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MTEP
3-((2-Methyl-4-thiazolyl)ethynyl)pyridine (MTEP) is a research drug that was developed by Merck & Co. as a selective allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5 Metabotropic glutamate receptor 5 is an excitatory Gq-coupled G protein-coupled receptor predominantly expressed on the postsynaptic sites of neurons. In humans, it is encoded by the ''GRM5'' gene. Function The amino acid L- glutamate is the .... Identified through structure-activity relationship studies on an older mGluR5 antagonist MPEP, MTEP has subsequently itself acted as a lead compound for newer and even more improved drugs. MTEP is both more Potency (pharmacology), potent and more Functional selectivity, selective than MPEP as a mGluR5 antagonist, and produces similar neuroprotective, antidepressant, analgesic, and anxiolytic effects but with either similar or higher efficacy depending on the test used. MTEP also has similar efficacy to MPEP in reducing the symptoms of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2-Methyl-6-(phenylethynyl)pyridine
2-Methyl-6-(phenylethynyl)pyridine (MPEP) is a research drug which was one of the first compounds found to act as a selective Antagonist (pharmacology), antagonist for the metabotropic glutamate receptor subtype Metabotropic glutamate receptor 5, mGluR5. After being originally patented as a liquid crystal for LCDs, it was developed by the pharmaceutical company Novartis in the late 1990s. It was found to produce neuroprotective effects following acute brain injury in animal studies, although it was unclear whether these results were purely from mGluR5 blockade as it also acts as a weak NMDA antagonist, and as a positive allosteric modulator of another subtype Metabotropic glutamate receptor 4, mGlu4, and there is also evidence for a functional interaction between mGluR5 and NMDA receptors in the same populations of neurons. It was also shown to produce antidepressant and anxiolytic effects in animals, and to reduce the effects of morphine withdrawal, most likely due to direct inter ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |