scholarly journals Ethanol-induced GABAA receptor alpha4 subunit plasticity involves phosphorylation and neuroactive steroids

2016 ◽  
Vol 72 ◽  
pp. 1-8 ◽  
Author(s):  
David F. Werner ◽  
Patrizia Porcu ◽  
Kevin N. Boyd ◽  
Todd K. O'Buckley ◽  
Jenna M. Carter ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Neuroactive Steroids

Neuroactive steroids inhibit spinal reflex potentiation by selectively enhancing specific spinal GABAA receptor subtypes

Pain ◽  
2009 ◽  
Vol 143 (1) ◽  
pp. 12-20 ◽  
Author(s):  
Hsien-Yu Peng ◽  
Gin-Den Chen ◽  
Shin-Da Lee ◽  
Cheng-Yuan Lai ◽  
Chun-Hsien Chiu ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Neuroactive Steroids ◽  
Spinal Reflex ◽  
Receptor Subtypes ◽  
Gabaa Receptor Subtypes

Neuroactive Steroids Differ in Potency but Not in Intrinsic Efficacy at the GABAA Receptor in Vivo

2002 ◽  
Vol 303 (2) ◽  
pp. 616-626 ◽  
Author(s):  
S. A. G. Visser ◽  
W. W. F. T. Gladdines ◽  
P. H. van der Graaf ◽  
L. A. Peletier ◽  
M. Danhof
Keyword(s):  
Gabaa Receptor ◽  
Neuroactive Steroids ◽  
Intrinsic Efficacy

scholarly journals Social Isolation-Induced Decreases in Both the Abundance of Neuroactive Steroids and GABAA Receptor Function in Rat Brain

2002 ◽  
Vol 75 (2) ◽  
pp. 732-740 ◽  
Author(s):  
Mariangela Serra ◽  
Maria Giuseppina Pisu ◽  
Martino Littera ◽  
Giacomo Papi ◽  
Enrico Sanna ◽  
...  
Keyword(s):  
Rat Brain ◽  
Gabaa Receptor ◽  
Social Isolation ◽  
Neuroactive Steroids ◽  
Receptor Function

Subunit dependent modulation of GABAA receptor function by neuroactive steroids

1999 ◽  
Vol 819 (1-2) ◽  
pp. 75-82 ◽  
Author(s):  
Rajatavo Maitra ◽  
James N Reynolds
Keyword(s):  
Gabaa Receptor ◽  
Neuroactive Steroids ◽  
Receptor Function

The neuroactive steroid allopregnanolone suppresses hypothalamic gonadotropin-releasing hormone release through a mechanism mediated by the gamma-aminobutyric acidA receptor

1998 ◽  
Vol 158 (1) ◽  
pp. 121-125 ◽  
Author(s):  
AE Calogero ◽  
MA Palumbo ◽  
AM Bosboom ◽  
N Burrello ◽  
E Ferrara ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Gonadotropin Releasing Hormone ◽  
Neuroactive Steroids ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Hpg Axis ◽  
Releasing Hormone ◽  
Brain Functions ◽  
Gnrh Release

The central nervous system (CNS) is able to synthesize and/or metabolize steroid hormones. These neuroactive steroids are capable of modulating several brain functions and, among these, they seem to regulate the hypothalamic-pituitary-gonadal (HPG) axis. Indeed, recent observations have shown that 5 alpha-pregnane-3 alpha-ol-20-one (allopregnanolone), one of the most abundant naturally occurring neuroactive steroids, suppresses ovulation and sexual behaviour when administered within the CNS. The present study was undertaken to evaluate the effects of allopregnanolone and its inactive stereoisomer, 5 alpha-pregnane-3 beta-ol-20-one, upon the release of gonadotropin-releasing hormone (GnRH) from individually-incubated hemihypothalami. Allopregnanolone suppressed GnRH release in a concentration-dependent manner with maximal activity in the nanomolar range, a range at which this neurosteroid is capable of playing a biological action. The specificity of allopregnanolone suppression of GnRH release was provided by the lack of effect of its known inactive stereoisomer. To evaluate the involvement of gamma-aminobutyric acidA (GABAA) receptor, we examined the effects of two neurosteroids with GABA-antagonistic properties, pregnanolone sulfate (PREG-S) and dehydroepiandrosterone sulfate (DHEAS), and of bicuculline, a selective antagonist of the GABA binding site on the GABAA receptor, on allopregnanolone (10 nM)-suppressed GnRH release. Both PREG-S and bicuculline overcame the inhibitory effects of allopregnanolone on GnRH release, whereas DHEAS did not. To substantiate the involvement of the GABAA receptor further, we tested the effects of muscimol, a selective agonist for this receptor, which suppressed GnRH release. In conclusion, allopregnanolone suppressed hypothalamic GnRH release in vitro and this effect appeared to be mediated by an interaction with the GABAA receptor. We speculate that the inhibitory effect of allopregnanolone on the HPG axis may also be caused by its ability to suppress hypothalamic GnRH release.

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