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> Tiagabine [115103-54-3]

Tiagabine [115103-54-3]

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Cat# HY-B0696-5mg

Size : 5mg

Brand : MedChemExpress

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Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.

For research use only. We do not sell to patients.

Tiagabine Chemical Structure

Tiagabine Chemical Structure

CAS No. : 115103-54-3

This product is a controlled substance and not for sale in your territory.

Description

Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 300 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
> 300 μM
Compound: (R)-1a
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
HEK293 IC50
0.07 μM
Compound: 5
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis
[PMID: 23336362]
HEK293 IC50
0.64 μM
Compound: 5
Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting
Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting
[PMID: 25679268]
HEK293 IC50
0.8 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
0.8 μM
Compound: (R)-1a
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
HEK293 IC50
300 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
300 μM
Compound: (R)-1a
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
HEK293 IC50
800 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
800 μM
Compound: (R)-1a
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
Clinical Trial
Molecular Weight

375.55

Formula

C20H25NO2S2
CAS No.

115103-54-3
SMILES

O=C([C@H]1CN(CC/C=C(C2=C(C)C=CS2)/C3=C(C)C=CS3)CCC1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References

  • [1]. Braestrup C, et al. (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier. J Neurochem. 1990 Feb;54(2):639-47.  [Content Brief]

    [2]. Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40.  [Content Brief]

    [3]. Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70.  [Content Brief]

  • [1]. Braestrup C, et al. (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier. J Neurochem. 1990 Feb;54(2):639-47.

    [2]. Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40.

    [3]. Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70.

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Tiagabine Related Classifications

  • Membrane Transporter/Ion Channel Neuronal Signaling
  • GABA Receptor

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tiagabine115103-54-3NO050328 NO328 TGBNO 050328NO-050328NO328NO 328NO-328GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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