mGluR Agonist

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

VU0092273 is a potent mGlu5 positive allosteric modulator (PAM) that also binds to the MPEP site, with an EC₅₀ of 0.27 μM.

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.

MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research.

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.

GSK1331268 is a selective, orally active agonist for mGluR2 with a pEC₅₀ of 6.9. GSK1331268 exhibits good blood-brain barrier penetration. GSK1331268 regulates glutamate signaling, and can be used in research of neurodegenerative and neuropsychiatric diseases.

LBG30300 is a subtype-selective mGlu₂ receptor agonist EC₅₀ 0.6 nM. LBG30300 is blood-brain barrier permeable.

Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC₅₀=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.

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

MGS0008 is an orally active and brain-penetrant metabotropic glutamate receptor 2/3 (mGlu2/3) agonist with EC₅₀ values of 29.4 nM and 45.4 nM for mGluR2 and mGluR3, respectively. MGS0008 is promising for research of central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases.

L-Glutamine-2-¹³C is the ¹³C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) 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.

VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC₅₀ of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable.

cis-ACPD is a potent agonist of NMDA receptor, with an IC₅₀ of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC₅₀s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.

FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC₅₀ values of 48.3 μM and 56.2 μM, 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.

VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC₅₀ of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC₅₀ of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%.

(1S,3R)-ACPD is a mGluR agonist that can depolarize pyramidal cells.