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HomeProduct name listVU 0360223

VU 0360223

VU 0360223 Structural

What is VU 0360223?

Description

Glutamate, the major excitatory neurotransmitter in the central nervous system, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors (mGlus) discovered thus far, development of inhibitors to mGlu5 has been given significant attention in preclinical models of disease, including pain, anxiety, gastresophageal reflux disease, Parkinson’s associated dyskinesia, and fragile X syndrome, as well as in animal models of drug addiction. VU0360223 is a noncompetitive antagonist (negative allosteric modulator) of mGlu5 that demonstrates an IC50 value of 61 nM in a calcium mobilization assay and a Ki value of 477 nM in a radioligand binding assay. A 10 μM concentration of VU0360223 results in a near complete blockade of the glutamate response in cortical astrocytes. A 30 mg/kg dose of VU0360223 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.

The Uses of VU 0360223

VU 0360223 is a noncompetitive antagonist (negative allosteric modulator) of mGlu5 for use in drug addiction treatment.

storage

Room temperature

Properties of VU 0360223

Boiling point: 434.9±35.0 °C(Predicted)
Density  1.35±0.1 g/cm3(Predicted)
storage temp.  Store at RT
solubility  Soluble to 25 mM in DMSO
form  Powder
pka 1.10±0.10(Predicted)

Safety information for VU 0360223

Computed Descriptors for VU 0360223

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