ParkinsonCanadaV1, Main, Exploration, bibRecord, 003078

In vivo receptor assay with multiple ligand concentrations: An equilibrium approach

Identifieur interne : 003078 ( Main/Exploration ); précédent : 003077; suivant : 003079

In vivo receptor assay with multiple ligand concentrations: An equilibrium approach

Auteurs : James E. Holden [États-Unis] ; Salma Jivan [Canada] ; Thomas J. Ruth [Canada] ; Doris J. Doudet [Canada]

Source :

Journal of cerebral blood flow and metabolism [ 0271-678X ] ; 2002.

RBID : Pascal:02-0524445

Descripteurs français

Pascal (Inist)
- Tomographie émission positon, Raclopride, Récepteur dopaminergique D2, Ligand, Antagoniste dopamine, In vivo, Analyse quantitative, Capacité fixation, Méthode équilibre, Parkinson maladie, Méthode, Application médicale, Singe, Animal.
Wicri :
- topic : Analyse quantitative, Singe.

English descriptors

KwdEn :
- Animal, Binding capacity, D2 Dopamine receptor, Dopamine antagonist, Equilibrium method, In vivo, Ligand, Medical application, Method, Monkey, Parkinson disease, Positron emission tomography, Quantitative analysis, Raclopride.

Abstract

The ligand-receptor binding potential determined by in vivo PET studies at high ligand-specific radioactivity reflects both the receptor density and ligand-receptor affinity. This ambiguity has been resolved by various methods based on the administration of multiple unlabeled ligand concentrations. The authors aimed to implement and refine an approach to multiple ligand concentration receptor assay that combined maximum simplicity and a minimum of assumptions and model dependence that would nonetheless reliably distinguish density from affinity effects. The approach uses administration by bolus followed by infusion to obtain a true equilibrium between bound ligand and the other components of the ligand concentration, and does not require measurements of ligand in blood plasma. Four approaches to the optimization of the desired density and affinity parameters from the measured equilibrium data were implemented and compared in the analysis of raclopride studies performed in both normal control and MPTP-lesioned nonhuman primates. The authors conclude that the method is simple enough for routine use and yet reliable enough to apply in ongoing studies of both chronic and acute drug effects in the dopamine system.

Affiliations:

Links toward previous steps (curation, corpus...)

to stream PascalFrancis, to step Corpus: 000B55
to stream PascalFrancis, to step Curation: 000168
to stream PascalFrancis, to step Checkpoint: 000A15
to stream Main, to step Merge: 003524
to stream Main, to step Curation: 003078

Le document en format XML

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<front><div type="abstract" xml:lang="en">The ligand-receptor binding potential determined by in vivo PET studies at high ligand-specific radioactivity reflects both the receptor density and ligand-receptor affinity. This ambiguity has been resolved by various methods based on the administration of multiple unlabeled ligand concentrations. The authors aimed to implement and refine an approach to multiple ligand concentration receptor assay that combined maximum simplicity and a minimum of assumptions and model dependence that would nonetheless reliably distinguish density from affinity effects. The approach uses administration by bolus followed by infusion to obtain a true equilibrium between bound ligand and the other components of the ligand concentration, and does not require measurements of ligand in blood plasma. Four approaches to the optimization of the desired density and affinity parameters from the measured equilibrium data were implemented and compared in the analysis of raclopride studies performed in both normal control and MPTP-lesioned nonhuman primates. The authors conclude that the method is simple enough for routine use and yet reliable enough to apply in ongoing studies of both chronic and acute drug effects in the dopamine system.</div>
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In vivo receptor assay with multiple ligand concentrations: An equilibrium approach

In vivo receptor assay with multiple ligand concentrations: An equilibrium approach

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri