gat-1

6,7-Dimethylisatin (6,7-dimethyl-1H-indole-2,3-dione) inhibits hGAT3 with IC50 of 108 μM. 6,7-Dimethylisatin also inhibits hBGT1, hGAT2.

DGAT-1 inhibitor 2 is an effective DGAT-1 inhibitor and anti-obesity drug. DGAT-1 (acyl-CoA: diacylglycerol acyltransferase 1) is one of two known DGAT enzymes that catalyze the final step of triglyceride synthesis. Transgenic mice and pharmacological studies indicate that inhibiting DGAT1 is a promising strategy for treating obesity and type 2 diabetes.

NO 711（NNC-711 free acid） is a potent and selective inhibitor of GABA transporter 1 (GAT-1), which increases GABAergic transmission, enhances non-rapid eye movement sleep, and prevents and treats paclitaxel-induced neuropathic pain.

E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.

SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.

NNC 05-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1), which inhibits GABA reuptake and thereby increases GABA levels in the synaptic gap, exerting anticonvulsant and analgesic effects.

mGAT-IN-1 is a potent, non-selective GAT inhibitor that inhibits mGAT3 activity well (IC50: 2.5 μM, pIC50: 5.61).

SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.

Guvacine hydrobromide, an alkaloid derived from the Areca catechu nut, serves as a potent inhibitor of GABA (GABA uptakp) uptake. It effectively inhibits rat GABA transporter isoforms GAT-1, GAT-2, and GAT-3, with respective IC50 values of 39 μM, 58 μM, and 378 μM [1].

Guvacine can enhance the inhibition of spinal neurones by GABA.