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Guvacine hydrobromide

Cat. No. M42180
Guvacine hydrobromide Structure
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Biological Activity

Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor.

Chemical Information
Molecular Weight 208.05
Formula C6H10BrNO2
CAS Number 6027-92-5
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] S M McELVAIN et al. J Am Chem Soc. Piperidine derivatives; the preparation of l-benzoyl-3-carbethoxy-4-piperidone; a synthesis of guvacine

[4] W Soudijn et al. Curr Med Chem. The GABA transporter and its inhibitors

[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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