mGluR
MGluRs are a type of glutamate receptor that are active through an indirect metabotropic process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatory neurotransmitter. Like other metabotropic receptors, mGluRs have seven transmembrane domains that span the cell membrane. Unlike ionotropic receptors, metabotropic glutamate receptors are not ion channels. Instead, they activate biochemical cascades, leading to the modification of other proteins, as for example ion channels. This can lead to changes in the synapse's excitability, for example by presynaptic inhibition of neurotransmission, or modulation and even induction of postsynaptic responses. Eight different types of mGluRs, labeled mGluR1 to mGluR8 (GRM1 to GRM8), are divided into groups I, II, and III. Receptor types are grouped based on receptor structure and physiological activity. The mGluRs are further divided into subtypes, such as mGluR7a and mGluR7b.
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FTIDC是mGlu1活性选择性阴性变构的调节剂(negative allosteric modulator),也是mGlu1 反向激动剂。
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Fenobam是活性选择性 mGlu5 拮抗剂。
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EGLU是高选择性 group II mGlu 拮抗剂。
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E4CPG是Group I/group II mGlu 拮抗剂。
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DMeOB是 mGlu5的阴性变构调节剂(negative allosteric modulator)。
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FTIDC是mGlu1活性选择性阴性变构的调节剂(negative allosteric modulator),也是mGlu1 反向激动剂。
More
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Fenobam是活性选择性 mGlu5 拮抗剂。
More
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EGLU是高选择性 group II mGlu 拮抗剂。
More
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E4CPG是Group I/group II mGlu 拮抗剂。
More
-
DMeOB是 mGlu5的阴性变构调节剂(negative allosteric modulator)。
More