mglur1

IEM 1754 2HBr (IEM 1754 dihydrobromide) is a selective AMPA kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

S-Sulfo-L-cysteine sodium salt shows a weak affinity for mGluR1α and mGluR5a at high concentrations and has potential antioxidant activity.

L-Glutamic acid monosodium salt (MSG) (Monosodium glutamate) is an activator of mGlu1 receptor.

(S)-3-Hydroxyphenylglycine is an agonist of group I metabotropic glutamate receptors (mGluRs).

LY341495 is a potent metabotropic glutamate receptor antagonist that exhibits high activity against a wide range of glutamate receptor subtypes and can be used for the study of neurological disorders.

VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.

FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 val

FPTQ is a highly effective antagonist of mGluR 1, displaying IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively [1]. In addition to its robust inhibitory properties, FPTQ exhibits notable antioxidant and anti-inflammatory effects in both in vitro and in vivo settings [2].

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. No activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM.

VU 0469650 is a potent and selective negative allosteric modulator of mGluR1 (IC50 = 99 nM).

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

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

DHPG ((RS)-3,5-DHPG) is an effective antagonist of mGluR linked to phospholipase D. As an amino acid, it serves as a selective and potent agonist for Group I mGluR (mGluR 1 and mGluR 5) without affecting Group II or Group III mGluRs.

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

GYKI 53655 hydrochloride (LY300168 hydrochloride) is an antagonist of AMPA and is used in the study of neurological disorders.

FO-4-15 is an activator of mGluR1 CaMKIIα. It exhibits protective effects against H2O2 in human neuroblastoma (SH-SY5Y) cells. In mice with Alzheimer's disease, FO-4-15 enhances cognitive function by activating the mGluR1 CaMKIIα pathway, reducing Aβ accumulation, Tau hyperphosphorylation, and synaptic damage.

VU6024578 (BI02982816) is an orally bioavailable and selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR1. It demonstrates activation with EC50 values of 54 nM for human mGluR1 and 46 nM for rat mGluR1. VU6024578 shows antipsychotic activity in rat models of amphetamine-induced hyperactivity and MK-801-induced novel object recognition (NOR). Additionally, it possesses blood-brain barrier permeability.

A-841720 is a potent, selective, and non-competitive antagonist of the mGlu1 receptor, exhibiting an IC 50 value of 10 nM specifically for the human mGlu1 receptor. It demonstrates a 34-fold greater selectivity for mGlu1 over mGlu5 (IC 50 of 342 nM), with negligible activity across a spectrum of other neurotransmitter receptors, ion channels, and transporters. Additionally, A-841720 possesses analgesic potential within a certain dose range [1] [2].

CPCCOEt is a low-affinity, selective, non-competitive, and reversible antagonist of mGluR1b.

Ro 67-4853 is a selective mGluR1 positive allosteric modulator, enhancing the response to the agonist (S)-3,5-dihydroxyphenylglycine (DHPG) in anesthetized rats through iontophoretic administration.

VU-29 is a positive allosteric mGlu5 receptor modulator with an EC50 of 9 nM and a Ki of 244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes [EC50: rmGluR1 rmGluR2=557 nM 1.5 μM; hmGluR4=154 nM].

metabotropic glutamate receptor type 1 (mGlu1) antagonist