YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.

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, and has anti-tumor activity.

VU6031545 is a potent mGlu 5 negative allosteric modulator with an IC50 of 15 nM. VU6031545 has excellent brain penetrant and oral bioavailability in rats.

VU6024945 is an orally active negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGlu5 NAM) with an IC50 value of 110 nM. VU6024945 can be used in the research of anti-anxiety, anti-depression and Parkinson's disease and other neurological diseases.

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, and has anti-tumor activity.

UBP 1112 is a selective group III mGluR antagonist, with a Kd of 5.1 μM.UBP 1112 shows 96-fold affinity for group III over group II mGlu receptor (Kd, 488 μM), and shows no significant activity at group I mGlu receptor or iGlu receptor.

Troriluzole hydrochloride is a third-generation peptide precursor of Riluzole and is an orally active glutamate modulator. Troriluzole hydrochloride can reduce synaptic glutamate levels and enhance the uptake of synaptic glutamate. Troriluzole hydrochloride shows potential for treating Alzheimer's disease and Generalized Anxiety Disorder (GAD).

Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites[1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment.

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.

FO-4-15 is an mGluR1/CaMKIIα activator. FO-4-15 has a protective effect against H2O2 in human neuroblastoma (SH-SY5Y) cells. FO-4-15 can improve cognitive impairment in Alzheimer’s disease mice by activating the mGluR1/CaMKIIα pathway, and can reduce Aβ accumulation, hyperphosphorylated Tau, and synaptic damage.

BOMA (Compound 7) is a potent and selective metabotropic glutamate receptor 5 (mGluR 5) antagonist with an IC50 value of 3 nM and an Ki value of 3 nM. BOMA is promising for research of various pain states, including acute, persistent and chronic pain, inflammatory pain and neuropathic pain.

AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrochloride activates the BDNF/trkB signaling pathway. AZD 2066 hydrochloride can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.

A-850002 is a metabotropic glutamate receptor (mGluR) antagonist (IC50=27 nM) that significantly attenuates spontaneous pain behavior after skin incision in rats. A-850002 can be used for analgesia research.

1-Benzyl-APDC acts as an agonist for mGluR6, with an EC50 of 20 μM in CHO cells. 1-Benzyl-APDC is a weak antagonist of mGluR2, with an IC50 of 200 μM.

VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM.

For the detailed information of JNJ40411813, the solubility of JNJ40411813 in water, the solubility of JNJ40411813 in DMSO, the solubility of JNJ40411813 in PBS buffer, the animal experiment (test) of JNJ40411813, the cell expriment (test) of JNJ40411813, the in vivo, in vitro and clinical trial test of JNJ40411813, the EC50, IC50,and Affinity of JNJ40411813, Please contact DC Chemicals..

RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.

ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity.

MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.

Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.

VU6046980 is a potent, selective and in vivo active mGlu7 positive allosteric modulator (PAM) with EC50 of 0.15 uM (rat mGlu7).

MK-8768 (MK8768) is a potent, selective mGluR2 negative allosteric modulator (NAM) with IC50 of 9.6 nM, shows no activity against mGluR 1,3,4,5,6,8.

CVN636 is a potent, selective, CNS penetrant and allosteric agonist of mGluR7 with EC50 of 7 and 2 nM for human and mouse mGluR7, respectively.

LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.

JNJ-40411813 is a novel potent positive allosteric modulator of mGlu2 with EC50 of 147 nM. JNJ-40411813 displays >30-fold selectivity over mGlu1 and mGlu3-8, 10-fold over 5-HT2A. JNJ-40411813 displays an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity; has been investigated in the clinic for schizophrenia and anxious depression disorders.

CPPHA is a selective positive allosteric modulator of mGluR5 receptor.

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research.

L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for mGluR2 with an EC50 value of 0.3 nM. L-CCG-I can be used for the research of mGluR family.

VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours).

VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.