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Guvacine ethyl ester

Cat. No. M39024
Guvacine ethyl ester Structure
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Biological Activity

Guvacine ethyl ester (3.1b) is an alkaloid that can be found in betel nut. Guvacine ethyl ester can be used in the synthesis of GABA uptake inhibitor.

Chemical Information
Molecular Weight 155.19
Formula C8H13NO2
CAS Number 18513-76-3
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] M Eltze et al. Eur J Pharmacol. Characterization of muscarinic receptors mediating vasodilation in rat perfused kidney

[2] W Löscher. Neuropharmacology. Comparative assay of anticonvulsant and toxic potencies of sixteen GABAmimetic drugs

[3] E Falch et al. Drug Des Deliv. GABA uptake inhibitors. Synthesis and effects on audiogenic seizures of ester prodrugs of nipecotic acid, guvacine and cis-4-hydroxynipecotic acid

[4] M Wolf-Pflugmann et al. Arzneimittelforschung. Synthesis and muscarinic activity of a series of tertiary and quaternary N-substituted guvacine esters structurally related to arecoline and arecaidine propargyl ester

[5] E Bungardt et al. Eur J Pharmacol. Characterization of muscarinic receptors mediating vasodilation in guinea-pig ileum submucosal arterioles by the use of computer-assisted videomicroscopy

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