Date published: 2025-9-18

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mGluR-5 Inhibitors

The array of mGluR-5 inhibitors encompasses a sophisticated cadre of compounds meticulously designed to intricately modulate the activation of metabotropic glutamate receptor 5 (mGluR-5). These compounds, exemplified by MTEP, Fenobam, and MPEP, function as negative allosteric modulators, finely tuning the receptor's responsiveness to glutamate and subsequently interfering with downstream signaling pathways. MTEP, for instance, is a potent antagonist that disrupts the receptor's response to glutamate, showcasing the precision with which these inhibitors can be tailored to regulate mGluR-5 activity. Further expanding the toolkit are competitive antagonists like BAY 36-7620, selective inhibitors such as Mavoglurant, and positive allosteric modulators like CTEP and VU0361737. These compounds not only inhibit mGluR-5 but also bring a nuanced layer of modulation, influencing the receptor's intricate signaling dynamics. Mavoglurant, for instance, serves as a selective antagonist, offering researchers a specific tool to dissect mGluR-5 function in various cellular contexts. Positive allosteric modulators like CTEP and VU0361737, on the other hand, showcase the complexity of mGluR-5 modulation by enhancing receptor activity in a unique manner. The diverse chemical mechanisms exhibited by these inhibitors enable researchers to investigate the detailed regulatory processes that govern mGluR-5 activation. Whether through competitive inhibition or allosteric modulation, these compounds provide invaluable insights into the specific pathways influenced by mGluR-5 inhibition. This class of inhibitors thus stands as a testament to the meticulous design and understanding required for precise modulation of glutamatergic signaling. In summary, the inhibitors of mGluR-5 present a sophisticated repertoire of compounds, each with a unique mode of action, allowing researchers to precisely manipulate the receptor's activity. This nuanced toolkit not only contributes to the detailed understanding of mGluR-5 but also broadens our comprehension of the intricate signaling networks that govern cellular processes influenced by glutamate receptors.

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