Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor [PDF]
In the 1980s particular endogenous metabolites of progesterone and of deoxycorticosterone were revealed to be potent, efficacious, positive allosteric modulators (PAMs) of the GABAA receptor (GABAAR).
Belelli, Delia +3 more
core +1 more source
Neurosteroids as regulators of neuroinflammation.
Neuroinflammation is a physiological protective response in the context of infection and injury. However, neuroinflammation, especially if chronic, may also drive neurodegeneration. Neurodegenerative diseases, such as multiple sclerosis (MS), Alzheimer's
Canelif Yilmaz +6 more
semanticscholar +1 more source
Temporal changes in the expression of the translocator protein TSPO and the steroidogenic enzyme 5a-reductase in the dorsal spinal cord of animals with neuropathic pain: effects of progesterone administration [PDF]
Neuropathic pain is a frequent complication of spinal cord injury (SCI), still refractory to conventional treatment. The presence and biological activity of steroidogenic regulatory proteins and enzymes in the spinal cord suggests that neurosteroids ...
Adler, Natalia Sol +6 more
core +2 more sources
Block of NMDA receptor channels by endogenous neurosteroids: implications for the agonist induced conformational states of the channel vestibule [PDF]
N-methyl-D-aspartate receptors (NMDARs) mediate synaptic plasticity, and their dysfunction is implicated in multiple brain disorders. NMDARs can be allosterically modulated by numerous compounds, including endogenous neurosteroid pregnanolone sulfate ...
A Malayev +61 more
core +1 more source
Site-specific effects of neurosteroids on GABAA receptor activation and desensitization
This study examines how site-specific binding to the three identified neurosteroid binding sites in the α1β3 GABAA receptor (GABAAR) contributes to neurosteroid allosteric modulation. We found that the potentiating neurosteroid, allopregnanolone, but not
Yusuke Sugasawa +12 more
semanticscholar +1 more source
Neurosteroids and epilepsy [PDF]
Neurosteroids are a family of compounds synthesized directly in the brain by transforming cholesterol into pregnenolone, which is then converted to compounds such as allopregnanolone and allotetrahydrodeoxycorticosterone. In view of their ability to modulate neurotransmission, neurosteroids may influence the clinical course of epileptic disorders.
Giuseppe Biagini +2 more
openaire +4 more sources
Role of Hormones and Neurosteroids in Epileptogenesis
This article describes the emerging evidence of hormonal influence on epileptogenesis, which is a process whereby a brain becomes progressively epileptic due to an initial precipitating event of diverse origin such as brain injury, stroke, infection, or ...
D Samba eReddy
doaj +1 more source
Midazolam inhibits hippocampal long-term potentiation and learning through dual central and peripheral benzodiazepine receptor activation and neurosteroidogenesis [PDF]
Benzodiazepines (BDZs) enhance GABA(A) receptor inhibition by direct actions on central BDZ receptors (CBRs). Although some BDZs also bind mitochondrial receptors [translocator protein (18 kDa) (TSPO)] and promote the synthesis of GABA-enhancing ...
Izumi, Yukitoshi +3 more
core +2 more sources
Treatment of Postpartum Depression with Neurosteroids
Neurosteroids, such as allopregnanolone, are primarily synthesized substances in the central nervous system which influence processes occurring in the brain.
Reda Stankevičiūtė, Robertas Strumila
doaj +3 more sources
Neurosteroids and GABAA receptor interactions: a focus on stress
Since the pioneering discovery of the rapid CNS depressant actions of steroids by the father of stress, Hans Seyle 70 years ago, brain-derived neurosteroids have emerged as powerful endogenous modulators of neuronal excitability.
Benjamin George Gunn +3 more
doaj +1 more source

