gabaa α1  receptor

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

α5-GABAA receptor modulator 1 (Compound A-4) is a selective silent allosteric modulator (SAM) targeting the α5 subunit of GABAA receptors, useful for research into central nervous system (CNS) disorders.

GABAA receptor agonist 1 (compound 3e) is a potent agonist that binds to the GABA binding site of the GABAA receptor, producing GABAergic effects and exhibiting anti-depression activities in classical mouse models of FST and TST, indicating its potential in depression research [1].

Broflanilide is an insecticide-resistant GABA receptor antagonist for dieldrin. Its metabolite, Desmethyl-Broflanilide, can inhibit the RDL GABAR of the striped night moth, with an IC50 value of 1.3 nM.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

TPA-023B is an orally active and high-affinity agonist of the GABAA receptor α2/α3 subtype (Kis: 0.73 nM/2 nM) partial and an antagonist α1 subtype (Ki: 1.8 nM), has non-sedating anxiolytic-like properties.

MK-0343, also known as MRK-409, is a GABAA receptor subtype-selective partial agonist that exhibits non-sedating anxiolytic activity in preclinical species but induces sedation in humans, binding with high affinity to α1-, α2-, α3-, and α5-containing human recombinant GABA(A) receptors while demonstrating greater agonist efficacy at α3 relative to α1 subtypes, thereby providing mechanistic insight into subtype-specific modulation of inhibitory neurotransmission.

L-838417 is a GABAA receptor subtype-selective benzodiazepine site-selective ligand and GABAA receptor-positive modulator.L-838417 is a selective partial agonist of the α2, α3, and α5 subtypes and an antagonist of the α1 subtype and is used in the study of anxiety disorders.

NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) > α(3) > α(2) > α(1) at GABA(A) alpha subunit-containing receptors.

ZK93423 is a potent agonist of benzodiazepine receptor (IC50 = 1 nM) with non-selective between α1-, α2-, α3- and α5-subunit containing GABAA receptors, Ki values are 4.1, 4.2, 6 and 4.5 nM for inhibition of [3H]Ro15-1788 binding to human recombinant α1β3

MRK-898, an orally active modulator of the GABA(A) receptor, selectively interacts with the α1, α2, α3, and α5 subunits, displaying K i values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. It is noteworthy that the α1-containing receptors of GABA(A) are classified as "sedative," whereas receptors containing α2 and/or α3 are designated as "anxiolytic" subtype(s) [1].

Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep.