|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|
The hydrochloride salt form of ACDPP, which has been found to be a mGluR-5 antagonist.
Disodium salt of LY 341495. LY 341495 is a group II metabotropic glutamate receptor antagonist.
(±)-LY 395756 is a mixed mGlu2 agonist/mGlu3 antagonist.
(RS)-PPG is a potent and selective group III metabotropic glutamate receptor (mGluR) agonist, with approximately 25-fold selectivity for hmGlu8. (RS)-PPG exhibi...
Very selective nanomolar potent antagonist for group II mGlu receptors. Also a relatively potent antagonist for group III mGlu receptors at high nanomolar to lo...
BAY 36-7620 elective mGlu1 receptor non-competitive antagonist (IC50 = 0.16 μM) with inverse agonist activity.
L-AP4 is a selective group III metabotropic glutamate receptor (mGluR) agonist. It also acts as an agonist at the quisqualate-sensitized AP6 site in hippocampus...
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 ...