Date published: 2026-4-30

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mGLuR-8 Activators

Chemical activators of mGluR-8 include a variety of compounds that engage the receptor at either orthosteric or allosteric sites to initiate intracellular signaling pathways. DCG-IV, (S)-3,4-DCPG, and (S)-4C3HPG are examples of agonists that bind to the same site as glutamate, the natural ligand of mGluR-8, to activate the receptor. These compounds mimic the action of glutamate, causing a conformational change that results in receptor activation. Similarly, LY379268 and LY354740 act on group II metabotropic glutamate receptors and function as agonists for mGluR-8, stimulating its activity by promoting its natural signal transduction mechanisms. This activation triggers a cascade of intracellular events leading to the receptor's functional response. In addition to orthosteric agonists, several allosteric modulators play a role in mGluR-8 activation. Compounds like AMN082, Ro 67-7476, ADX88178, AZ12216052, and CPPHA bind to sites distinct from the glutamate binding site, enhancing the receptor's response to the presence of its ligand. These positive allosteric modulators do not activate mGluR-8 on their own but increase the receptor's sensitivity to glutamate, leading to a potentiated response. BAY36-7620, although a negative allosteric modulator, can paradoxically function as an agonist under specific conditions, further illustrating the complex regulation of mGluR-8 activation by chemical means. These chemicals, through their interaction with the mGluR-8, induce a series of biochemical changes within the cell that result in the receptor's activation and the promotion of its role in signal transduction.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

O-Phospho-L-serine

407-41-0sc-202257
1 g
$37.00
(1)

O-Phospho-L-serine acts as a modulator of mGluR-8, engaging in specific hydrogen bonding and electrostatic interactions that influence receptor activity. Its phosphorylated structure enhances binding affinity, promoting conformational changes that can either activate or inhibit signaling pathways. This compound's unique ability to interact with key residues within the receptor's binding pocket may alter downstream effects, thereby impacting synaptic transmission and neuronal communication.

Z-Cyclopentyl-AP4

103439-17-4sc-204413
sc-204413A
10 mg
50 mg
$169.00
$681.00
(0)

Z-Cyclopentyl-AP4 selectively targets mGluR-8, exhibiting unique stereochemical properties that facilitate its interaction with the receptor's allosteric site. Its cyclopentyl group enhances hydrophobic interactions, stabilizing the ligand-receptor complex. This compound's kinetic profile suggests rapid binding and dissociation rates, allowing for fine-tuning of receptor modulation. Additionally, its structural conformation may influence the receptor's downstream signaling cascades, affecting neuronal excitability and synaptic plasticity.

LY 341495

201943-63-7sc-361244
sc-361244A
1 mg
10 mg
$89.00
$223.00
1
(1)

A potent and selective group II metabotropic glutamate receptor antagonist that can functionally activate mGluR-8 when used in a paradoxical agonist-like mode at specific concentrations.

(S)-3,4-DCPG

201730-11-2sc-204255
sc-204255A
10 mg
50 mg
$202.00
$833.00
(0)

A potent and selective agonist at the mGluR-8, which can activate the receptor by binding to its orthosteric site, inducing a conformational change that triggers intracellular signaling cascades.

(S)-4C3H-PG

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

A selective agonist for group II mGluRs, including mGluR-8, which activates the receptor by binding to the same site as glutamate, mimicking its excitatory action on this G-protein-coupled receptor.

LY 379268

191471-52-0sc-361247
sc-361247A
10 mg
50 mg
$318.00
$1775.00
2
(0)

A selective group II metabotropic glutamate receptor agonist, which can activate mGluR-8 by simulating the natural neurotransmitter′s binding, initiating the receptor′s typical response.

LY 354740

176199-48-7sc-204064
sc-204064A
10 mg
50 mg
$266.00
$886.00
2
(1)

Acts as an agonist for group II metabotropic glutamate receptors, including mGluR-8, effectively activating the receptor by stimulating its natural signal transduction mechanisms.