mGluR Agonist

CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..

CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC₅₀ value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability.

Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC₅₀ of 79 nM. Antiparkinsonian effect.

L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC₅₀s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC₅₀ of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression.

L-Glutamine-1-¹³C is the ¹³C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na⁺-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.

L-Cysteinesulfinic acid monohydrate is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC₅₀s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

VU6005649 is a blood-brain-barrier penetrant mGlu_7/8 receptor agonist with EC₅₀s of 0.65 μM and 2.6 μM for mGlu₇ receptor and mGlu₈ receptor, respectively.

JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC₅₀ of 260 nM.

(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with K_i values of 0.9 μM and 3.9 μM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with K_is of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.

VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC₅₀ value of 16 nM and a K_i of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice. VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC₅₀ of 500 nM for mGlu4 receptor.

DCG-IV is a potent agonist of group II mGluRs with EC₅₀s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC₅₀: mGlu1R/5R=389/630 μM) and III receptors (IC₅₀: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.

(S)-3,4-DCPG ((S)-3,4-Dicarboxyphenylglycine) is a potent and selective mGlu8a receptor agonist with an EC₅₀ of 31 nM for human mGlu8a. (S)-3,4-DCPG inhibits Forskolin (HY-15371)-stimulated cAMP formation by activating mGlu8, and modulates presynaptic glutamatergic transmission and synaptic plasticity. (S)-3,4-DCPG can be used in research on inflammatory pain, neuropathic pain, autism spectrum disorder, and glutamatergic synaptic plasticity.

Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.

AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

Kainic acid hydrate is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid hydrate induces seizures.

VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.