Date published: 2026-4-9

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mGluR-2 Activators

The metabotropic glutamate receptor 2 (mGluR2) is an integral component of the glutamatergic system in the central nervous system (CNS), playing a pivotal role in modulating synaptic transmission and neuronal excitability. As a member of the group II metabotropic glutamate receptors, mGluR2 is primarily coupled to Gi/o proteins, which mediate inhibitory neurotransmission through the suppression of cyclic AMP (cAMP) production, inhibition of voltage-gated calcium channels, and activation of inward-rectifying potassium channels. This receptor modulates glutamate neurotransmission in a negative feedback manner, reducing the release of glutamate and other neurotransmitters, thus contributing to the fine-tuning of synaptic activity and preventing excitotoxicity. The distribution of mGluR2 across various brain regions, including the hippocampus, cortex, and cerebellum, underscores its significance in regulating cognitive functions, emotional responses, and sensory processing. Through its action, mGluR2 is implicated in a myriad of physiological processes, including learning, memory, anxiety regulation, and the maintenance of neural circuit homeostasis. Activation of mGluR2 occurs through the binding of glutamate or other agonists to the extracellular venus flytrap domain, triggering a conformational change that facilitates interaction with and activation of the associated G-proteins. The activation process is tightly regulated by the receptor's extracellular glutamate concentration, with specific agonists enhancing the receptor's sensitivity or efficacy. Additionally, the receptor's activity can be modulated by allosteric modulators, which bind to sites distinct from the glutamate binding domain, promoting receptor activation or enhancing its response to glutamate. Intracellularly, mGluR2 activation can be influenced by post-translational modifications, such as phosphorylation, which may affect receptor sensitivity, trafficking, and interaction with G-proteins or other signaling molecules. This intricate regulation of mGluR2 activation plays a crucial role in maintaining synaptic plasticity and CNS functionality, highlighting the receptor's importance in neural communication and its potential as a focal point for understanding the complex dynamics of neuronal signaling pathways.

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Items 11 to 18 of 18 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

trans-(1S,3R)-ACPD

111900-32-4sc-391145
5 mg
$197.00
(0)

Trans-(1S,3R)-ACPD is a potent allosteric modulator of mGluR-2, characterized by its ability to induce conformational changes that enhance receptor sensitivity to endogenous ligands. Its unique stereochemistry facilitates specific hydrogen bonding and hydrophobic interactions, promoting efficient signal transduction. The compound's kinetic profile reveals a fast association rate with the receptor, leading to pronounced effects on downstream signaling pathways, including alterations in cyclic AMP levels and phosphoinositide turnover.

cis-1,3-homo-ACPD

194785-82-5sc-205932
5 mg
$44.00
(0)

Cis-1,3-homo-ACPD acts as a selective agonist for mGluR-2, exhibiting unique binding dynamics that stabilize receptor conformations. Its distinct molecular structure allows for enhanced electrostatic interactions, which fine-tune receptor activation. The compound demonstrates a notable affinity for modulating intracellular calcium levels, influencing neuronal excitability. Additionally, its reaction kinetics suggest a slower dissociation rate, prolonging its functional impact on synaptic transmission.

trans-1,3-homo-ACPD

sc-205981
5 mg
$44.00
(0)

Trans-1,3-homo-ACPD serves as a selective agonist for mGluR-2, characterized by its unique stereochemistry that influences receptor binding affinity. This compound engages in specific hydrogen bonding interactions, promoting a stable receptor state that enhances downstream signaling pathways. Its kinetic profile indicates a prolonged engagement with the receptor, leading to sustained modulation of neurotransmitter release. The compound's distinct conformational flexibility may also facilitate diverse allosteric effects, impacting synaptic plasticity.

LY 487379 hydrochloride

353229-59-1sc-204065
sc-204065A
10 mg
50 mg
$145.00
$615.00
(0)

LY 487379 hydrochloride acts as a selective modulator of mGluR-2, exhibiting unique binding dynamics that enhance receptor activation. Its structural features allow for specific electrostatic interactions, which stabilize the receptor-ligand complex. The compound's rapid association and slower dissociation kinetics contribute to its prolonged effects on intracellular signaling cascades. Additionally, its ability to induce conformational changes in the receptor may influence downstream pathways, affecting neuronal excitability and synaptic function.

LY404039

635318-11-5sc-364524
sc-364524A
5 mg
25 mg
$112.00
$418.00
(0)

LY404039 is a selective allosteric modulator of mGluR-2, characterized by its unique ability to engage in specific hydrophobic interactions with the receptor's binding site. This compound demonstrates a distinct profile of receptor modulation, enhancing the efficacy of endogenous ligands. Its kinetic properties reveal a fast onset of action, coupled with a sustained receptor engagement, which may lead to nuanced alterations in signaling pathways. The compound's structural conformation allows for tailored interactions that can fine-tune neuronal signaling dynamics.

LY 395756

852679-66-4sc-359013
sc-359013A
10 mg
50 mg
$176.00
$982.00
(0)

(±)LY 395756 acts as a selective modulator of mGluR-2, exhibiting unique binding characteristics that facilitate specific electrostatic interactions within the receptor's allosteric site. This compound influences receptor dynamics by stabilizing particular conformational states, thereby altering downstream signaling cascades. Its reaction kinetics suggest a gradual modulation of receptor activity, allowing for prolonged engagement and subtle shifts in neurotransmitter release patterns. The compound's structural features enable it to selectively influence receptor behavior, contributing to its distinct pharmacological profile.

CBiPES hydrochloride

856702-40-4sc-358830
sc-358830A
10 mg
50 mg
$145.00
$645.00
(0)

CBiPES hydrochloride serves as a selective allosteric modulator of mGluR-2, characterized by its ability to engage in specific hydrogen bonding and hydrophobic interactions with the receptor. This compound enhances receptor stability, promoting unique conformational changes that fine-tune intracellular signaling pathways. Its kinetic profile indicates a slow onset of action, allowing for nuanced modulation of receptor activity and influencing synaptic transmission dynamics without abrupt alterations.

BINA

866823-73-6sc-361121
sc-361121A
10 mg
50 mg
$134.00
$756.00
1
(0)

BINA acts as a selective modulator of mGluR-2, distinguished by its capacity to form unique electrostatic interactions with the receptor's binding site. This compound facilitates a distinct allosteric effect, leading to altered receptor dynamics and enhanced signal transduction efficiency. Its reaction kinetics reveal a gradual engagement with the receptor, allowing for sustained modulation of downstream pathways, thereby influencing neuronal excitability and synaptic plasticity.