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L-655,708

Cat. No. M7899
L-655,708 Structure
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Biological Activity

Novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.

Chemical Information
Molecular Weight 341.36
Formula C18H19N3O4
CAS Number 130477-52-0
Solubility (25°C) DMSO: 6 mg/mL
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] Congcong Yuan, et al. A multi-dosing regimen to enhance the spatial memory of normal rats with α5-containing GABA A receptor negative allosteric modulator L-655,708

[2] Vladislav Bugay, et al. Mechanisms associated with the antidepressant-like effects of L-655,708

[3] Teng Gao, et al. L-655,708 Does not Prevent Isoflurane-induced Memory Deficits in Old Mice

[4] John R Atack, et al. L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors

[5] John R Atack, et al. In vivo labelling of alpha5 subunit-containing GABA(A) receptors using the selective radioligand [(3)H]L-655,708

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