mGluR Modulator

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.

VU0404251 is a highly potent positive allosteric modulator of mGlu for the study of psychosis.

(S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of mGluR1a and an agonist of mGluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice.

AZ12559322 is a positive allosteric modulator of mGluR2, with the K_i value of 1.31 nM. AZ12559322 can be used in neurological research.

VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.

VU0418506 is a selective positive allosteric modulator of mGlu₄, with EC₅₀ values of 68 nM and 46 nM for hmGlu₄ and rmGlu₄, respectively. VU0418506 exhibits antiparkinsonian activity.

VU0410425 is an mGlu₁ negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu₁ with an IC₅₀ value of 140 nM. VU0410425 can be used for the research of central nervous system disorders.

mGluR2 modulator 6 (Compound 25-a) is a mGluR2 modulator. mGluR2 modulator 6 has anticonvulsant activity in the 6Hz epilepsy model, and the effect is better when combined with Levetiracetam (HY-B0106). mGluR2 modulator 6 can be used in the research of epilepsy.

Troriluzole 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) .

BMS-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.

BMS-952048 is a positive allosteric modulator of mGluR5 with an EC₅₀ of 10 nM.

VU0359516 is a compound that modulates mGluR4 activity, obtained through structure-activity relationship analysis of mGluR4 positive allosteric modulators, with improved potency and efficacy, as well as selectivity for mGluR4.

Raseglurant hydrochloride (Standard) is the analytical standard of Raseglurant hydrochloride (HY-103574). This product is intended for research and analytical applications. Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine.

MNI137 (Standard) is the analytical standard of MNI137 (HY-103572). This product is intended for research and analytical applications. 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.

NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases.

GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats.

RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [³h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers.

LSN2463359 (Standard) is the analytical standard of LSN2463359 (HY-110152). This product is intended for research and analytical applications. LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model. LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

LY2389575 hydrochloride (Standard) is the analytical standard of LY2389575 (hydrochloride) (HY-107509). This product is intended for research and analytical applications. LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC₅₀ value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.

Ro 01-6128 (Standard) is the analytical standard of Ro 01-6128 (HY-107507). This product is intended for research and analytical applications. Ro 01-6128 is a positive allosteric modulator of mGluR1.