Issue 11, 2011

A highly selective agonist for the metabotropic glutamate receptor mGluR2

Abstract

The three conformationally restricted cyclopropyl glutamate analogues (3, 4, 5) were synthesised and their affinity for ionotropic and activity at metabotropic glutamate receptors were probed. Compound 4 turned out to be a highly selective agonist at the metabotropic glutamate receptor mGluR2 with at least two orders of magnitude selectivity in potency compared to the very homologous mGluR3 as well as mGluR1, 4, 5, 7. We also tried to synthesise the two epimers of 6, but the two compounds underwent fast epimerisation in H2O. Furthermore, two cyclopropyl arginine analogues (7, 8) were synthesised and characterised pharmacologically at GPRC6A.

Graphical abstract: A highly selective agonist for the metabotropic glutamate receptor mGluR2

Supplementary files

Article information

Article type
Concise Article
Submitted
20 Jul 2011
Accepted
25 Aug 2011
First published
23 Sep 2011

Med. Chem. Commun., 2011,2, 1120-1124

A highly selective agonist for the metabotropic glutamate receptor mGluR2

S. D. Nielsen, M. Fulco, M. Serpi, B. Nielsen, M. B. Hansen, K. L. Hansen, C. Thomsen, R. Brodbeck, H. Bräuner-Osborne, R. Pellicciari, P. Norrby, J. R. Greenwood and R. P. Clausen, Med. Chem. Commun., 2011, 2, 1120 DOI: 10.1039/C1MD00186H

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements