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 GABAA 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.
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- CAS. Nr.: 1615763-33-1
- Formel: C7H11NO2
- Molecular Weight:141.17
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.59 μM
Compound: 4
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Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
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[PMID: 25147609] |
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 (KB = 0.47 μM)[1].
Bicyclo-GABA (0.01-100 μM) shows agonistic activity at human α1β2γ2 GABAA 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.
Chemical Information
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CAS. Nr. 1615763-33-1
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Molecular Weight 141.17
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Formel C7H11NO2
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SMILES
N[C@]12[C@](C2)([H])[C@H](CC1)C(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Bicyclo-GABA Related Classifications
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