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Abecarnil

Cat. No. M27809
Abecarnil Structure
Synonym:

ZK 112119

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Quality Control & Documentation
Biological Activity

Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.

Chemical Information
Molecular Weight 404.46
Formula C24H24N2O4
CAS Number 111841-85-1
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] Christopher K Gale, et al. BMJ Clin Evid. Generalised anxiety disorder

[2] D N Stephens, et al. Psychopharmacol Ser. Abecarnil: a novel anxiolytic with mixed full agonist/partial agonist properties in animal models of anxiety and sedation

[3] I Pribilla, et al. Psychopharmacol Ser. Abecarnil is a full agonist at some, and a partial agonist at other recombinant GABAA receptor subtypes

[4] G K Mumford, et al. J Pharmacol Exp Ther. Abecarnil and alprazolam in humans: behavioral, subjective and reinforcing effects

[5] D N Stephens, et al. J Pharmacol Exp Ther. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors

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