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RWJ-51204 

Cat. No. M29148
RWJ-51204  Structure
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Biological Activity

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

Chemical Information
Molecular Weight 399.39
Formula C21H19F2N3O3
CAS Number 205701-85-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] W N Wu, et al. Eur J Drug Metab Pharmacokinet. Metabolism of the new nonbenzodiazepine anxiolytic agent, RWJ-51204, in mouse, rat, dog, monkey and human hepatic S9 fractions, and in rats, dogs and humans

[2] John R Atack. Curr Drug Targets CNS Neurol Disord. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site

[3] Barry Dubinsky, et al. J Pharmacol Exp Ther. 5-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5]imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide (RWJ-51204), a new nonbenzodiazepine anxiolytic

[4] M K Scott, et al. Prog Med Chem. New directions in anxiolytic drug research

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Keywords: RWJ-51204  supplier, GABA Receptor, inhibitors, activators


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