Related Experiment Video
Updated: Feb 20, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
GABAB receptor modulation-to B or not to be B a pro-cognitive medicine?
Jordi Serrats1, Mark Oliver Cunningham2, Ceri Hywel Davies3
1CNS Drug Discovery Unit, Takeda Pharmaceuticals Limited, Takeda California, 10275 Science Center Drive, San Diego, CA 92121, USA.
Abstract:
Metabotropic GABAB receptors clearly modify cognitive performance in preclinical animal models, yet translation to treating human disease has been elusive. Compared to their ionotropic GABAA receptor counterpart GABAB receptors not only regulate postsynaptic excitability but also regulate diverse synaptic inputs by presynaptically inhibiting neurotransmitter release. As such, the choice of agonist, antagonist, -ve or +ve modulator as well as CNS exposure level, timing of delivery and longevity of action strongly influence the probability of unlocking the procognitive potential of GABAB receptors in human disease. Quantitative clinical analysis of target/mechanistic engagement of GABAB receptors within cognitive circuits at the level of distinct pre-synaptic and post-synaptic subpopulations is required to determine the optimal pharmacological/dosing profile for different cognitive disorders.
More Related Videos
07:51Inhibitory Synapse Formation in a Co-culture Model Incorporating GABAergic Medium Spiny Neurons and HEK293 Cells Stably Expressing GABAA Receptors
Published on: November 14, 2014
07:01Electrophoretic Delivery of γ-aminobutyric Acid GABA into Epileptic Focus Prevents Seizures in Mice
Published on: May 16, 2019
Related Concept Videos
Antiepileptic Drugs: GABAergic Pathway Potentiators
The key GABA pathway potentiators used in epilepsy management are as follows.
Benzodiazepines are a well-known class of drugs used for...
Ligand-Gated Ion Channel Receptor: Gating Mechanism
Cognitive Enhancers: Cholinesterase Inhibitors and NMDA Receptor Antagonists
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Antiepileptic Drugs: Potassium Channel Activators
Ezogabine has gained approval as an adjunctive treatment...
Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...