dhpg

(RS)-3,5-DHPG is an mGluR1/5 agonist (EC50 = 60 nM for mGluR1) that activates the phospholipase C (PLC) pathway, thereby activating protein kinase C (PKC).

DHPG ((RS)-3,5-DHPG) is an effective antagonist of mGluR linked to phospholipase D. As an amino acid, it serves as a selective and potent agonist for Group I mGluR (mGluR 1 and mGluR 5) without affecting Group II or Group III mGluRs.

(S)-3,5-DHPG is a weak but selective agonist of group I metabotropic glutamate receptors with Ki values of 0.9 μM for mGluR1a and 3.9 μM for mGluR5a. (S)-3,5-DHPG demonstrates anxiolytic activity in hypoxia-exposed rats, supporting its application in neuropharmacological studies of glutamatergic signaling, stress responses, and anxiety-related behaviors.

LY456236 free base is a selective, non-competitive, orally active antagonist of the glutamate receptor 1 (mGlu1), effectively inhibiting phosphoinositide hydrolysis with an IC50 of 0.145 μM. Additionally, it inhibits EGFR with an IC50 of 0.918 μM. By suppressing the MAPK pathway, LY456236 free base blocks cell proliferation and counters the anti-apoptotic effects of DHPG. This compound is useful for seizure research.

ACDPP is a specific antagonist of metabotropic glutamate receptor 5 (mGluR5) that partially blocks the DHPG-induced increase of fragile X mental retardation protein (FMRP), ACDPP is used as a pharmacological tool in neuroscience research to study group I mGluR signaling, synaptic plasticity, and molecular mechanisms underlying fragile X syndrome.

Ro 67-4853 is a selective mGluR1 positive allosteric modulator, enhancing the response to the agonist (S)-3,5-dihydroxyphenylglycine (DHPG) in anesthetized rats through iontophoretic administration.

Peptide neurotoxin; selectively and reversibly blocks N-type calcium channels (IC50 = 0.15 nM). Reduces (RS)-3,5-DHPG -induced long term depression in vivo.