DPAP (CAS 890764-36-0)
Alternate Names:
VU 29
Application:
DPAP is a potent, postive allosteric, potentiator at mGluR-5
CAS Number:
890764-36-0
Molecular Weight:
384.39
Molecular Formula:
C22H16N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Description
Safety Information
SDS & Certificate of Analysis
DPAP is a potent allosteric potentiator at the rat mGluR-5 (EC50 = 9 nM). DPAP binds to the MPEP (sc-279454) allosteric site (Ki app = 244 nM). This compound selects mGluR-5 over mGluR-1 and mGluR-2 (EC50 values are 557 nM and 1.51 μM for mGluR-1 and mGluR-2 respectively). DPAP potentiates both DHPG-induced LTP and TBS- induced LTP in rat hippocampal slices.
DPAP (CAS 890764-36-0) References
- Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. | Chen, Y., et al. 2007. Mol Pharmacol. 71: 1389-98. PMID: 17303702
- Recent developments of the PET imaging agents for metabotropic glutamate receptor subtype 5. | Yu, M. 2007. Curr Top Med Chem. 7: 1800-5. PMID: 17979788
- N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. | Chen, Y., et al. 2008. Mol Pharmacol. 73: 909-18. PMID: 18056795
- Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. | Noetzel, MJ., et al. 2012. Mol Pharmacol. 81: 120-33. PMID: 22021324
- The role of ventral and dorsal striatum mGluR5 in relapse to cocaine-seeking and extinction learning. | Knackstedt, LA., et al. 2014. Addict Biol. 19: 87-101. PMID: 23710649
- Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site. | Gregory, KJ., et al. 2014. ACS Chem Neurosci. 5: 282-95. PMID: 24528109
- Modulation of neuronal microcircuit activities within the medial prefrontal cortex by mGluR5 positive allosteric modulator. | Pollard, M., et al. 2014. J Psychopharmacol. 28: 935-46. PMID: 25031220
- Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Impairment of Novel Object Recognition Induced by Acute Ethanol and Ethanol Withdrawal in Rats. | Marszalek-Grabska, M., et al. 2018. Neurotox Res. 33: 607-620. PMID: 29294238
- Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding. | Butkiewicz, M., et al. 2019. ACS Chem Neurosci. 10: 3427-3436. PMID: 31132237
- mGlu5 Positive Allosteric Modulators Facilitate Long-Term Potentiation via Disinhibition Mediated by mGlu5-Endocannabinoid Signaling. | Xiang, Z., et al. 2019. ACS Pharmacol Transl Sci. 2: 198-209. PMID: 31259318
- Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism. | Sengmany, K., et al. 2020. Biochem Pharmacol. 177: 114011. PMID: 32380090
- Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site. | Hellyer, SD., et al. 2020. Biochem Pharmacol. 177: 114013. PMID: 32389635
- Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Maintenance Association between Environmental Cues and Rewarding Properties of Ethanol in Rats. | Marszalek-Grabska, M., et al. 2020. Biomolecules. 10: PMID: 32443872
Activator of:
mGluR-5.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
DPAP, 1 mg | sc-364741 | 1 mg | $64.00 | |||
DPAP, 5 mg | sc-364741A | 5 mg | $99.00 |