mglur1

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.

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

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.

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

CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist (IC50: 2.6 nM). The selectivity of CFMTI to mGluR1 is higher 2000-fold than mGluR5.

NPS2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 (IC50 of 5.2 and 82 nM, respectively)

JNJ16259685 (TN.T 16259685) is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM.

L-Cysteinesulfinic acid monohydrate is a potent agonist at 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 [1].

Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. It is a selective antagonist of mycotoxins M1 receptors, exhibiting high (Ki=84 nM, M1 receptors) and low (Ki=1.65 μM, M2 receptors) affinity, with a 20-fold difference. Oxomemazine is an antihistamine and anticholinergic agent used in cough studies[1][2].

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.

(RS)-MCPG ((±)-MCPG) is a non-selective group I/II metabotropic glutamate receptor antagonist.

Ro0711401 is an agonist of mGlu1 receptor.

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].

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

LY456066 is a mGluR1 receptor-selective, negative allosteric modulator.

trans-ACPD ((±)-trans-ACPD) is an equimolecular mixture of (1S, 3R)- and (1R, 3S)-ACPD. trans-ACPD is a selective agonist of the mGluR (metabotropic glutamate receptor); active at the group I II mGlu receptors (EC50: 2 15 23 800 μM, mGluR2 1 5 4).

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].

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

CFMMC is an allosteric mGluR1 antagonist agent.

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.

L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors [mGluRs, pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively].

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