Discrimination of Excitatory Amino Acid Receptor Sub-types Using Radioligand Binding Techniques

Fagg, Graham E.; Lanthorn, Thomas H.; Foster, Alan C.; Maier, L.; Dingwall, J. G.; Lane, John D.; Matus, Andrew

doi:10.1007/978-1-349-08479-1_18

Cited by 9 publications

(12 citation statements)

References 47 publications

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“…( (9, 12-22, 24, 25). Some of the quantitative differences between agonist and antagonist binding could correspond to differences between one of the multiple points of agonist-and antagonist-receptor attachment, as we and others have suggested (26,27 (10,34) and has been suggested to be occurring in Huntington disease (35,36). The hypothesis of a receptor form exhibiting greater responsiveness could also account for observations of altered NMDA receptor activity occurring in development (37) and following kindling (38).…”

Section: Discussionmentioning

confidence: 92%

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

Monaghan

Olverman

Nguyen

et al. 1988

Proc. Natl. Acad. Sci. U.S.A.

398

111

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The N-methyl-D-aspartate (NMDA) receptor, a subtype of excitatory amino acid receptor, mediates synaptic responses in many regions of the central nervous system. This receptor plays a critical role in the mechanisms of both synaptic plasticity and excitotoxicity. Although these receptors were generally thought to be a single homogeneous receptor population, we report observations indicating that two anatomically distinct forms of the NMDA-receptor complex exist. buffer, pH 7.0, preincubated at 30°C for 10 min, and then incubated for 10 min in ice-cold buffer containing 100 nM L-[3H]glutamate. NMDA receptors were selectively labeled by the inclusion of 100 ,uM 4-acetamido-4'-isothiocyanoatostilbene-2,2'-disulfonic acid, 5 ,uM amino-3-hydroxy-5-methylisoxazole-4-propionic acid, and 1 ,M kainic acid, which displace all detectable non-NMDA-receptor binding. Under these conditions the specific binding is fully displaced by NMDA agonists and antagonists at concentrations appropriate for NMDA receptors (12)(13)(14)(15)(16)(17)(18).Sections were then rinsed for 30 s, air dried, and placed against tritium-sensitive film along with tritium standards. Tissue sections in the experiments described in Fig. 2 9836The publication costs of this article were defrayed in part by page charge payment. This article must therefore be hereby marked "advertisement" in accordance with 18 U.S.C. §1734 solely to indicate this fact.

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Section: Discussionmentioning

confidence: 92%

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

Monaghan

Olverman

Nguyen

et al. 1988

Proc. Natl. Acad. Sci. U.S.A.

398

111

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“…In the absence of C1-and Ca2+ ions 13H]~-Glu labels a population of binding sites which in autoradiographic studies can be nearly quantitatively accounted for by the NMDA, QUIYAMPA, and KAIN receptors (32,36). However, in the presence of CaCl,, a large number of new binding sites are revealed (153). The binding to these sites is potently displaced by L -A P~ and is abolished by freezing and thawing (154,155).…”

Section: A Binding Studies Using Radiolabeled L-g~umentioning

confidence: 96%

“…The binding to these sites is potently displaced by L -A P~ and is abolished by freezing and thawing (154,155). The pharmacological profile, requirement for C1-ions, enhancement by Ca2+ ions, and lability to freeze-thawing indicate, that this is the most prevalent [3H]~-Glu binding site and the principal site investigated in most studies of [3H]~-Glu binding (31,153). The physiological function of these CaC1,-dependent [3H]~-Glu binding sites is at present uncertain.…”

Section: A Binding Studies Using Radiolabeled L-g~umentioning

confidence: 96%

“…The physiological function of these CaC1,-dependent [3H]~-Glu binding sites is at present uncertain. They were at one time thought to represent the putative L-AP4 receptors, a notion which now has been abandoned (153,156). Rather, these binding sites seem to be associated with transport processes (157), different from the conventional high-affinity uptake, and they may correspond to reuptake into resealed membrane vesicles (154,156) or a glial transport mechanism (158).…”

Section: A Binding Studies Using Radiolabeled L-g~umentioning

confidence: 98%

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Structural, conformational, and stereochemical requirements of central excitatory amino acid receptors

Hansen¹,

Krogsgaard‐Larsen²

1990

Medicinal Research Reviews

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“…In this review, the word will be applied only as referring to those loci with which the amino acids combine to evoke neuronal excitation: the properties of the attachment sites defined by radioligand binding to membrane fractions-also frequently called "receptors" [Fagg et al, 1986;Fagg and Baud, 1988;Honor6 and Drejer, 19881-and which are not necessarily always pharmacologically identical with the excitatory receptors, will not be considered here. Similarly, the sites responsible for uptake mechanisms or those mediating cytotoxicity will not be further discussed.…”

Section: Introductionmentioning

confidence: 99%

Pharmacology of receptors for excitatory amino acids

McLennan

1989

Drug Development Research

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McLennan, H.: Pharmacology of receptors for excitatory amino acids. Drug Dev. Res. 17~253-262, 1989.The pharmacological evidence for the existence of three distinct neuronal receptors for the excitatory amino acids is reviewed. Although most or all central neurones respond to the eponymous agonists N-methyl-D-aspartate (NMDA), quisqualate, and kainate, and the blockade of their effects is reasonably consistent throughout the neuraxis, subtle regional variations are detected when other agonists are tested. Thus, the tryptophan metabolite quinolinate is completely NMDA-mimetic in the hippocampus and neocortex but is almost inactive in the spinal cord. L-Homocysteate resembles NMDA in the cord and striatum but is quisqualate-like in the hippocampus. There is good evidence for the involvement of amino acids in the mediation of excitatory synaptic events; however, the regional differences in the actions of the endogenous agonists make positive identification of the chemical species active at a particular synaptic site, ,at best, rather tentative.

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Discrimination of Excitatory Amino Acid Receptor Sub-types Using Radioligand Binding Techniques

Cited by 9 publications

References 47 publications

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

Structural, conformational, and stereochemical requirements of central excitatory amino acid receptors

Pharmacology of receptors for excitatory amino acids

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