A competitive mGluR1 antagonist (Ki = 298 μM; IC50 = 1 mM for rat mGluR1α when challenged with glutamate); at concentrations from 10-300 μM

DL-AP3 – 100 mg

Brand:
Cayman
CAS:
5652-28-8
Storage:
-20
UN-No:
Non-Hazardous - /

Metabotropic glutamate receptors (mGluR1-8) are G protein-coupled receptors that function to modulate brain excitatory signaling via presynaptic, postsynaptic, and glial mechanisms.{21634} DL-AP3 is a competitive mGluR1 antagonist that demonstrates a Ki value of 298 μM and an IC50 value of 1mM for rat mGluR1α when challenged with glutamate.{21635} DL-AP3 can antagonize excitatory amino acid-induced phosphoinositide hydrolysis, induce Ca2+ mobilization in rat hippocampal slices, and inhibit phosphoserine phosphatase in rat brain cortex.{21634,21632} At concentrations from 10-300 μM DL-AP3 has been used to characterize the role of mGluR in long-term potentiation in the hippocampus in a model of learning and memory, the release of glutamate in Parkinson’s disease, and the increased activity of mGluR implicated in fragile X syndrome.{21633,21631,21630}  

 

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Description

A competitive mGluR1 antagonist (Ki = 298 μM; IC50 = 1 mM for rat mGluR1α when challenged with glutamate); at concentrations from 10-300 μM, used to characterize the role of mGluR in LTP in the hippocampus in a model of learning and memory, the release of glutamate in Parkinson’s disease, and the activity of mGluR implicated in fragile X syndrome

Formal name: 3-phosphono-alanine

Synonyms:  DL-2-Amino-3-Phosphonopropionic Acid|NSC 30078

Molecular weight: 169.1

CAS: 5652-28-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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