Molecular structure of mGluR5 Ligand, CDPPB, CAS Number: 781652-57-1
mGluR5 Ligand, CDPPB (CAS 781652-57-1)
Alternate Names:
3-Cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide
Application:
mGluR5 Ligand, CDPPB is a selective, reversible, positive allosteric modulator for mGluR-5
CAS Number:
781652-57-1
Molecular Weight:
364.4
Molecular Formula:
C23H16N4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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). This also exerts anti-psychotic-like effects. It is 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. The specificity was determined using a panel of kinases and receptors. It does not potentiate the activity of other glutamate receptors.
mGluR5 Ligand, CDPPB (CAS 781652-57-1) References
- 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. | Lindsley, CW., et al. 2004. J Med Chem. 47: 5825-8. PMID: 15537338
- A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. | Kinney, GG., et al. 2005. J Pharmacol Exp Ther. 313: 199-206. PMID: 15608073
- Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. | de Paulis, T., et al. 2006. J Med Chem. 49: 3332-44. PMID: 16722652
- Positive allosteric modulation of metabotropic glutamate 5 (mGlu5) receptors reverses N-Methyl-D-aspartate antagonist-induced alteration of neuronal firing in prefrontal cortex. | Lecourtier, L., et al. 2007. Biol Psychiatry. 62: 739-46. PMID: 17511968
- Positive allosteric modulation of mGluR5 receptors facilitates extinction of a cocaine contextual memory. | Gass, JT. and Olive, MF. 2009. Biol Psychiatry. 65: 717-20. PMID: 19100966
- Activation of type 5 metabotropic glutamate receptors attenuates deficits in cognitive flexibility induced by NMDA receptor blockade. | Stefani, MR. and Moghaddam, B. 2010. Eur J Pharmacol. 639: 26-32. PMID: 20371234
- Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5. | Zou, MF., et al. 2011. Bioorg Med Chem Lett. 21: 2650-4. PMID: 21295978
- mGluR5 positive allosteric modulation enhances extinction learning following cocaine self-administration. | Cleva, RM., et al. 2011. Behav Neurosci. 125: 10-9. PMID: 21319882
- Importance of Shank3 protein in regulating metabotropic glutamate receptor 5 (mGluR5) expression and signaling at synapses. | Verpelli, C., et al. 2011. J Biol Chem. 286: 34839-50. PMID: 21795692
- Therapeutic effects of metabotropic glutamate receptor 5 positive allosteric modulator CDPPB on phencyclidine-induced cognitive deficits in mice. | Horio, M., et al. 2013. Fundam Clin Pharmacol. 27: 483-8. PMID: 22594375
- Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGluR5) attenuate microglial activation. | Xue, F., et al. 2014. CNS Neurol Disord Drug Targets. 13: 558-66. PMID: 24168364
- Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine. | Kufahl, PR., et al. 2013. F1000Res. 2: 84. PMID: 24358885
- Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias. | Arsova, A., et al. 2021. Mol Pharmacol. 99: 328-341. PMID: 33602724
- Binding of a positive allosteric modulator CDPPB to metabotropic glutamate receptor type 5 (mGluR5) probed by all-atom molecular dynamics simulations. | Uba, AI., et al. 2022. Life Sci. 309: 121014. PMID: 36179814
Activator of:
mGluR-5.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
mGluR5 Ligand, CDPPB, 1 mg | sc-221942 | 1 mg | $64.00 | |||
mGluR5 Ligand, CDPPB, 5 mg | sc-221942A | 5 mg | $93.00 |