Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA

descriptionPublicationkeyboard_double_arrow_right Article 01 Mar 2007 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 17, pages 1,386-1,391 (issn: 0960-894X,

Copyright policy )

Authors: Zhijian, Zhao; David D, Wisnoski; Julie A, O'Brien; Wei, Lemaire; David L, Williams; Marlene A, Jacobson; Marion, Wittman; +8 Authors

doi: 10.1016/j.bmcl.2006.11.081

pmid: 17210250

Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA

- Summary
- Subjects
- Metrics

Abstract

This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs, CPPHA has been the focus of numerous pharmacology studies by several laboratories.

Related Organizations

Vanderbilt University Medical Center
United States
Merck & Co.
United States

Keywords

Receptor, Metabotropic Glutamate 5, Phthalimides, Receptors, Metabotropic Glutamate, Rats, Structure-Activity Relationship, Allosteric Regulation, Benzamides, Animals, Humans, Allosteric Site

Impact byBIP!

	selected citations These citations are derived from selected sources. This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	81
	popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.	Top 10%
	influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	Top 10%
	impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.	Top 1%