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Wf-516 

Cat. No. M29884
Wf-516  Structure
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Biological Activity

Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.

Chemical Information
Molecular Weight 502.39
Formula C25H25Cl2N3O4
CAS Number 310392-94-0
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] Takeaki Saijo, et al. PLoS One. Presynaptic selectivity of a ligand for serotonin 1A receptors revealed by in vivo PET assays of rat brain

[2] Takeaki Saijo, et al. Int J Neuropsychopharmacol. Utility of small-animal positron emission tomographic imaging of rats for preclinical development of drugs acting on the serotonin transporter

[3] M El Mansari, et al. Naunyn Schmiedebergs Arch Pharmacol. In vivo electrophysiological assessment of the putative antidepressant Wf-516 in the rat raphe dorsalis, locus coeruleus and hippocampus

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Keywords: Wf-516  supplier, Serotonin Transporter, inhibitors, activators


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