mGluR Agonist

AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.

rel-ACPT-I is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects.

(2R,4R)-APDC is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC can be used in the study of epilepsy and other neurological diseases.

(rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC₅₀s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively.

L-Glutamine-¹⁵N₂,d₅ is the deuterium and ¹⁵N-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.

3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC₅₀s in the 2 to 5 μM range.

(2R,4R)-APDC hydrate ((2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate) is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC hydrate affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC hydrate can be used in the study of epilepsy and other neurological diseases.

L-Glutamine-d₄ (L-Glutamic acid 5-amide-d₄) is the deuterium labeled L-Glutamine (HY-N0390). L-Glutamine is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells.

Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.

CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC₅₀: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease, such as Parkinson's disease (PD).

L-Cysteinesulfinic acid (Standard) is the analytical standard of L-Cysteinesulfinic acid. This product is intended for research and analytical applications. 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.

(S)-3-Hydroxyphenylglycine ((S)-3HPG) is a metabotropic glutamate receptor (mGluR) agonist with an EC₅₀ of 98 μM in rats. (S)-3-Hydroxyphenylglycine stimulates phosphoinositide hydrolysis, inhibits ACPD-induced depolarization, and exerts weak agonistic and inhibitory effects on mGluR1-mediated signal transduction. (S)-3-Hydroxyphenylglycine selectively activates mGluR1/5, downregulates NMDA receptor channels, reduces NMDA whole-cell currents and intracellular Ca²⁺ accumulation, and induces rapid intracellular Ca²⁺ oscillations in cortical neurons.

NPEC-caged-LY379268 is a type II mGluR agonist.

DL-AP4 sodium (2-Amino-4-phosphonobutyric acid sodium) is an agonist for metabotropic glutamate receptors (mGluR). DL-AP4 sodium binds to mGluR4, activates the signaling pathway that is negatively correlated with adenylate cyclase, and inhibits the Forskolin (HY-15371)-induced production of cAMP. DL-AP4 sodium is also an inhibitor for ON channel, that reduces the sensitivity of photoreceptors to brightness changes.

mGluR2 agonist 1 hydrochloride is a potent selective agonist for metabotropic glutamate receptors mGluR 2 with EC₅₀ of 82 nM.

THIIC (LY2607540) is a compound with anxiolytic and antidepressant potential. It is a positive allosteric modulator of mGlu receptors, exhibits anxiolytic and antidepressant-like activities in multiple animal models, and can also affect sleep and neurochemical changes.

Lu AF11205 is a mGlu5 receptor positive allosteric modulator with activity modulating mGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.

LY2979165 free base is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist.

TC-N 22A is a potent, selective, orally active and brain-permeable mGlu₄ PAM with an EC₅₀ of 9 nM in human mGlu₄-expressing BHK cells. TC-N 22A is less active (EC₅₀>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.

Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8.