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GABA Receptors
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NCS-382
NCS-382 is a γ-Hydroxybutyric acid antagonist, anticonvulsant. Learn MoreStarting at: $80.00
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U 90042
U 90042 is a GABAA receptor ligand that binds with comparable affinities to three receptor subtypes: α1β2γ2, α3β2γ2 and α6β2γ2 (Ki values are 7.8, 9.5 and 11.0 nM respectively). Learn MoreStarting at: $115.00
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CGP 52432
CGP 52432 is a potent, selective GABAB receptor antagonist (IC50 = 85 nM). Learn MoreStarting at: $140.00
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TB 21007
TB 21007 is a GABAA receptor inverse agonist selective for the α5-subtype (Ki values are 1.6, 16, 20 and 20 nM for α5, α2, α1 and α3 subtypes respectively). Learn MoreStarting at: $110.00
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MK 0343
MK 0343 is a subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Learn MoreStarting at: $159.00
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Alphaxalone
Alphaxalone is a neurosteroid anesthetic that directly activates and potentiates GABAA receptor-activated membrane current (IGABA). Learn MoreStarting at: $90.00
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trans-4-Hydroxycrotonic acid
trans-4-Hydroxycrotonic acid binds to the γ-hydroxybutyric acid (GHB) receptor with higher affinity than GHB itself. Learn MoreStarting at: $90.00
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L-838,417
L-838,417 is a subtype-selective GABAA receptor partial agonist, which selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Learn MoreStarting at: $139.00
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SCS
SCS is a potent and selective partial inhibitor of β1-containing GABAA receptors (IC50 values are 4.5, 5.3 and 7.9 nM at α2β1γ1θ, α2β1γ1 and α2β1γ2s GABAA receptors respectively). Learn MoreStarting at: $79.00
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TCS 1205
TCS 1205 is a GABAA α2 agonist and GABAA α1 partial agonist in vitro (Ki values are 14 and 121 nM respectively), which exhibits non-sedative anxiolytic activity in vivo. Learn MoreStarting at: $109.00
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DS2
DS2 is a positive allosteric modulator of δ-subunit containing GABAA receptors (EC50 = 142 nM for α4β3δ receptors), which displays no effects on GABA responses mediated by α4β3γ2 and α1β3γ2 receptors. Learn MoreStarting at: $109.00
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TCS 1105
TCS 1105 is a GABAA benzodiazepine receptor (BZR) ligand which acts as an agonist at α2 and antagonist at α1 benzodiazepine receptors (Ki values are 118 and 245 nM respectively). Learn MoreStarting at: $100.00
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TPMPA
TPMPA is a selective, competitive GABAC antagonist with only minimal effects on GABAA and GABAB receptors (Kb values are 2.1 μM (antagonist), 320 μM (antagonist) and EC50 ~ 500 μM (weak agonist) respectively). Learn MoreStarting at: $110.00
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FGIN-1-27
FGIN-1-27 binds specifically and with high affinity to the peptide DBI receptor (benzodiazepine receptor) on mitochondrial membranes, inducing production of neurosteroids, which modulate GABA receptors (EC50 = 3 nM for increase in production of pregnenolone in glial cells). Learn MoreStarting at: $90.00
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Hispidulin
Hispidulin is a partial positive allosteric modulator at the benzodiazepine receptor (IC50 = 1.3 μM for inhibition of flumazenil binding). Learn MoreStarting at: $155.00
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FGIN-1-43
FGIN-1-43 is the most active of the 2-aryl-3-indoleacetamides; a new class of potent and specific ligands as probes for the mitochondial DBI receptor (peripheral benzodiazepine receptor). Learn MoreStarting at: $90.00
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CGP 54626 hydrochloride
CGP 54626 hydrochloride is a potent, selective GABAB receptor antagonist (IC50 = 4 nM). Learn MoreStarting at: $135.00
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CGP 55845 hydrochloride
CGP 55845 hydrochloride is a potent, selective GABAB receptor antagonist (IC50 = 5 nM) that prevents agonist binding (pKi = 8.35) and inhibits GABA and glutamate release (pEC50 values are 8.08 and 7.85 respectively). Learn MoreStarting at: $140.00
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U 93631
U 93631 is a GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Learn MoreStarting at: $118.00
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Org 20599
Org 20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptors (EC50 = 1.1 μM) which displays positive modulation of glycine receptors (EC50 = 22.9 μM). Learn MoreStarting at: $140.00
