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You are here:Home-Inhibitors & Agonists-Membrane Transporter/Ion Channel-GABA Transporter (GAT)

Request The Product List ofGABA Transporter (GAT) GABA Transporter (GAT)

Cat. No. Product Name CAS No. Information
GY06968

Propyl pyrazole triol

263717-53-9

Propyl pyrazole triol(PPT) is an allosteric GABAA receptor modulator that strongly suppresses GABA-induced chloride currents.

GY06850

HZ-166

612527-56-7

HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors; displays a statistically significant higher affinity for receptors not containing the α1 subunit with a rank order of α5 (Ki=140nM) > α2 (Ki=269 nM) > α1 (Ki=382 nM); The Ki value of HZ166 for the α3β3γ2 combination (185± 47 nM) was statistically significantly lower than the Ki value observed for α1β3γ2 but not different from those of α2β3γ2 and α5β3γ2; HZ-166 is antihyperalgesic in mouse models of inflammatory and neuropathic pain.

GY06849

KRM-II-81

2014348-91-3

KRM-II-81 is a potent, selective α1/α2/α3 GABAA receptors positive allosteric modulator with EC50 of 937 nM for α1β3γ2, negligible efficacy at α4/α5/α6 GABAA receptors; shows α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits.

GY06838

GR3027

2089238-18-4

GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC; inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor; during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor; restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy.

GY06673

CI-966 hydrochloride

110283-66-4

CI-966 (PD 126141) is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively; displays >200-fold selectivity over GAT-2 and GAT-3; shows anticonvulsive and neuroprotective activity in vivo.

GY06672

CI-966

110283-79-9

CI-966 (PD 126141) is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively; displays >200-fold selectivity over GAT-2 and GAT-3; shows anticonvulsive and neuroprotective activity in vivo.

GY06619

NNC-711

145645-62-1

NNC-711 is a potent and selective inhibitor of GABA uptake by GAT-1 with IC50 of 0.04 uM; displays excellent selectivty over rGAT-2, hGAT-3 and hBGT-1, and other other neurotransmitter receptors; inhibits synaptosomal (IC50=47 nM), neuronal (IC50=1238 nM) and glial (IC50=636 nM) GABA uptake in vitro; demonstrates potent anticonvulsant activity against rodent seizures induced by DMCM.

GY06610

SNAP 5114

157604-55-2

SNAP 5114 is a GABA transport inhibitor with IC50 of 5, 21, 388 and 140 uM for hGAT-3, rGAT-2, hGAT-1 and BGT-1, respectively; increases thalamic GABA levels and is an anticonvulsant following systemic administration in vivo.

GY06578

NNC 05-2090 hydrochloride

184845-18-9

NNC 05-2090 is a potent selective GABA transporter inhibitor of mGAT2 with Ki of 1.4 uM; displays >10 fold selectivity over mGAT1, mGAT3 and mGAT4, also has alpha 1- and D2-receptor affinity of 266 and 1632 nM, respectively; inhibits 3HGABA uptake into synaptosomes from cerebral cortex with IC50 of 4.4 uM; significantly reduces generalized seizure severity and afterdischarge duration in rats.

GY06470

SKF-89976A hydrochloride

85375-15-1

SKF-89976A hydrochloride is a potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1; shows little to no activity for rGAT-2, hGAT-3 and hBGT-1 (IC50>500 uM); blocks GABA uptake and uncoupled transmitter-gated current with Ki of 7 uM and 0.03 uM, respectively.

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