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MTEP 

Cat. No. M29921
MTEP  Structure
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Quality Control & Documentation
Biological Activity

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research.

Chemical Information
Molecular Weight 200.26
Formula C11H8N2S
CAS Number 329205-68-7
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] Alexandra V Dyomina, et al. Int J Mol Sci. MTEP, a Selective mGluR5 Antagonist, Had a Neuroprotective Effect but Did Not Prevent the Development of Spontaneous Recurrent Seizures and Behavioral Comorbidities in the Rat Lithium-Pilocarpine Model of Epilepsy

[2] Xiaohua Zhang, et al. J Neurosci Res. MTEP impedes the neuronal polarization and the activity of the Akt-NF-κB pathway in rat hippocampal neurons

[3] Matthew J McIldowie, et al. J Pharm Sci. Physical and crystallographic characterisation of the mGlu5 antagonist MTEP and its monohydrochloride

[4] Paul M Lea 4th, et al. CNS Drug Rev. Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP

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