mGluR2 Modulator

O-Phospho-L-serine is the immediate precursor to L-cystein in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.

AZD-8418 is an orally active positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2), with an EC₅₀ of 0.86 μM for rat mGlu2 receptors. AZD-8418 reduces the in vitro binding level of [³H]AZ12559322 in prefrontal cortex brain tissues of non-human primates. AZD8418 enhances the inhibitory effect of the mGlu2/3 agonist DCG-IV (HY-101335) on field excitatory postsynaptic potentials (fEPSP) in rat hippocampal brain slices. AZD-8418 reduces nicotine self-administration behavior in rats, and blocks cue-induced reinstatement of nicotine-seeking and food-seeking behaviors. The attenuating effect on nicotine self-administration behavior develops rapid tolerance, while inhibition of food self-administration behavior requires chronic administration. AZD-8418 can be used in research related to nicotine dependence and neuropsychiatric disorders.

Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.

mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC₅₀ of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research.

JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC₅₀ of 17 nM.

TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC₅₀ values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity.

mGluR2 modulator 5 (Compound 11) is an orally active, selective mGluR2 negative allosteric modulator with an IC₅₀ of 8.9 nM. Pharmacokinetic studies in rats show that mGluR2 modulator 5 can effectively cross the blood-brain barrier. It can modulate cognitive and neurological functions in mood disorders and is suitable for research in the field of neurodegenerative diseases.

mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC₅₀ value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic.

mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC₅₀ value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.