Chemical Name:(3a,5a)-3-Hydroxy-3-methyl-pregnan-20-one
Biological Activity:
Potent
positive allosteric modulator of GABAA receptors. Enhances
GABA-evoked chloride currents in Xenopus oocytes expressing GABAA
receptors (EC50 values are 94, 122 and 213 nM for α2β1γ2L, α3β1γ2L and α1β1γ2L receptors
respectively). Exerts anticonvulsive effects in a broad range of animal seizure
models.
Carteret al (1997) Characterization
of the anticonvulsive properties of ganaxolone (CCD 1044; 3α-hydroxy-3β-methyl-5α-pregnan-20-one), a selective, high
affinity, steroid modulator of the γ-aminobutyric acidA receptor.
J.Pharmacol.Exp.Ther. 280 1284. Lydenet al (2000)
Effect of ganaxolone in a rodent model of cerebral hematoma. Stroke 31
169. Ungardet al (2000) Modification of behavioral effects of
drugs in mice by neuroactive steroids. Psychopharmacology 148
336.
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.
