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MTEP hydrochloride 

Cat. No. M27900
MTEP hydrochloride  Structure
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 236.72
Formula C11H9ClN2S
CAS Number 1186195-60-7
Form Solid
Solubility (25°C) Water 20 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
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] Karima Schwab, et al. Cell Signal. Glutamatergic transmission and receptor expression in the synucleinopathy h-α-synL62 mouse model: Effects of hydromethylthionine

[2] D L Arndt, et al. Psychopharmacology (Berl). Environmental condition alters amphetamine self-administration: role of the MGluR₅ receptor and schedule of reinforcement

[3] Richard W Foltin. Behav Pharmacol. The behavioral pharmacology of anorexigenic drυgs in nonhuman primates: 30 years of progress

[4] Margaret J Gill, et al. Psychopharmacology (Berl). Impact of mGluR5 during amphetamine-induced hyperactivity and conditioned hyperactivity in differentially reared rats

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

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  Catalog
Abmole Inhibitor Catalog




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