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Guvacine

Cat. No. M11530
Guvacine  Structure
Size Price Availability Quantity
10mg USD 300  USD300 In stock
20mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

Guvacine, an alkaloid found in areca nut, is an effective inhibitor of GABA uptake. Guvacine inhibited rat GAT-1 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.

Chemical Information
Molecular Weight 127.14
Formula C6H9NO2
CAS Number 498-96-4
Storage 2-8℃
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Maren Schaarschmidt, et al. ChemMedChem. Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3-Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1

[2] Qihai Xu, et al. Org Lett. Catalytic Enantioselective Synthesis of Guvacine Derivatives through [4 + 2] Annulations of Imines with α-Methylallenoates

[3] L J Knutsen, et al. J Med Chem. Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents

[4] M R Pavia, et al. J Med Chem. Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake

[5] D Lodge, et al. Brain Res. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system

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