Description: Positive allosteric modulator at mGlu5
Chemical Name: 3-Cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Brain penetrant, selective positive allosteric modulator at the mGlu5 receptor (EC50 values are 10 and 20 nM for human and rat receptors respectively). Antipsychotic; reverses amphetamine-induced locomotor activity and amphetamine-induced deficits in prepulse inhibition in rats.
Licensing Information
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Compound Libraries
CDPPB is also offered as part of the
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
27.33
75
Preparing Stock Solutions
The following data is based on the product molecular weight 364.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.74 mL
13.72 mL
27.44 mL
5 mM
0.55 mL
2.74 mL
5.49 mL
10 mM
0.27 mL
1.37 mL
2.74 mL
50 mM
0.05 mL
0.27 mL
0.55 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Lindsleyet al (2004) Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J.Med.Chem. 47 5825 PMID: 15537338
Kinneyet al (2005) A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rats behavioral models. J.Pharmacol.Exp.Ther. 313 199 PMID: 15608073
Chenet al (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol.Pharmacol. 71 1389 PMID: 17303702
Keywords: CDPPB, supplier, Positive, allosteric, modulators, mGlu5, mGluR5, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience