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α5IA

Cat. No. M42182
α5IA Structure
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Biological Activity

α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential.

Chemical Information
Molecular Weight 362.35
Formula C17H14N8O2
CAS Number 215874-86-5
Form Solid
Storage 4°C, protect from light
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] Jun-Wei Cao et al. Neuroscience. Synaptic Transmission from Somatostatin-expressing Interneurons to Excitatory Neurons Mediated by α5-subunit-containing GABAA Receptors in the Developing Visual Cortex

[2] Arnaud Duchon et al. Br J Pharmacol. Long-lasting correction of in vivo LTP and cognitive deficits of mice modelling Down syndrome with an α5-selective GABAA inverse agonist

[3] John R Atack. Curr Top Med Chem. GABAA receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement

[4] John R Atack. Pharmacol Ther. Preclinical and clinical pharmacology of the GABAA receptor alpha5 subtype-selective inverse agonist alpha5IA

[5] John R Atack. CNS Neurosci Ther. GABA(A) receptor subtype-selective efficacy: TPA023, an alpha2/alpha3 selective non-sedating anxiolytic and alpha5IA, an alpha5 selective cognition enhancer

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