mGluR
Metabotropic glutamate receptors
mGluR (metabotropic glutamate receptor) is a type of glutamate receptor that are active through an indirect metabotropic process. They are members of thegroup C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatoryneurotransmitter. The mGluRs perform a variety of functions in the central and peripheral nervous systems: mGluRs are involved in learning, memory, anxiety, and the perception of pain. mGluRs are found in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, and the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Eight different types of mGluRs, labeled mGluR1 to mGluR8, are divided into groups I, II, and III. Receptor types are grouped based on receptor structure and physiological activity.
mGluR Isoform Specific Products
All Product Categories
-
mGluR Related Products (404)
Related Products (404)
-
Antibodies (8)
-
mGluR Isoform Comparison
-
HexylHIBO hydrobromide
0 ImagesCat. No.: HY-175100HexylHIBO hydrobromide is a potent group I mGluR antagonist with Kbs of 140 μM and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO hydrobromide does not inhibits mGlu2 and mGlu4a. HexylHIBO hydrobromide decreases spontaneous excitatory postsynaptic currents (sEPSCs) in rat.
-
Troriluzole hydrochloride
0 ImagesCat. No.: HY-122487ACAS No.: 1926204-76-3Synonyms: BHV-4157 hydrochloride; Trigriluzole hydrochlorideTroriluzole hydrochloride is a third-generation peptide precursor of Riluzole (HY-B0211) 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) .
-
FO-4-15
0 ImagesFO-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.
-
L-Glutamine-2-13C
0 ImagesCat. No.: HY-N0390S11CAS No.: 180991-02-0Synonyms: L-Glutamic acid 5-amide-2-13CL-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
0 ImagesCat. No.: HY-170499CAS No.: 3100913-05-8Synonyms: BI02982816VU6024578 (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
0 ImagesCat. No.: HY-19434ACAS No.: 477331-06-9cis-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.
-
Remeglurant
0 ImagesCat. No.: HY-118238CAS No.: 1309783-00-3Synonyms: MRZ-8456Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the mGlu5 receptor, with an IC50 of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD).
-
FP0429
0 ImagesCat. No.: HY-119060CAS No.: 870860-41-6FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC50 values of 48.3 μM and 56.2 μM, respectively.
-
BMS-955829
0 ImagesCat. No.: HY-120641CAS No.: 1375751-08-8BMS-955829 is an orally active and selective mGluR5 positive allosteric modulator with an EC50 of 2.6 nM. BMS-955829 has no intrinsic agonist activity and a low glutamate fold shift (2.4). BMS-955829 can effectively improve cognitive and executive function deficits in rodents. BMS-955829 can be used in the research of cognitive impairment diseases such as schizophrenia.
-
MAP4
0 ImagesCat. No.: HY-101164CAS No.: 157381-42-5MAP4 is a selective group III mGluR antagonist in some electrophysiological systems.
-
BMS-952048
0 ImagesCat. No.: HY-123874CAS No.: 1375751-32-8BMS-952048 is a positive allosteric modulator of mGluR5 with an EC50 of 10 nM.
-
(S)-3-Hydroxyphenylglycine
0 ImagesCat. No.: HY-100841ACAS No.: 71301-82-1Synonyms: (S)-3HPG(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.
-
BOMA
0 ImagesCat. No.: HY-169808CAS No.: 540496-84-2BOMA (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.
-
VU6033685
0 ImagesCat. No.: HY-173032VU6033685 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%.
-
YM-202074 fumarate
0 ImagesCat. No.: HY-103556CAS No.: 299900-84-8YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate 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 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.
-
mGluR2 modulator 3
0 ImagesCat. No.: HY-147529CAS No.: 1004614-58-7mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.
-
mGluR2 modulator 4
0 ImagesCat. No.: HY-147530CAS No.: 2582758-47-0mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic.
-
VU0366248
0 ImagesCat. No.: HY-119765CAS No.: 1243310-20-4VU0366248 is a mGlu5 negative allosteric modulator.
