Bicyclo-GABA 

Bicyclo-GABA is a selective betaine/GABA transporter 1 (BGT1) competitive, non-transported inhibitor with an IC₅₀ of 590 nM. Bicyclo-GABA exhibits low micromolar agonistic activity at α₁β₂γ₂ GABA_A receptors with an EC₅₀ 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^[1].

Bicyclo-GABA (0.1-10000 nM; 3 min) potently inhibits [³H]GABA uptake at human BGT1 (IC₅₀ = 1.5 μM)^[1].
Bicyclo-GABA (0-10 μM) acts as a non-transported competitive inhibitor of human BGT1 (K_B = 0.47 μM)^[1].
Bicyclo-GABA (0.01-100 μM) shows agonistic activity at human α₁β₂γ₂ GABA_A receptors (EC₅₀ = 5.1 μM)^[1].
Bicyclo-GABA modulates inhibitory activity at BGT1 and GAT3 mutants (IC₅₀ range: 0.040-610 μM) in the cell-based [³H]GABA uptake assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

141.17

C₇H₁₁NO₂

1615763-33-1

N[C@]12[C@](C2)([H])[C@H](CC1)C(O)=O

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• [1]. Kickinger S, et al. Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1. Front Chem. 2021;9:736457. Published 2021 Sep 14.  [Content Brief]