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TPA 023 

Cat. No. M29696
TPA 023  Structure
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Biological Activity

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.

Chemical Information
Molecular Weight 395.43
Formula C20H22FN7O
CAS Number 252977-51-8
Form Solid
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] Lakshmi Rajagopal, et al. Neuropsychopharmacology. TPA-023 attenuates subchronic phencyclidine-induced declarative and reversal learning deficits via GABAA receptor agonist mechanism: possible therapeutic target for cognitive deficit in schizophrenia

[2] Elif Engin, et al. Pharmacol Ther. α2-containing GABA(A) receptors: a target for the development of novel treatment strategies for CNS disorders

[3] Hanns Möhler. Neuropharmacology. The GABA system in anxiety and depression and its therapeutic potential

[4] John R Atack. Curr Top Behav Neurosci. GABAA receptor alpha2/alpha3 subtype-selective modulators as potential nonsedating anxiolytics

[5] John R Atack. Curr Top Med Chem. GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics

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