Date published: 2026-5-6

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mGluR-5 Activators

The assemblage of chemicals outlined in the tabulated form represents a comprehensive compilation of both direct and indirect activators of mGluR-5, a pivotal receptor involved in modulating cellular responses to glutamate. These compounds, meticulously selected for their distinct mechanisms of action, collectively serve as indispensable tools for investigating the intricate regulatory networks governing mGluR-5 activation. Direct activators, such as CDPPB, VU0360172, DFB, CHPG, L-SOP, and Ro67-7476, directly engage with mGluR-5, acting as positive allosteric modulators that enhance the receptor's sensitivity to glutamate. This direct interaction promotes robust receptor activation, initiating downstream signaling cascades and modulating cellular responses. On the other hand, negative allosteric modulators, including MPEP, Fenobam, Basimglurant, and MTEP, exert inhibitory effects on mGluR-5 activation. These chemicals attenuate the receptor's response to glutamate, providing a means to precisely regulate mGluR-5 activity. The nuanced interplay of these chemicals unveils the intricate landscape of mGluR-5 activation, shedding light on the multifaceted signaling pathways associated with this receptor. Whether acting as positive or negative modulators, each compound plays a pivotal role in elucidating the regulatory mechanisms dictating mGluR-5 function. Researchers leveraging this diverse toolkit gain unprecedented insights into the specific biochemical and cellular pathways influenced by these chemicals, providing a foundation for understanding mGluR-5's role in diverse physiological contexts. In conclusion, the elucidation of mGluR-5 activators transcends conventional pharmacological exploration. This comprehensive array of chemicals not only serves as invaluable probes for investigating mGluR-5 activation but also contributes to the broader understanding of glutamatergic signaling and its implications in cellular processes. The intricate details of these compounds' actions on mGluR-5 provide a nuanced perspective, offering researchers a sophisticated toolkit to unravel the complexities of this essential receptor in diverse physiological and pathological scenarios.

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Items 11 to 17 of 17 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

cis-ACPD

39026-63-6sc-202102
5 mg
$60.00
(0)

Cis-ACPD acts as a potent agonist for mGluR5, uniquely engaging the receptor to initiate intracellular signaling pathways. Its structural conformation allows for effective binding to the receptor's orthosteric site, leading to enhanced activation of phospholipase C and subsequent inositol trisphosphate production. This compound's ability to modulate calcium release from intracellular stores plays a crucial role in synaptic transmission and neuronal communication, influencing various neurophysiological processes.

(S)-4C3H-PG

85148-82-9sc-203249
sc-203249A
1 mg
5 mg
$30.00
$123.00
(0)

(S)-4C3H-PG selectively targets mGluR5, exhibiting a unique binding affinity that stabilizes the receptor in an active conformation. This interaction promotes downstream signaling cascades, particularly enhancing the activation of protein kinase pathways. Its distinct stereochemistry facilitates specific molecular interactions, influencing receptor dimerization and altering synaptic plasticity. The compound's kinetic profile suggests rapid receptor engagement, contributing to its dynamic role in cellular signaling networks.

trans-(1S,3R)-ACPD

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

Trans-(1S,3R)-ACPD is a potent mGluR5 agonist that uniquely modulates receptor activity through its stereospecific interactions. This compound enhances intracellular calcium mobilization, triggering a cascade of signaling events that influence neuronal excitability. Its ability to stabilize receptor conformations allows for prolonged signaling, while its distinct molecular structure promotes selective receptor interactions, impacting synaptic transmission and plasticity. The compound's rapid kinetics enable swift modulation of cellular responses, underscoring its role in neurophysiological processes.

VU 0357121

433967-28-3sc-364645
sc-364645A
10 mg
50 mg
$145.00
$615.00
(0)

VU 0357121 is a selective mGluR5 antagonist that exhibits unique binding characteristics, disrupting receptor-mediated signaling pathways. Its distinct molecular architecture allows for high affinity interactions with the allosteric site, leading to altered receptor conformations. This modulation results in decreased intracellular calcium levels and influences downstream signaling cascades. The compound's rapid dissociation kinetics facilitate dynamic regulation of synaptic activity, highlighting its role in neuronal communication.

DPAP

890764-36-0sc-364741
sc-364741A
1 mg
5 mg
$64.00
$99.00
(0)

DPAP acts as a selective modulator of mGluR5, showcasing a unique ability to stabilize receptor conformations through specific hydrogen bonding and hydrophobic interactions. Its distinct structural features enable it to engage with the receptor's allosteric site, influencing ligand binding dynamics. This interaction alters the receptor's signaling profile, impacting intracellular pathways and calcium flux. The compound's kinetic properties allow for precise temporal control over receptor activity, underscoring its role in synaptic modulation.

Fenobam

57653-26-6sc-202608
sc-202608A
5 mg
25 mg
$86.00
$306.00
(0)

Fenobam is a negative allosteric modulator of mGluR-5, exerting inhibitory effects on the receptor's response to glutamate, thereby modulating its activation.

(±)-1-Aminocyclopentanl-trans-1,3-Dicarboxylic acid

67684-64-4sc-287072
sc-287072A
sc-287072B
1 mg
5 mg
10 mg
$35.00
$103.00
$187.00
(0)

(+/-)-1-Aminocyclopentanl-trans-1,3-Dicarboxylic acid exhibits intriguing properties as a modulator of mGluR5, characterized by its capacity to form intricate electrostatic interactions with the receptor. Its unique stereochemistry facilitates selective binding, enhancing receptor activation and influencing downstream signaling cascades. The compound's dynamic conformational flexibility allows it to adapt to various binding states, thereby fine-tuning the receptor's functional responses and impacting synaptic plasticity.