Relating neurosteroid modulation of inhibitory neurotransmission to behaviour

2021 ◽  
Author(s):  
Delia Belelli ◽  
Grant D. Phillips ◽  
John R. Atack ◽  
Jeremy J. Lambert
Keyword(s):  
Inhibitory Neurotransmission

Artemisinins and their impact on inhibitory neurotransmission

2021 ◽  
Vol 59 ◽  
pp. 19-25
Author(s):  
Anabel Pacios-Michelena ◽  
Vikram Babu Kasaragod ◽  
Hermann Schindelin
Keyword(s):  
Inhibitory Neurotransmission

scholarly journals Author Correction: Inhibitory neurotransmission drives endocannabinoid degradation to promote memory consolidation

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Christophe J. Dubois ◽  
Jessica Fawcett-Patel ◽  
Paul A. Katzman ◽  
Siqiong June Liu
Keyword(s):  
Memory Consolidation ◽  
Inhibitory Neurotransmission

A Correction to this paper has been published: https://doi.org/10.1038/s41467-021-21329-7.

scholarly journals The phytocannabinoid Δ9 -tetrahydrocannabivarin modulates inhibitory neurotransmission in the cerebellum

2008 ◽  
Vol 154 (1) ◽  
pp. 204-215 ◽  
Author(s):  
Y-L Ma ◽  
S E Weston ◽  
B J Whalley ◽  
G J Stephens
Keyword(s):  
Inhibitory Neurotransmission

Identification of Positive Allosteric Modulators of Glycine Receptors from a High-Throughput Screen Using a Fluorescent Membrane Potential Assay

2016 ◽  
Vol 21 (10) ◽  
pp. 1042-1053 ◽  
Author(s):  
Clara Stead ◽  
Adam Brown ◽  
Cathryn Adams ◽  
Sarah J. Nickolls ◽  
Gareth Young ◽  
...  
Keyword(s):  
Membrane Potential ◽  
High Throughput ◽  
Glycine Receptor ◽  
Functional Characterization ◽  
In Vitro Assays ◽  
Allosteric Modulators ◽  
Inhibitory Neurotransmission ◽  
Starting Point ◽  
Positive Allosteric Modulators

Glycine receptor 3 (GlyRα3) is a ligand-gated ion channel of the cys-loop family that plays a key role in mediating inhibitory neurotransmission and regulation of pain signaling in the dorsal horn. Potentiation of GlyRα3 function is therefore of interest as a putative analgesic mechanism with which to target new therapeutics. However, to date, positive allosteric modulators (PAMs) of this receptor with sufficient selectivity to enable target validation studies have not been described. To address this lack of pharmacological tools, we developed a suite of in vitro assays comprising a high-throughput fluorescent membrane potential screen and a medium-throughput electrophysiology assay using IonFlux HT together with conventional manual patch clamp. Using these assays, we conducted a primary screening campaign and report the structures of hit compounds identified as GlyR PAMs. Our functional characterization data reveal a hit compound with high efficacy relative to current known potentiators and selectivity over GABAAR, another major class of inhibitory neurotransmission receptors of importance to pain. These small-molecule GlyR PAMs have high potential both as early tool compounds to enable pharmacological studies of GlyR inhibitory neurotransmission and as a starting point for the development of potent, selective GlyRα3 PAMs as novel analgesics.

Opioid agonists modulate excitatory and inhibitory neurotransmission in human colon

2008 ◽  
Vol 5 (4) ◽  
pp. 289-297 ◽  
Author(s):  
F. ANGEL ◽  
P. CHAMOUARD ◽  
A. KLEIN ◽  
E. MARTIN
Keyword(s):  
Human Colon ◽  
Inhibitory Neurotransmission ◽  
Opioid Agonists

scholarly journals Overexpression of wild-type human amyloid precursor protein alters GABAergic transmission

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Anna Kreis ◽  
Jana Desloovere ◽  
Nuria Suelves ◽  
Nathalie Pierrot ◽  
Xavier Yerna ◽  
...  
Keyword(s):  
Amyloid Precursor Protein ◽  
Neuronal Loss ◽  
Gaba Release ◽  
Long Term Potentiation ◽  
Precursor Protein ◽  
Wild Type ◽  
Inhibitory Neurotransmission ◽  
Gaba Production ◽  
Synaptic Functions ◽  
Term Potentiation

AbstractThe function of the amyloid precursor protein (APP) is not fully understood, but its cleavage product amyloid beta (Aβ) together with neurofibrillary tangles constitute the hallmarks of Alzheimer’s disease (AD). Yet, imbalance of excitatory and inhibitory neurotransmission accompanied by loss of synaptic functions, has been reported much earlier and independent of any detectable pathological markers. Recently, soluble APP fragments have been shown to bind to presynaptic GABAB receptors (GABABRs), subsequently decreasing the probability of neurotransmitter release. In this body of work, we were able to show that overexpression of wild-type human APP in mice (hAPPwt) causes early cognitive impairment, neuronal loss, and electrophysiological abnormalities in the absence of amyloid plaques and at very low levels of Aβ. hAPPwt mice exhibited neuronal overexcitation that was evident in EEG and increased long-term potentiation (LTP). Overexpression of hAPPwt did not alter GABAergic/glutamatergic receptor components or GABA production ability. Nonetheless, we detected a decrease of GABA but not glutamate that could be linked to soluble APP fragments, acting on presynaptic GABABRs and subsequently reducing GABA release. By using a specific presynaptic GABABR antagonist, we were able to rescue hyperexcitation in hAPPwt animals. Our results provide evidence that APP plays a crucial role in regulating inhibitory neurotransmission.

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