Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5)

Stefan Tasler; Jürgen Kraus; Stefano Pegoraro; Andrea Aschenbrenner; Elena Poggesi; Rodolfo Testa; Gianni Motta; Amedeo Leonardi

doi:10.1016/j.bmcl.2005.03.089

Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5)

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2876-80. doi: 10.1016/j.bmcl.2005.03.089.

Authors

Stefan Tasler¹, Jürgen Kraus, Stefano Pegoraro, Andrea Aschenbrenner, Elena Poggesi, Rodolfo Testa, Gianni Motta, Amedeo Leonardi

Affiliation

¹ 4SC AG, Martinsried, Germany. [email protected]

PMID: 15878659
DOI: 10.1016/j.bmcl.2005.03.089

Abstract

Based on a pharmacophore alignment on known non-competitive mGluR5 inhibitors applying 4SCan technology, a new lead series was identified and further structurally investigated. K(i)'s as low as around 100 nM were achieved.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Excitatory Amino Acid Antagonists / chemistry
Excitatory Amino Acid Antagonists / pharmacology*
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Excitatory Amino Acid Antagonists
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate