European Journal of Pharmacology: Molecular Pharmacology
The neuroactive steroid 3α-hydroxy-5β-pregnan-20-one is a two-component modulator of ligand binding to the GABAA receptor
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Cited by (61)
Mechanisms of neurosteroid interactions with GABA<inf>A</inf> receptors
2007, Pharmacology and TherapeuticsCitation Excerpt :The latter effect was proposed to result from channel block due to steroid binding to yet another site, distinct from those involved in potentiation or the type of inhibition produced by pregnenolone sulfate. Also, Morrow et al. (1990) found that the potentiation curves of muscimol-stimulated chloride uptake into rat brain synaptosomes were biphasic for many steroids suggesting that steroid interactions with multiple binding sites underlie their effects on the receptor, and others have found biphasic effects of 5β-reduced potentiating steroids on TBPS binding (Hawkinson et al., 1994). However, the caveat to these findings is that several subtypes of GABAA receptors, each with their own distinct pharmacological properties, could exist in the synaptoneurosome preparation used.
Attack behaviors in mice: From factorial structure to quantitative trait loci mapping
2005, European Journal of PharmacologyHigh affinity, heterogeneous displacement of [<sup>3</sup>H]EBOB binding to cerebellar GABA<inf>A</inf> receptors by neurosteroids and GABA agonists
2005, NeuropharmacologyCitation Excerpt :The minor high affinity component could be fitted only for the pooled experiments with IC50 values of about 4 nM (Table 2). Interestingly, displacement of cerebellar [3H]EBOB binding by allopregnanolone did not display this kind of heterogeneity (Fodor et al., 2005) such as that of [35S]TBPS binding (e.g. Hawkinson et al., 1994b). Displacement of [3H]EBOB binding was also studied by GABA agonists and neurosteroids in combination.
Nanomolar allopregnanolone potentiates rat cerebellar GABA<inf>A</inf> receptors
2005, Neuroscience Letters
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Present address: Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, 1985 Zonal Ave., Los Angeles, CA 90033, USA.