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  • GABA Receptor
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Results for "

gabaa α5

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    16
    TargetMol | Inhibitors_Agonists
  • Isotope Products
    1
    TargetMol | Isotope_Products
L-822179
L822179, L-822,179, L822,179, L 822179, L 822,179
T24381215874-86-5
L-822179 (α5IA) is a selective inverse agonist for the Α5 subtype of GABAA receptor with higher intrinsic activity at the A5 subtype than other drugs.
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6-8 weeks
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α5-GABAA receptor modulator 1
T205217
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.
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DMCM hydrochloride
T110611215833-62-7In house
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.
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6-8 weeks
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NS11394
NS 11394
T2067951650-22-9
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.
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L-838417 D9
C-21191, CTP-354, CTP354
T223011213669-91-0
L-838417 D9 (C-21191) is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].
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CL 218872
T857266548-69-4
CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxi
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MRK-016
MRK016
T12105342652-67-9
MRK-016 is a selective GABAA α5 receptor inverse agonist negative allosteric modulator, (IC50=3 nM) with the advantages of being orally available and penetrating the blood-brain barrier.MRK-016 increases long time period potentiation (LTP) in mouse hippocampal slices, with memory-improvement, antidepressant, and pain-treating effects.
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7-10 days
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MK-0343
MRK-409
T16084233275-76-8
MK0343 is an orally bioavailable GABAA receptor subtype-selective partial agonist and is a non-sedating anxiolytic.
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6-8 weeks
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RO 4938581
T16794883093-10-5
RO 4938581 is an effective and selective agonist of GABAA α5 inverse (Ki: 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively)).
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6-8 weeks
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L-838417
L838417, L 838417
T19702286456-42-6
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.
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6-8 weeks
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ZK93423
ZK-93423,ZK 93423
T2922883910-44-5
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
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6-8 weeks
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Afizagabar
T373881398496-82-6
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. It enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy [1].
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8-10 weeks
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GABAA receptor modulator-2
T628852413850-54-9
GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM) that exhibits high metabolic stability and a good central nervous system safety profile.
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6-8 weeks
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Basmisanil
RG1662, RO5186582
T71651159600-41-5
Basmisanil (RG1662) is a negative allosteric modulator inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.
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mrk-898
T86930461450-30-6
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].
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10-14 weeks
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ONO-8590580
CS-2894
TQ00401802661-73-9
ONO-8590580 (CS-2894) is a negative allosteric modulator of GABAA α5.
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