524924-75-2
Chemical Structure
Methoxymethyl-MTEP
- CAS No.: 524924-75-2
- Formula:C13H12N2OS
- Molecular Weight:244.31
InChIKey: AWDRAHDWMICWJM-UHFFFAOYSA-N
SMILES: COCC1=CC(C#CC2=CSC(C)=N2)=CN=C1
Biological Activity: Methoxymethyl-MTEP is a selective, high-affinity mGluR5 antagonist. Methoxymethyl-MTEP can serve as a radiotracer ligand, readily entering the brain and providing mGluR5-specific signal in gray matter regions. Methoxymethyl-MTEP exhibits a Kd = 20 nM as measured by saturation binding assays in rat brain cell membranes, and an IC50 = 30 nM in competitive binding assays. Methoxymethyl-MTEP can be used for research on diseases related to the glutamatergic nervous system, such as excitotoxicity and schizophrenia[1][2].
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Methoxymethyl-MTEP | Methoxymethyl-MTEP is a selective, high-affinity mGluR5 antagonist. Methoxymethyl-MTEP can serve as a radiotracer ligand, readily entering the brain and providing mGluR5-specific signal in gray matter regions. Methoxymethyl-MTEP exhibits a Kd = 20 nM as measured by saturation binding assays in rat brain cell membranes, and an IC50 = 30 nM in competitive binding assays. Methoxymethyl-MTEP can be used for research on diseases related to the glutamatergic nervous system, such as excitotoxicity and schizophrenia. | |||||||||||||||||||||
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References
- [1]. Anderson JJ, et al. [3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. The Journal of pharmacology and experimental therapeutics. 2002 Dec;303(3):1044-51.
- [2]. Williams T, et al. Activation of the mGlu₅ Receptor for the Treatment of Schizophrenia and Cognitive-Deficit-Associated Disorders. In: Celanire S, Poli S (eds). Small Molecule Therapeutics for Schizophrenia. Topics in Medicinal Chemistry, vol 13. Springer, Cham; 2014.
