1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Guvacine

Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Guvacine hydrochloride) usually boasts enhanced water solubility and stability.

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

Guvacine Chemical Structure

Guvacine Chemical Structure

CAS No. : 498-96-4

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Description

Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively[1].

IC50 & Target

IC50: 39 μM (rat GAT-1), 58 μM (rat GAT-2), 378 μM (rat GAT-3), 14 μM (human GAT-1), 119 μM (huam GAT-3) and 1870 μM (human BGT-3)[1]

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 1000 μM
Compound: 21
Inhibition of mouse BGT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse BGT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
[PMID: 26706177]
HEK293 IC50
114.8 μM
Compound: 21
Inhibition of mouse GAT3 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse GAT3 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
[PMID: 26706177]
HEK293 IC50
14 μM
Compound: 3
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
20.9 μM
Compound: 21
Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
[PMID: 26706177]
HEK293 IC50
72.4 μM
Compound: 21
Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
[PMID: 26706177]
Molecular Weight

127.14

Formula

C6H9NO2

CAS No.
SMILES

O=C(C1=CCCNC1)O

Structure Classification
Initial Source
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
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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.

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