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GABAA receptor agent 1 

Cat. No. M28615
GABAA receptor agent 1  Structure
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Biological Activity

GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity.

Chemical Information
Molecular Weight 273.67
Formula C13H8ClN3O2
CAS Number 1571-87-5
Form Solid
Solubility (25°C) DMSO 83.33 mg/mL (ultrasonic)
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] Vikram Babu Kasaragod, et al. Nature. Mechanisms of inhibition and activation of extrasynaptic αβ GABAA receptors

[2] Yuya Sakimoto, et al. Int J Mol Sci. Significance of GABAA Receptor for Cognitive Function and Hippocampal Pathology

[3] Alison L Althaus, et al. Neuropharmacology. Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator

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

[5] K Nishikawa, et al. Anesthesiology. Agent-selective effects of volatile anesthetics on GABAA receptor-mediated synaptic inhibition in hippocampal interneurons

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