rat gabaa

Pivagabine (CXB-722), a hydrophobic 4-aminobutyric acid derivative, exhibits neuromodulatory activity and successfully penetrates the blood-brain barrier in rats. It counteracts the impact of foot shock on GABAA receptor function and corticotropin-releasing factor (CRF) levels in the rat brain.

Isoguvacine hydrochloride (1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride) is a GABA receptor agonist. Isoguvacine hydrochloride binds to rat synaptic cortical membranes and activates α1β2γ2S, α2β2γ2S, α3β2γ2S, α5β2γ2S, and ρ1 subunit GABAA receptors.

Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.

MK0343 is an orally bioavailable GABAA receptor subtype-selective partial agonist and is a non-sedating anxiolytic.

(+)-Bicuculline methiodide is a γ-aminobutyric acid type A (GABAA) receptor blocker that crosses the rat blood-brain barrier (BBB) and blocks epileptogens, which can be used to study neurological disorders such as epilepsy. (+)-Bicuculline methiodide reduces liver injury in septic rats.

KRM-II-81 is a γ‑Aminobutyric Acid Type A (GABAA) Receptor Ligand. KRM-II-81 exhibits improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.

Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC50 of 8.6 nM for human recombinant GABA B receptors. It has an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, determined by displacement of [3H]GABA binding in brain membranes. Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

GABAA receptor agent 2 TFA is a potent, high-affinity GABAA receptor antagonist with an IC50 of 24 nM [human α1β2γ2GABAA-expressing tsA201 cells] and a Ki of 28 nM [rat GABAA receptor]. GABAA receptor agent 2 TFA has no effect on four human GABA transport proteins [hGAT-1, hBGT-1, hGAT-2, and hGAT-3].

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA B receptor agonist with an EC 50 of 8.6 nM for human recombinant GABA B receptor. The affinity ( K i s) of Lesogaberan hydrochloride for rat GABA B and GABA A receptors, as measured by displacement of GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.