potent and specific ligands for the mitochondrial DBI receptor (MDR).
J.Pharmacol.Exp.Ther. 262 971. Kozikowski et al
(1992) Synthesis of (2-arylindol-3-yl)acetamides as probes for mitochondrial
steroidogenesis - a new mechanism of GABAB receptor modulation.
Angew.Chem.Int.Ed.31 1060.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.
