hgat-3

(S)-SNAP5114 是一种选择性的 GABA 转运抑制剂，对 hGAT-3 的 IC50 为 5 μM，对 rGAT-2 的 IC50 为 21 μM。 (S)-SNAP5114 具有抗惊厥性质。

NNC052090 is a GABA uptake inhibitor that displays moderate selectivity for BGT-1 transporters with Ki values are 1.4, 15, 19 and 41 μM for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively. NNC052090 also displays affinity at α1- and D2-receptors with IC50

GABAA receptor agent 2 TFA 是一种有效的、高亲和力的 GABAA 受体拮抗剂，IC50为 24 nM (表达人 α1β2γ2GABAA 的 tsA201 细胞)，Ki 为 28 nM (大鼠GABAA 受体)。GABAA receptor agent 2 TFA 对四种人类 GABA 转运蛋白 (hGAT-1，hBGT-1，hGAT-2 和 hGAT-3) 没有作用。

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.