The history of the pharmacology and cloning of ionotropic glutamate receptors and the development of idiosyncratic nomenclature

• Published in: Neuropharmacology 2009-01, Vol.56 (1), p.6-21
• Main Author: Lodge, David
• Format: Article
• Language: English
• Subjects: AMPA receptors; Animals; Cloning, Molecular; Glutamic Acid - pharmacology; History; History, 20th Century; History, 21st Century; Humans; Ionotropic glutamate receptors; Kainate receptors; NMDA receptors; Nomenclature; Receptors, Glutamate - classification; Receptors, Glutamate - genetics; Receptors, Glutamate - history; Terminology as Topic
• ISSN: 0028-3908; 1873-7064
• DOI: 10.1016/j.neuropharm.2008.08.006

In this article, the beginnings of glutamate pharmacology are traced from the early doubts about ‘non-specific’ excitatory effects, through glutamate- and aspartate-preferring receptors, to NMDA, quisqualate/AMPA and kainate subtypes, and finally to the cloning of genes for these receptor subunits. The development of selective antagonists, crucial to the subtype classification, allowed the fundamental importance of glutamate receptors to synaptic activity throughout the CNS to be realised. The ability to be able to express and manipulate cloned receptor subunits is leading to huge advances in our understanding of these receptors. Similarly the tortuous path of the nomenclature is followed from naming with reference to exogenous agonists, through abortive early attempts at generic schemes, and back to the NC-IUPHAR system based on the natural agonist, the defining exogenous agonist and the gene names.