mGluR Modulator

O-Phospho-L-serine-¹³C₃,¹⁵N is the ¹³C- and ¹⁵N-labeled O-Phospho-L-serine. O-Phospho-L-serine is the immediate precursor to L-serine 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.

VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease.

Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice.

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

TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC₅₀ of 1 μM.

Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC₅₀ values of 64.6 nM and 197 nM for hmGlu₄/Gqi5 and rmGlu₄ GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.

ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an K_i value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker. ML353 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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.

VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC₅₀ of 4.6 μM.

(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC₅₀ of 168 nM for potentiation .

ML254 is a potent mGlu₅ potentiator, with EC₅₀ and pEC₅₀ of 9.3 nM and 8.03 nM for rat mGlu₅, respectively. ML254 can be used for researching schizophrenia. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Ro 01-6128 is a positive allosteric modulator of mGluR1.

PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC₅₀ of 1.5 μM) negative allosteric modulator and mGluR3 (EC₅₀ of 8.9 μM) positive allosteric modulator.

mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC₅₀ of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay.

DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).

VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu₁ receptor, with an IC₅₀ of 99 nM.

mG2N001 is a negative allosteric modulator (NAM) (IC₅₀: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope ^[11C]mG2N001 can be used in PET imaging. ^[11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images.

LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu₅ (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC₅₀ values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.

JNJ-40068782 is a potent positive allosteric modulator of the mGlu2 receptor, with the IC₅₀ of 38 nM.

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.