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445865

mGluR5 Ligand, CDPPB

Name: mGluR5 Ligand, CDPPB
Brand: MM

A pyrazole amide compound that crosses the blood-brain barrier and acts as a potent, selective, reversible, positive allosteric modulator for metabotropic glutamate receptor subtype 5 (mGluR5).

Synonym(s):

mGluR5 Ligand, CDPPB, 3- Cyano-N-(1,3- di phenyl-1H- pyrazol-5-yl) benzamide, 3-Cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

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About This Item

Empirical Formula (Hill Notation):

C₂₃H₁₆N₄O

CAS Number:

781652-57-1

Molecular Weight:

364.40

UNSPSC Code:

12352200

Quality Level

100

Assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C23H16N4O/c24-16-17-8-7-11-19(14-17)23(28)25-22-15-21(18-9-3-1-4-10-18)26-27(22)20-12-5-2-6-13-20/h1-15H,(H,25,28)

InChI key

BKUIZWILNWHFHD-UHFFFAOYSA-N

General description

A pyrazole amide compound that crosses the blood-brain barrier and acts as a potent, selective, reversible, positive allosteric modulator for metabotropic glutamate receptor subtype 5 (mGluR5). Also exerts anti-psychotic-like effects. Reported to potentiate the response to glutamate (~300 nM) in CHO-mGluR5 cells (EC₅₀ = 10 nM for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation) and reverse amphetamine-induced disruption of pre-pulse inhibition (PPI) in rats. Specificity was determined using a panel of kinases and receptors. Does not potentiate the activity of other glutamate receptors.

Biochem/physiol Actions

Cell permeable: no

EC50 = 10 nM in potentiating the response to glutamate (~300 nM) in CHO-mGluR5 cells for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation

Primary Target
Metabotropic glutamate receptor subtype 5 (mGluR5)

Product does not compete with ATP.

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Kinney, G.G., et al. 2005. J. Pharmacol. Exp. Ther.313, 199.
Lindsley, C.W., et al. 2004. J. Med. Chem.47, 5825.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)