|Description||Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7, and 8) inhibit adenylyl cyclase. MTEP is a negative allosteric modulator of the mGlu5a receptor subtype (Ki = 42 nM; IC50 = 110 nM). MTEP at 0.3 mg/kg produces antidepressant effects in several rodent models of depression. It also demonstrates neuroprotective potential by preventing excitotoxic neuronal damage when administered through either intrahippocampal or intraperitoneal injection. Additionally, MTEP demonstrates an anxiolytic-like phenotype in rodent models similar to that of benzodiazepines while lacking undesirable sedative and addictive effects.|
|Synonyms||3-((2-Methyl-1,3-thiazol-4-yl)ethyn-yl)pyridine hydrochloride; MTEP|
Lu AF21934 is a selective and brain-penetrating positive allosteric modulator (PAM) of mGlu4 receptors (IC50= 500 nM) on the harmaline-induced tremor and other ...
A caged version of LY 379268. LY 379268 is a selective group II mGlu receptor agonist.
TASP 0433864 is a selective and positive allosteric modulator of mGlu2 receptor (EC50 = 199 and 206 nM for human and rat receptors, respectively) with no agonis...
E4CPG is a group I/group II metabotropic glutamate receptor antagonist with higher potency than (RS)-MCPG.
BMT-145027 is a potent mGluR5 PAM without inherent agonist activity with an EC50 of 47 nM. BMT-145027 is a non-MPEP site PAM to demonstrate in vivo efficacy.
(±)-LY 395756 is a mixed mGlu2 agonist/mGlu3 antagonist.
LY 2389575 hydrochloride
LY 2389575 hydrochloride is a mGluR3 receptor antagonist with IC50 value of 190 nM.
ADX-47273 is a drug used in scientific research which acts as a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5.
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist.
LY-404,039, also known as pomaglumetad, is an amino acid analog drug that acts as a highly selective agonist for the metabotropic glutamate receptor group II su...
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CHPG Sodium salt
The sodium salt of CHPG, which is the selective metabotropic glutamate 5 (mGlu5) receptor agonist.
A caged version of (1S,3R)-ACPD. (1S,3R)-ACPD is a group I/II mGlu agonist.
(2R,4R)-APDC is a selective and relatively potent group II mGluR agonist (EC50 = 0.4, 0.4, > 100, > 100, > 300 and > 300 μM for human mGlu2, mGlu3, mGlu1, mGlu5...
EGLU is a group II mGluR antagonist and also a selective antagonist of presynaptically-mediated (1S,3S)-ACPD-induced depression of motoneuron excitation in neon...
Cinnabarinic acid is a kynurenine pathway metabolite of tryptophan and is produced by the oxidation of 3-Hydroxyanthranilic acid. It is a metabotropic glutamate...
LY2979165 is a mGlu2 agonist, which is a novel potent agent that is used as anti-depressants.
(S)-3-Carboxy-4-hydroxyphenylglycine has been found to be a mixed group II mGlu agonist as well as group I metabotropic glutamate receptor antagonist.
ACET, a potent and selective GluR5-containing kainate receptor antagonist, has been found to exhibit activities in blocking induction of NMDA receptor-independe...
Ro 64-5229 is a selective, non-competitive mGlu2 antagonist.