Date published: 2025-10-9

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mGluR-5 Inhibitors

The array of mGluR-5 inhibitors encompasses a sophisticated cadre of compounds meticulously designed to intricately modulate the activation of metabotropic glutamate receptor 5 (mGluR-5). These compounds, exemplified by MTEP, Fenobam, and MPEP, function as negative allosteric modulators, finely tuning the receptor's responsiveness to glutamate and subsequently interfering with downstream signaling pathways. MTEP, for instance, is a potent antagonist that disrupts the receptor's response to glutamate, showcasing the precision with which these inhibitors can be tailored to regulate mGluR-5 activity. Further expanding the toolkit are competitive antagonists like BAY 36-7620, selective inhibitors such as Mavoglurant, and positive allosteric modulators like CTEP and VU0361737. These compounds not only inhibit mGluR-5 but also bring a nuanced layer of modulation, influencing the receptor's intricate signaling dynamics. Mavoglurant, for instance, serves as a selective antagonist, offering researchers a specific tool to dissect mGluR-5 function in various cellular contexts. Positive allosteric modulators like CTEP and VU0361737, on the other hand, showcase the complexity of mGluR-5 modulation by enhancing receptor activity in a unique manner. The diverse chemical mechanisms exhibited by these inhibitors enable researchers to investigate the detailed regulatory processes that govern mGluR-5 activation. Whether through competitive inhibition or allosteric modulation, these compounds provide invaluable insights into the specific pathways influenced by mGluR-5 inhibition. This class of inhibitors thus stands as a testament to the meticulous design and understanding required for precise modulation of glutamatergic signaling. In summary, the inhibitors of mGluR-5 present a sophisticated repertoire of compounds, each with a unique mode of action, allowing researchers to precisely manipulate the receptor's activity. This nuanced toolkit not only contributes to the detailed understanding of mGluR-5 but also broadens our comprehension of the intricate signaling networks that govern cellular processes influenced by glutamate receptors.

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

MTEP hydrochloride

1186195-60-7sc-361267
sc-361267A
5 mg
25 mg
$117.00
$469.00
(0)

MTEP hydrochloride is a selective antagonist of the mGluR5 receptor, known for its ability to disrupt specific protein-protein interactions within the receptor complex. Its unique binding affinity is attributed to hydrophobic interactions and hydrogen bonding, which stabilize the ligand-receptor complex. This compound also exhibits notable kinetic properties, influencing the rate of receptor desensitization and internalization, thereby modulating synaptic signaling pathways with precision.

MPEP hydrochloride

96206-92-7sc-279454A
sc-279454
10 mg
50 mg
$133.00
$510.00
(0)

MPEP hydrochloride acts as a selective antagonist of the mGluR5 receptor, characterized by its unique ability to alter conformational dynamics within the receptor. Its binding involves intricate electrostatic interactions and van der Waals forces, which enhance specificity. Additionally, MPEP hydrochloride influences downstream signaling cascades, affecting calcium ion flux and second messenger systems, thereby providing a nuanced modulation of neuronal excitability and synaptic plasticity.

E4CPG

170846-89-6sc-205943
sc-205943A
10 mg
50 mg
$129.00
$548.00
(0)

E4CPG serves as a selective modulator of the mGluR-5 receptor, distinguished by its capacity to stabilize specific receptor conformations. Its binding mechanism is marked by unique hydrogen bonding and hydrophobic interactions, which fine-tune receptor activity. E4CPG also impacts intracellular signaling pathways, particularly those involving phosphoinositide turnover, leading to alterations in neurotransmitter release and synaptic strength, thereby influencing neural circuit dynamics.

(RS)-MCPG disodium salt

1303994-09-3sc-358840
10 mg
$160.00
(0)

(RS)-MCPG disodium salt acts as a selective antagonist of the mGluR-5 receptor, characterized by its ability to disrupt receptor dimerization and alter downstream signaling cascades. Its interaction profile includes specific ionic and hydrophobic contacts that modulate receptor affinity and efficacy. This compound also influences calcium ion flux and second messenger systems, contributing to the regulation of synaptic plasticity and neuronal excitability.

MTEP

329205-68-7sc-205956
sc-205956A
5 mg
25 mg
$86.00
$341.00
(0)

MTEP is a selective antagonist of the mGluR-5 receptor, known for its unique ability to stabilize the inactive conformation of the receptor. This stabilization alters the receptor's interaction with G-proteins, effectively modulating intracellular signaling pathways. MTEP exhibits distinct binding kinetics, characterized by a slow dissociation rate, which enhances its duration of action. Additionally, it influences receptor phosphorylation states, impacting cellular responses and synaptic dynamics.

ACDPP hydrochloride

37804-11-8sc-203494
sc-203494A
10 mg
50 mg
$163.00
$648.00
(0)

ACDPP hydrochloride acts as a potent modulator of the mGluR-5 receptor, exhibiting a unique binding affinity that promotes receptor desensitization. Its interaction with the receptor alters conformational dynamics, influencing downstream signaling cascades. The compound demonstrates rapid kinetics in receptor engagement, facilitating transient signaling events. Furthermore, ACDPP hydrochloride can impact calcium ion flux, thereby affecting neuronal excitability and synaptic plasticity.

DMEOB

40252-74-2sc-203569
sc-203569A
10 mg
50 mg
$75.00
$290.00
(0)

DMEOB serves as a selective modulator of the mGluR-5 receptor, characterized by its ability to stabilize specific receptor conformations. This compound engages in unique hydrogen bonding interactions that enhance receptor affinity, leading to altered signaling pathways. DMEOB exhibits distinct reaction kinetics, allowing for a nuanced modulation of intracellular calcium levels. Its influence on receptor dynamics can significantly affect synaptic transmission and neuronal network activity.

(S)-3-Carboxy-4-hydroxyphenylglycine

55136-48-6sc-203689
sc-203689A
10 mg
50 mg
$352.00
$1479.00
(0)

(S)-3-Carboxy-4-hydroxyphenylglycine acts as a selective antagonist of the mGluR-5 receptor, exhibiting a unique ability to disrupt receptor dimerization. This compound engages in specific electrostatic interactions that modulate receptor activation, influencing downstream signaling cascades. Its kinetic profile reveals a rapid binding affinity, allowing for transient modulation of glutamatergic neurotransmission, which can lead to significant alterations in synaptic plasticity and neuronal excitability.

Fenobam

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

Fenobam is a selective antagonist of the mGluR-5 receptor, characterized by its unique ability to stabilize the inactive conformation of the receptor. This compound exhibits distinct hydrophobic interactions that hinder receptor activation, effectively altering the conformational dynamics of mGluR-5. Its binding kinetics suggest a moderate affinity, enabling it to fine-tune glutamatergic signaling pathways, thereby impacting synaptic function and neuronal communication.

(RS)-MCPG

146669-29-6sc-202325
5 mg
$134.00
(0)

(RS)-MCPG acts as a competitive antagonist at the mGluR-5 receptor, exhibiting a unique binding profile that disrupts glutamate-mediated signaling. Its structural conformation allows for specific hydrogen bonding and hydrophobic interactions, which modulate receptor activity. The compound's kinetics reveal a rapid association and dissociation rate, influencing downstream signaling cascades. This dynamic behavior highlights its role in regulating synaptic plasticity and neurotransmitter release.