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Talampanel

Cat. No. M7351
Talampanel Structure
Synonym:

GYKI-53773; LY-300164

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Biological Activity

Talampanel is a non-competitive AMPA/kainate receptor antagonist that displays 2.3-3-fold more potent activity than GYKI 52466. Potentiates the anticonvulsive activity of antiepileptic drugs in animal models of seizures. Orally active.

Chemical Information
Molecular Weight 337.37
Formula C19H19N3O3
CAS Number 161832-65-1
Solubility (25°C) DMSO 33.74 mg/mL
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] Eglen, et al. Br J Pharmacol. The action of SDZ 205,557 at 5-hydroxytryptamine (5-HT3 and 5-HT4) receptors.

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Keywords: Talampanel, GYKI-53773; LY-300164 supplier, inhibitors, activators


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