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Loreclezole hydrochloride
Chemical Name:(Z)-1-[2-Chloro-2-(2,4-dichlorophenyl)ethenyl]-1H-1,2,4
-triazole hydrochloride
Biological Activity:
Subtype selective GABAA
receptor modulator. Acts as a positive allosteric modulator of β2
or β3-subunit containing receptors. Also acts as a negative modulator at a
novel regulatory site, enhancing GABAA receptor sensitisation.
Inhibits homomeric r1 GABAC
receptors.
Donnelly and Macdonald (1996) Loreclezole enhances apparent desensitisation of recombinant
GABAA receptor currents. Neuropharmacology 35 1233. Fisheret al (2000) Loreclezole inhibition of recombinant α1β1γ2L GABAA
receptor single channel currents. Neuropharmacology 39 235. Thometet al (2000) Loreclezole as a simple functional marker for homomeric rtype GABAC receptors.
Eur.J.Pharmacol. 408 R1. Smithet al (2004)
Compounds exhibiting selective efficacy for different β subunits of human
recombinant γ-aminobutyric acidA receptors. J.Pharmacol.Exp.Ther. 311
601.
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.