[HTML][HTML] Molecular targets for antiepileptic drug development

BS Meldrum, MA Rogawski - Neurotherapeutics, 2007 - Elsevier
This review considers how recent advances in the physiology of ion channels and other
potential molecular targets, in conjunction with new information on the genetics of idiopathic …

The betaine/GABA transporter and betaine: roles in brain, kidney, and liver

SA Kempson, Y Zhou, NC Danbolt - Frontiers in physiology, 2014 - frontiersin.org
The physiological roles of the betaine/GABA transporter (BGT1; slc6a12) are still being
debated. BGT1 is a member of the solute carrier family 6 (the neurotransmitter, sodium …

GABA: homeostatic and pharmacological aspects

A Schousboe, HS Waagepetersen - Progress in brain research, 2007 - Elsevier
The central nervous system (CNS) operates by a fine-tuned balance between excitatory and
inhibitory signalling. In this context, the inhibitory neurotransmission may be of particular …

[HTML][HTML] γ-Aminobutyric acid transporters as relevant biological target: Their function, structure, inhibitors and role in the therapy of different diseases

K Łątka, J Jończyk, M Bajda - International journal of biological …, 2020 - Elsevier
Abstract γ-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the nervous
system. It plays a crucial role in many physiological processes. Upon release from the …

Anticonvulsant active inhibitor of GABA transporter subtype 1, tiagabine, with activity in mouse models of anxiety, pain and depression

K Sałat, A Podkowa, P Kowalczyk, K Kulig… - Pharmacological …, 2015 - Elsevier
Background Tiagabine, a selective inhibitor of GABA transporter subtype 1 is used as an
add-on therapy of partial seizures in humans but its mechanism of action suggests other …

Müller glia as an active compartment modulating nervous activity in the vertebrate retina: neurotransmitters and trophic factors

RA de Melo Reis, ALM Ventura, CS Schitine… - Neurochemical …, 2008 - Springer
Müller cells represent the main type of glia present in the retina interacting with most, if not
all neurons in this tissue. Müller cells have been claimed to function as optic fibers in the …

Structural and molecular aspects of betaine-GABA transporter 1 (BGT1) and its relation to brain function

S Kickinger, E Hellsberg, B Frølund, A Schousboe… - …, 2019 - Elsevier
Abstract ɣ-aminobutyric-acid (GABA) functions as the principal inhibitory neurotransmitter in
the central nervous system. Imbalances in GABAergic neurotransmission are involved in the …

Astrocytic GABA transporters: pharmacological properties and targets for antiepileptic drugs

A Schousboe, P Wellendorph, B Frølund… - Glial Amino Acid …, 2017 - Springer
Inactivation of GABA-mediated neurotransmission is achieved by high-affinity transporters
located at both GABAergic neurons and the surrounding astrocytes. Early studies of the …

Structure-activity relationships of selective GABA uptake inhibitors

S Hog, JR Greenwood, KB Madsen… - Current topics in …, 2006 - ingentaconnect.com
For more than four decades there has been a search for selective inhibitors of GABA
transporters. This has led to potent and selective inhibitors of the cloned GABA transporter …

Cloning and characterization of a functional human γ-aminobutyric acid (GABA) transporter, human GAT-2

B Christiansen, AK Meinild, AA Jensen… - Journal of Biological …, 2007 - ASBMB
Plasma membrane γ-aminobutyric acid (GABA) transporters act to terminate GABA
neurotransmission in the mammalian brain. Intriguingly four distinct GABA transporters have …