gaba receptor antagonist 1

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg L. This compound also exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg adult) and low toxicity to zebrafish (LC50: 42.4 mg L) [1].

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

Saclofen is a sulfonic analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50: 7.8 μM).1 This compound can be used to determine the functional roles for the GABAB receptor as

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg kg and prevents memory deficits induced by the AMPA kainate glutamate receptor antagonist NBQX at 0.1 mg kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine with potential to treat Alzheimer's disease, prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors, and is a potent GABA A receptor antagonist[1] [2] [3].

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].

NCS-382 (sodium) is a potent GABA receptor antagonist with anti-sedative and anti-hypnotic properties, used in neurological disease research [1].

CGP36216 hydrochloride acts as a selective antagonist at the presynaptic GABA receptor, specifically binding to the GABAB receptor with a Ki value of 0.3 μM. This compound is leveraged in research focused on anxiety and trauma-related disorders [1] [2].