Date published: 2025-11-25

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mGluR-6 Inhibitors

mGluR-6 inhibitors are a category of chemical compounds specifically designed to target and inhibit the metabotropic glutamate receptor 6 (mGluR-6). mGluR-6 is a type of G-protein coupled receptor (GPCR) that plays a significant role in cellular signaling processes. It is primarily found in the retina, where it is involved in the phototransduction cascade, a critical process for visual perception. The functioning of mGluR-6 is distinctive as it is activated by the neurotransmitter glutamate, leading to a series of intracellular events that modulate neuronal activity. The structure of mGluR-6 is characterized by a large extracellular domain, seven transmembrane domains, and an intracellular C-terminal. This structural configuration is essential for its ability to bind glutamate and transduce signals across the cell membrane. The inhibitors of mGluR-6 are designed to interact with the receptor in a way that prevents its activation by glutamate, thereby modulating the receptor's signaling pathway. The development of mGluR-6 inhibitors involves a complex and multifaceted approach that combines insights from molecular biology, pharmacology, and chemistry. The design of these inhibitors is based on a deep understanding of the receptor's three-dimensional structure and the molecular dynamics of its interaction with glutamate. Advanced techniques such as X-ray crystallography and cryo-electron microscopy are employed to elucidate the receptor's structure, particularly focusing on the binding site for glutamate. This structural information is pivotal in guiding the synthesis of compounds that can effectively bind to and inhibit mGluR-6. Computational methods, including molecular docking and virtual screening, play a crucial role in predicting the binding affinity and specificity of inhibitors. These computational predictions are instrumental in the initial stages of inhibitor development, helping to identify promising compounds for further testing. The process of developing mGluR-6 inhibitors is iterative, involving the synthesis, characterization, and biological testing of numerous compounds. This process is aimed at achieving optimal interaction with the receptor while minimizing off-target effects. The field of mGluR-6 inhibitors is continuously evolving, with ongoing research contributing to a greater understanding of GPCR-mediated signaling and its modulation.

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Items 1 to 10 of 13 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

MAP4

157381-42-5sc-202221
5 mg
$39.00
(0)

MAP4 acts as a selective modulator of the mGluR-6 receptor, characterized by its ability to stabilize receptor conformations through specific hydrophobic interactions and van der Waals forces. This compound influences downstream signaling pathways by altering G-protein coupling dynamics, leading to distinct modulation of intracellular calcium levels. Its unique structural attributes enable it to fine-tune synaptic responses, impacting neuronal excitability and synaptic strength.

LY 341495

201943-63-7sc-361244
sc-361244A
1 mg
10 mg
$87.00
$219.00
1
(1)

LY341495 is a selective antagonist for metabotropic glutamate receptors. It could theoretically downregulate mGluR-6 expression by feedback mechanisms that respond to receptor blockade.

(RS)-CPPG

183364-82-1sc-203448
sc-203448A
5 mg
25 mg
$408.00
$1224.00
1
(0)

(RS)-CPPG serves as a selective antagonist of the mGluR-6 receptor, exhibiting unique binding characteristics that disrupt typical receptor activation. Its molecular structure allows for specific electrostatic interactions with key amino acid residues, influencing receptor desensitization and internalization processes. By modulating the receptor's conformational landscape, (RS)-CPPG alters downstream signaling cascades, affecting neurotransmitter release and synaptic plasticity.

UBP1112

339526-74-8sc-204368
sc-204368A
10 mg
50 mg
$673.00
$1479.00
2
(0)

UBP1112 acts as a selective modulator of the mGluR-6 receptor, showcasing distinct binding dynamics that influence receptor functionality. Its unique molecular architecture facilitates targeted interactions with critical binding sites, leading to alterations in receptor signaling pathways. This compound exhibits a nuanced effect on receptor kinetics, promoting specific conformational changes that can enhance or inhibit downstream signaling events, thereby impacting cellular responses and synaptic behavior.

MTPG

169209-66-9sc-204106
sc-204106A
5 mg
50 mg
$119.00
$709.00
(0)

MTPG serves as a selective modulator of the mGluR-6 receptor, characterized by its ability to engage in specific allosteric interactions that fine-tune receptor activity. Its structural features enable it to stabilize particular receptor conformations, influencing the dynamics of signal transduction. This compound demonstrates unique reaction kinetics, allowing for rapid modulation of receptor responses, which can lead to differential activation of intracellular pathways and affect synaptic transmission.

(RS)-MSPG

169209-64-7sc-203247
sc-203247A
5 mg
10 mg
$48.00
$201.00
(0)

(RS)-MSPG acts as a selective modulator of the mGluR-6 receptor, exhibiting unique binding affinities that facilitate distinct conformational changes. Its molecular structure promotes specific interactions with receptor sites, enhancing or inhibiting downstream signaling cascades. The compound's kinetic profile allows for nuanced regulation of receptor activity, impacting neurotransmitter release and synaptic plasticity, thereby influencing neuronal communication in a targeted manner.

Fenobam

57653-26-6sc-202608
sc-202608A
5 mg
25 mg
$84.00
$300.00
(0)

Fenobam, another mGluR5 antagonist, could influence mGluR-6 expression by altering the signaling pathways shared among metabotropic glutamate receptors in the central nervous system.

Topiramate

97240-79-4sc-204350
sc-204350A
10 mg
50 mg
$105.00
$362.00
(1)

Topiramate, a compound with multiple actions including modulation of glutamate receptors, might affect mGluR-6 expression indirectly through its broad effects on glutamatergic signaling.

Memantine hydrochloride

41100-52-1sc-203628
50 mg
$68.00
4
(2)

Memantine, another NMDA receptor antagonist, might have indirect effects on mGluR-6 expression by modulating glutamatergic neurotransmission and receptor homeostasis in the nervous system.

Gabapentin

60142-96-3sc-201481
sc-201481A
sc-201481B
20 mg
100 mg
1 g
$52.00
$92.00
$132.00
7
(1)

Gabapentin, which modulates GABAergic signaling, could theoretically affect mGluR-6 expression by influencing the overall balance of excitatory and inhibitory neurotransmission in the retina.