Binding properties of 3-[125I]iodophencyclidine, a new radioligand for N-methyl-D-aspartate-gated ionic channels

Autor: Robert Chicheportiche, Jean Pierre Beaucourt, Michel Ponchant, Jean Marc Kamenka, Janique Guiramand
Přispěvatelé: Laboratoire de chimie biomoléculaire (LCB), Université Montpellier 2 - Sciences et Techniques (UM2)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-MAYOLI SPINDLER SA-Centre National de la Recherche Scientifique (CNRS), Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Neurobiologie de l'audition-plasticité synaptique, Institut National de la Santé et de la Recherche Médicale (INSERM), Centre de recherches de biochimie macromoléculaire (CRBM), Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-IFR122-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Spectrométrie Physique (LSP), Université Joseph Fourier - Grenoble 1 (UJF)-Centre National de la Recherche Scientifique (CNRS)
Jazyk: angličtina
Rok vydání: 1992
Předmět:
N-Methylaspartate
MESH: Rats
Stereochemistry
Glycine
MESH: Neurons
Ionic bonding
Biochemistry
MESH: Radioligand Assay
Dissociation (chemistry)
Ion Channels
Iodine Radioisotopes
03 medical and health sciences
Cellular and Molecular Neuroscience
chemistry.chemical_compound
Radioligand Assay
0302 clinical medicine
MESH: Glutamates
Glutamates
Radioligand
Animals
heterocyclic compounds
MESH: Animals
Binding site
030304 developmental biology
Neurons
0303 health sciences
Cell Membrane
Rats
Inbred Strains
MESH: Iodine Radioisotopes
MESH: Ion Channel Gating
Ligand (biochemistry)
MESH: Rats
Inbred Strains
MESH: Glycine
3. Good health
Rats
MESH: N-Methylaspartate
Membrane
chemistry
MESH: Ion Channels
NMDA receptor
[SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]
Piperidine
Ion Channel Gating
030217 neurology & neurosurgery
MESH: Cell Membrane
Zdroj: Journal of Neurochemistry
Journal of Neurochemistry, Wiley, 1992, 59 (2), pp.492-9. ⟨10.1111/j.1471-4159.1992.tb09397.x⟩
ISSN: 0022-3042
1471-4159
DOI: 10.1111/j.1471-4159.1992.tb09397.x⟩
Popis: International audience; The binding properties of the 125I-labeled phencyclidine derivative N-[1-(3-[125I]iodophenyl)cyclohexyl]piperidine (3-[125I]iodo-PCP), a new ligand of the N-methyl-D-aspartate (NMDA)-gated ionic channel, were investigated. Association and dissociation kinetic curves of 3-[125I]iodo-PCP with rat brain homogenates were well described by two components. About 32% of the binding was of fast association and fast dissociation, and the remaining binding was of slow association and slow dissociation. Saturation curves of 3-[125I]iodo-PCP also were well described using two binding sites: one of a high affinity (KDH = 15.8 +/- 2.3 nM) and the other of a low affinity (KDL = 250 +/- 40 nM). 3-Iodo-PCP inhibited the binding of 3-[125I]iodo-PCP with inhibition curves that were well fitted by a two-site model. The binding constants (KiH, BmaxH; KiL, BmaxL) so obtained were close to those obtained in saturation experiments. Ligands of NMDA-gated ionic channels also inhibited the binding of 3-[125I]iodo-PCP with two constants, KiH and KiL. There was a very good correlation (r = 0.987) between the affinities of these ligands to bind to NMDA-gated ionic channels and their potencies to inhibit the binding of 3-[125I]iodo-PCP with a high affinity. Moreover, the regional distribution of the high-affinity binding of 3-[125I]-iodo-PCP paralleled that of tritiated N-[1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP). In contrast to that of [3H] TCP, the binding of 3-[125I]iodo-PCP to well-washed rat brain membranes was fast and insensitive to glutamate and glycine.(ABSTRACT TRUNCATED AT 250 WORDS)
Databáze: OpenAIRE
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