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

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.

journal_name

Bioorg Med Chem Lett

authors

Zhao Z,Wisnoski DD,O'Brien JA,Lemaire W,Williams DL Jr,Jacobson MA,Wittman M,Ha SN,Schaffhauser H,Sur C,Pettibone DJ,Duggan ME,Conn PJ,Hartman GD,Lindsley CW

doi

10.1016/j.bmcl.2006.11.081

subject

Has Abstract

pub_date

2007-03-01 00:00:00

pages

1386-91

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)01382-5

journal_volume

17

pub_type

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