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The NMDA Receptor$
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G. L. Collingridge and J. C. Watkins

Print publication date: 1995

Print ISBN-13: 9780192625021

Published to Oxford Scholarship Online: March 2012

DOI: 10.1093/acprof:oso/9780192625021.001.0001

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Agonists and competitive antagonists: structure-activity and molecular modelling studies

Agonists and competitive antagonists: structure-activity and molecular modelling studies

Chapter:
(p.31) 2 Agonists and competitive antagonists: structure-activity and molecular modelling studies
Source:
The NMDA Receptor
Author(s):

D. E. JANE

H. J. OLVERMAN

J. C. WATKINS

Publisher:
Oxford University Press
DOI:10.1093/acprof:oso/9780192625021.003.0002

A wealth of information has now been generated, especially from radioligand binding studies, regarding the structural requirements for agonist and antagonist binding to the glutamate recognition site on the NMDA receptor. In combination with a number of molecular modelling studies this has been used to elucidate the three-dimensional topology of the receptor site and thus provide a basis for a rational design of new pharmacological agents with agonist or antagonist action at these sites. This chapter outlines the required structural features for agonist and antagonist binding. It then discusses the various molecular modelling studies which have recently been carried out.

Keywords:   agonists, molecular modelling, NMDA receptor, receptor site, pharmacological agents

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