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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MK-801 (Dizocilpine)是一种有效的N-methyl-D-aspartate(NMDA)受体拮抗剂，Ki为30.5 nM。
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CTEP是一种新型，长效的，口服生物有效的，mGlu5受体变构拮抗剂，IC50为2.2 nM，比作用于其他mGlu受体选择性高1000倍以上。
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IEM 1754 dihydrobroMide是一种选择性AMPA/kainate受体抑制剂，作用于GluR1和GluR3，IC50为6 μM。
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MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.MPEP是mGlu5受体非竞争性拮抗剂，IC50为36 nM，还是mGlu4受体的正向变构调节剂。
More
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MK-801 (Dizocilpine)是一种有效的N-methyl-D-aspartate(NMDA)受体拮抗剂，Ki为30.5 nM。
More
-
CTEP是一种新型，长效的，口服生物有效的，mGlu5受体变构拮抗剂，IC50为2.2 nM，比作用于其他mGlu受体选择性高1000倍以上。
More
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IEM 1754 dihydrobroMide是一种选择性AMPA/kainate受体抑制剂，作用于GluR1和GluR3，IC50为6 μM。
More
-
MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.MPEP是mGlu5受体非竞争性拮抗剂，IC50为36 nM，还是mGlu4受体的正向变构调节剂。
More
