Co-operative binding assay for the characterization of mGlu4 allosteric modulators.

Abstract:

:The interest in the role of metabotropic glutamate receptor 4 (mGlu4) in CNS related disorders has increased the need for methods to investigate the binding of allosteric drug candidates. Our aim is to present the first fully characterized in vitro binding assay of mGlu4 positive allosteric modulators (PAMs). Results suggest that mGlu4 PAMs have characteristic co-operative binding with orthosteric glutamate, which offers a notable insight to the further development of mGlu4 targeted therapies.

journal_name

Neuropharmacology

journal_title

Neuropharmacology

authors

Poutiainen P,Kil KE,Zhang Z,Kuruppu D,Tannous B,Brownell AL

doi

10.1016/j.neuropharm.2015.05.017

subject

Has Abstract

pub_date

2015-10-01 00:00:00

pages

142-8

eissn

0028-3908

issn

1873-7064

pii

S0028-3908(15)00198-7

journal_volume

97

pub_type

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