mGluR Agonist

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.

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.

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

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.

MGS 0210 (BCI 838) is an orally active metabolite of glutamate receptor 2/3 (mGluR2/3) agonists. MGS 0210 improves amnesia and reduces anxiety in APP mice. MGS 0210 improves PTSD-related behaviors in a mouse model of post-traumatic stress disorder (PTSD). MGS 0210 can be used in research on neurological disorders such as Alzheimer's disease and major depressive disorder.

(±)-LY395756 is an agonist of mGlu2 receptor and an antagonist of mGlu3 receptor. (±)-LY395756 can distinguish the native mGlu2 and mGlu3 receptors.

mGluR2 agonist 1 (Compound 5b) is a potent and selective metabotropic glutamate 2 receptor (mGluR) agonist with an EC₅₀ of 82 nM. mGluR2 agonist 1 can be used for the research of central nervous system (CNS) diseases.

(RS)-PPG (Standard) is the analytical standard of (RS)-PPG (HY-107514). This product is intended for research and analytical applications. (RS)-PPG is a potent and selective agonist for group III mGluRs. The EC₅₀s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity.

CHPG (sodium salt) (Standard) is the analytical standard of CHPG (sodium salt). This product is intended for research and analytical applications. 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..

AZD-8529 mesylate (Standard) is the analytical standard of AZD-8529 (mesylate) (HY-107457A). This product is intended for research and analytical applications. 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.

VU-29 (Standard) is the analytical standard of VU-29 (HY-107508). This product is intended for research and analytical applications. VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC₅₀=9 nM and K_i=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC₅₀: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).

AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. 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.

Foliglurax monohydrochloride (Standard) is the analytical standard of Foliglurax (monohydrochloride) (HY-108703A). This product is intended for research and analytical applications. 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. AntiparK_insonian effect.

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

VU6005649 (Standard) is the analytical standard of VU6005649 (HY-107982). This product is intended for research and analytical applications. VU6005649 is a blood-brain-barrier penetrant mGlu7/8 receptor agonist with EC₅₀s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.

CBiPES (Standard) is the analytical standard of CBiPES (HY-107505A). This product is intended for research and analytical applications. CBiPES is a potent mGlu2 positive allosteric modulator with an EC₅₀ value of 92.8 nM. CBiPES attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity. CBiPES can be used for research of neurological diseases, such as ParK_inson's disease (PD).

VU0364770 (hydrochloride) (Standard) is the analytical standard of VU0364770 (hydrochloride) (HY-100588A). This product is intended for research and analytical applications. VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride 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 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.

VU0364770 (Standard) is the analytical standard of VU0364770 (HY-100588). This product is intended for research and analytical applications. 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 Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.

LSP1-2111 is a phosphinic glutamate derivative that agonists metabotropic glutamate (mGlu) receptor.