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CL 218872 

Cat. No. M30446
CL 218872  Structure
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Biological Activity

CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABAAreceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo.

Chemical Information
Molecular Weight 278.23
Formula C13H9F3N4
CAS Number 66548-69-4
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] K W Gee, et al. Life Sci. CL 218872 antagonism of diazepam induced loss of righting reflex: evidence for partial agonistic activity at the benzodiazepine receptor

[2] M E Goldberg, et al. Neuropharmacology. Novel non-benzodiazepine anxiolytics

[3] J H Skerritt, et al. Eur J Pharmacol. Benzodiazepine receptor ligand actions on GABA responses. Benzodiazepines, CL 218872, zopiclone

[4] A Lista, et al. J Neurochem. Modulation of the electrically evoked release of 5-[3H]hydroxytryptamine from rat cerebral cortex: effects of alpidem, CL 218872, and diazepam

[5] J K Wamsley. Am J Psychiatry. GABA-benzodiazepine receptors

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