Date published: 2025-10-15

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mGluR-2 Inhibitors

The metabotropic glutamate receptor 2 (mGluR2) is a G-protein coupled receptor (GPCR) that plays a crucial role in the modulation of neurotransmission and synaptic plasticity in the central nervous system (CNS). It is primarily involved in the regulation of glutamate, the most abundant excitatory neurotransmitter in the mammalian brain. Activation of mGluR2 by glutamate leads to a decrease in neuronal excitability and neurotransmitter release, serving as a critical feedback mechanism that prevents excessive neuronal firing and excitotoxicity. This receptor is distributed in various brain regions, including areas involved in cognition, perception, and mood regulation, thereby participating in a wide array of physiological processes. The functional significance of mGluR2 extends to its involvement in synaptic plasticity, learning, memory, and the regulation of anxiety and depressive behaviors, making it a pivotal element in the maintenance of CNS homeostasis. The inhibition of mGluR2 involves mechanisms that either prevent the binding of glutamate to the receptor or disrupt its ability to activate the associated G-proteins, leading to a reduction in its regulatory functions. This can be achieved through the interaction with specific sites on the receptor that are critical for its activation, such as the glutamate binding domain or the G-protein interaction interfaces. Inhibition can also occur via allosteric modulation, where compounds bind to sites distinct from the glutamate binding site, inducing conformational changes that reduce receptor activity. Additionally, post-translational modifications, such as phosphorylation, can modulate the receptor's responsiveness to glutamate or its interaction with intracellular signaling proteins. These inhibitory mechanisms contribute to the fine-tuning of glutamatergic signaling, affecting synaptic transmission and plasticity.

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Items 1 to 10 of 19 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

LY 341495

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

LY 341495 is a selective antagonist of mGluR-2, characterized by its ability to disrupt the receptor's conformational state through specific hydrophobic interactions. This compound exhibits rapid binding kinetics, leading to immediate inhibition of receptor activity. Its unique structural features enable it to selectively influence intracellular signaling cascades, modulating calcium ion flux and impacting neurotransmitter release dynamics, thereby affecting synaptic communication.

(RS)-CPPG

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

(RS)-CPPG acts as a potent mGluR-2 agonist, engaging the receptor through distinct electrostatic interactions that stabilize its active conformation. This compound demonstrates a unique ability to enhance receptor-mediated signaling pathways, promoting downstream effects on neuronal excitability. Its selective binding affinity allows for precise modulation of synaptic plasticity, influencing glutamate release and receptor desensitization, thereby shaping neural network dynamics.

E4CPG

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

E4CPG functions as a selective mGluR-2 agonist, characterized by its unique ability to form hydrogen bonds with key amino acid residues in the receptor's binding pocket. This interaction facilitates a conformational shift that enhances receptor activation. E4CPG exhibits distinct kinetic properties, allowing for rapid onset and prolonged engagement with the receptor, which influences intracellular calcium signaling and modulates synaptic transmission efficiency. Its specificity contributes to nuanced regulatory effects on neuronal circuits.

(RS)-MCPG disodium salt

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

(RS)-MCPG disodium salt acts as a selective mGluR-2 antagonist, distinguished by its capacity to disrupt the receptor's signaling pathways. It engages in specific electrostatic interactions with charged residues, leading to a stabilization of the inactive receptor conformation. This compound exhibits unique binding kinetics, characterized by a slow dissociation rate, which prolongs its inhibitory effects on downstream signaling cascades, ultimately influencing neurotransmitter release dynamics.

MPEP hydrochloride

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

Primarily an mGluR5 antagonist, but it can also influence other pathways that may affect mGluR-2 function indirectly.

(RS)-MCPG

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

(RS)-MCPG functions as a selective antagonist for mGluR-2, exhibiting unique molecular interactions that modulate receptor activity. Its binding affinity is influenced by hydrophobic contacts and hydrogen bonding with key amino acid residues, which alters receptor conformational states. The compound's distinct reaction kinetics reveal a prolonged engagement with the receptor, effectively modulating intracellular calcium levels and impacting synaptic plasticity through altered signaling pathways.

(S)-MCPG

150145-89-4sc-202329
sc-202329A
5 mg
25 mg
$143.00
$945.00
(0)

(S)-MCPG acts as a selective antagonist for mGluR-2, showcasing unique binding dynamics that influence receptor conformation. Its interactions involve specific electrostatic and hydrophobic forces, leading to a distinct modulation of downstream signaling cascades. The compound's kinetic profile indicates a slow dissociation rate from the receptor, which may enhance its regulatory effects on neurotransmitter release and synaptic transmission, contributing to nuanced cellular responses.

Ro 64-5229

246852-46-0sc-361308
sc-361308A
10 mg
50 mg
$350.00
$1575.00
(0)

Ro 64-5229 is a selective mGluR-2 modulator that exhibits unique allosteric properties, enhancing receptor activity through specific conformational changes. Its binding involves intricate hydrogen bonding and hydrophobic interactions, which stabilize the receptor in an active state. The compound demonstrates a rapid onset of action, influencing intracellular calcium signaling and gene expression pathways, thereby affecting neuronal excitability and synaptic plasticity in a distinctive manner.

L(+)-2-Amino-4-phosphonobutanoic acid (L-AP4)

23052-81-5sc-200432
5 mg
$92.00
1
(1)

It is an agonist for group III mGluRs, but its activity can indirectly influence mGluR-2.

LY 341495 disodium salt

sc-362765
sc-362765A
1 mg
10 mg
$112.00
$177.00
(0)

LY 341495 disodium salt acts as a selective modulator of mGluR-2, exhibiting unique binding dynamics that promote receptor desensitization. Its interaction profile includes specific electrostatic and van der Waals forces, which facilitate a nuanced alteration in receptor conformation. This compound influences downstream signaling cascades, particularly those involving phosphoinositide turnover, thereby modulating synaptic transmission and neuronal network activity with distinct kinetics.