mGluR Activator

Talaglumetad (LY-544344) is an orally active prodrug of Eglumegad (HY-18941) and a metabotropic glutamate receptor 2/3 (mGluR2/3) agonist. Talaglumetad undergoes transmembrane transport via the intestinal peptide transporter hPepT1, and is enzymatically hydrolyzed to produce L-alanine and the parent drug Eglumegad after entering the body. Talaglumetad can be used in research related to metabotropic glutamate receptor 2-associated neurological systems.

β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride activates mGluR3 and inhibits PKC. β-N-methylamino-L-alanine hydrochloride can be used in the research of neurodegenerative diseases and immune diseases.

Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC₅₀ of 45 nM and a K_i of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis indica.

ADX88178 is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC₅₀ of 3.5 nM against hmGluR4. ADX88178 modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease.

Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca²⁺ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.

VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC₅₀s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy.

Fasoracetam (NS 105) is the activator of metabotropic glutamate receptor (mGluR). Fasoracetam (NS 105) has the potential for the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimer's disease (AD).

ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC₅₀ of 2.4 nM and K_i of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury.

Clenbuterol (Standard) is the analytical standard of Clenbuterol. This product is intended for research and analytical applications. Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM. Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator.

VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC₅₀ of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research.

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.

VU0477886 is a metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator with potent activating activity on mGlu4 (EC₅₀ = 95nM, 89% Glu Max), good pharmacokinetic characteristics (brain: plasma Kp = 1.3), and significant therapeutic efficacy in Parkinson's disease models.

ADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC₅₀ of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease.

mGluR1 activator-1 is a stable Vitamin K (HY-B2172) analogue and a mGluR1 activator that can penetrate the blood-brain barrier. mGluR1 activator-1 exhibits strong transcriptional activation via steroid and xenobiotic receptor as well as retinoic acid receptor. mGluR1 activator-1 induces neuronal differentiation in mouse neural progenitor cells. mGluR1 activator-1 can be used for the study of neurodegenerative disease such as Alzheimer’s.

Nefiracetam (Standard) is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca²⁺ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.

Fasoracetam (Standard) is the analytical standard of Fasoracetam (HY-107481). This product is intended for research and analytical applications. Fasoracetam (NS 105) is the activator of metabotropic glutamate receptor (mGluR). Fasoracetam (NS 105) has the potential for the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimer's disease (AD).