Effects of ethylenediamine – a putative GABA-releasing agent – on rat hippocampal slices and neocortical activity in vivo [PDF]
The simple diamine diaminoethane (ethylenediamine, EDA) has been shown to activate GABA receptors in the central and peripheral nervous systems, partly by a direct action and partly by releasing endogenous GABA.
Lui, C. +5 more
core +1 more source
GABAA receptors mediate fast inhibitory neurotransmission in the brain. Dysfunction of these receptors is associated with various psychiatric/neurological disorders and drugs targeting this receptor are widely used therapeutic agents.
Ping eWang +8 more
doaj +1 more source
Endoplasmic reticulum sorting and kinesin-1 command the targeting of axonal GABAB receptors. [PDF]
In neuronal cells the intracellular trafficking machinery controls the availability of neurotransmitter receptors at the plasma membrane, which is a critical determinant of synaptic strength.
Viviana Valdés +7 more
doaj +1 more source
GABA-Independent GABAA Receptor Openings Maintain Tonic Currents [PDF]
Activation of GABAA receptors (GABAARs) produces two forms of inhibition: ‘phasic’ inhibition generated by the rapid, transient activation of synaptic GABAARs by presynaptic GABA release, and tonic inhibition generated by the persistent activation of ...
Herd, Murray B +27 more
core +1 more source
The Mechanism of Enantioselective Neurosteroid Actions on GABAA Receptors
The neurosteroid allopregnanolone (ALLO) and pregnanolone (PREG), are equally effective positive allosteric modulators (PAMs) of GABAA receptors. Interestingly, the PAM effects of ALLO are strongly enantioselective, whereas those of PREG are not.
Hiroki Tateiwa +10 more
doaj +1 more source
Actions of Agonists, Fipronil and Ivermectin on the Predominant In Vivo Splice and Edit Variant (RDLbd, I/V) of the Drosophila GABA Receptor Expressed in Xenopus laevis Oocytes [PDF]
Ionotropic GABA receptors are the targets for several classes of insecticides. One of the most widely-studied insect GABA receptors is RDL (resistance to dieldrin), originally isolated from Drosophila melanogaster.
Philip Biggin +11 more
core +2 more sources
Synaptic GABA release prevents GABA transporter type-1 reversal during excessive network activity. [PDF]
GABA transporters control extracellular GABA, which regulates the key aspects of neuronal and network behaviour. A prevailing view is that modest neuronal depolarization results in GABA transporter type-1 (GAT-1) reversal causing non-vesicular GABA ...
Rusakov, Dmitri A. +9 more
core +1 more source
Post-synaptic GABAA receptors potentiate transmission by recruiting CaV2 channels to their inputs
Summary: We describe a retrograde synaptic signal at the C. elegans GABAergic neuromuscular junction. At this synapse, GABA release is controlled by two voltage-activated calcium channels (UNC-2/CaV2 and EGL-19/CaV1), and muscle responses are mediated by
Jian Zhao +3 more
doaj +1 more source
Investigating the Role of Loop C Hydrophilic Residue 'T244' in the Binding Site of ρ1 GABAC Receptors via Site Mutation and Partial Agonism. [PDF]
The loop C hydrophilic residue, threonine 244 lines the orthosteric binding site of ρ1 GABAC receptors was studied by point mutation into serine, alanine and cysteine, and tested with GABA, some representative partial agonists and antagonists. Thr244 has
Moawiah M Naffaa +5 more
doaj +1 more source
Anaesthetic impairment of immune function is mediated via GABA(A) receptors.
BackgroundGABA(A) receptors are members of the Cys-loop family of neurotransmitter receptors, proteins which are responsible for fast synaptic transmission, and are the site of action of wide range of drugs.
Daniel W Wheeler +15 more
doaj +1 more source

