Bicyclo-GABA is a selective betaine/GABA transporter 1 (BGT1) competitive, non-transported inhibitor with an IC 50 of 590 nM. Bicyclo-GABA exhibits low micromolar agonistic activity at α 1 β 2 γ 2 GABA A receptors with an EC 50 of 5.1 μM. Bicyclo-GABA displays 129 times higher activity for BGT1 than GAT3. Bicyclo-GABA serves as a valuable tool compound for deciphering its elusive pharmacological role in the brain and periphery.
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