Published April 1988 | Version v1
Report Open

Preparation of radiopharmaceuticals labelled with bromine positron emitting isotopes for the study of dopaminergic receptors of the central nervous system using positron emission tomography

Creators

Description

The in vivo study of dopaminergic receptors of the central nervous system using positron emission tomography requires the preparation of radiopharmaceuticals labelled with β+ emitting isotopes. The chemical and pharmacological properties of these ligands are evaluated. Cyclotron produced 75 and 76 bromine β+ emitting isotopes are incorporated into dopaminergic ligands by electrophilic substitution using peracetic acid in a no-carrier added form. Purity, lipophilicity and specific activity are analyzed. Pharmacological criteria (specificity, saturability, displacement, localization) required for ligand-receptor binding studies are evaluated in vitro on striatal membranes and in vivo in the rat. Positron emission tomographic studies show that the study of dopaminergic D2 receptors is possible using 75 and 76 bromine labelled bromospiperone and bromolisuride. These ligands are used in physiological and pharmacological studies of the central nervous system

Availability note (English)

MF available from INIS under the Report Number.

Abstract (French)

L'etude in vivo des recepteurs dopaminergiques du systeme nerveux central au moyen de la tomographie par emission de positons necessite la preparation de molecules radiopharmaceutiques marquees avec des isotopes emetteurs β+. Les proprietes chimiques et pharmacologiques de ces ligands sont examinees avant leur utilisation. Preparation: les isotopes 75 et 76 du brome emetteurs β+ sont prepares au moyen d'un cyclotron et incorpores dans les ligands dopaminergiques par substitution electrophile au moyen d'acide peracetique sans ajout d'entraineur. La purete, la lipophilicite et l'activite specifique sont analysees. Caracterisations pharmacologiques: les criteres pharmacologiques (specificite, saturabilite, deplacement, localisation) necessaires aux etudes des liaisons ligand-recepteur sont verifies in vitro sur des membranes striatales et in vivo chez le rat. Etudes tomographiques: des etudes tomographiques par emission de positons montrent que la bromospiperone et la bromolisuride marquees avec les isotopes 75 et 76 du brome permettent l'etude des recepteurs dopaminergiques D2. Ces ligands ont ete utilises dans des etudes physiologiques et pharmacologiques du systeme nerveux central

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Additional details

Additional titles

Original title (French)
Preparation de molecules radiopharmaceutiques marquees avec des isotopes emetteurs de positons du brome et destinees a l'etude des recepteurs dopaminergiques centraux par tomographie d'emission de positons

Publishing Information

Imprint Pagination
162 p.
Report number
FRNC-TH--3340

INIS

Country of Publication
France
Country of Input or Organization
France
INIS RN
20007611
Subject category
S38: RADIATION CHEMISTRY, RADIOCHEMISTRY AND NUCLEAR CHEMISTRY; S62: RADIOLOGY AND NUCLEAR MEDICINE;
Resource subtype / Literary indicator
Thesis
Descriptors DEI
BIOLOGICAL LOCALIZATION; BROMINE 75; BROMINE 76; CARRIER-FREE ISOTOPES; CENTRAL NERVOUS SYSTEM; CHEMICAL PREPARATION; DOPAMINE; ISOTOPE PRODUCTION; LIGANDS; POSITRON COMPUTED TOMOGRAPHY; RADIOPHARMACEUTICALS; RATS; RECEPTORS
Descriptors DEC
AMINES; ANIMALS; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENT; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; BROMINE ISOTOPES; CARDIOTONICS; CARDIOVASCULAR AGENTS; COMPUTERIZED TOMOGRAPHY; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; EMISSION COMPUTED TOMOGRAPHY; HOURS LIVING RADIOISOTOPES; HYDROXY COMPOUNDS; INTERMEDIATE MASS NUCLEI; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; MAMMALS; MATERIALS; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ODD-EVEN NUCLEI; ODD-ODD NUCLEI; ORGANIC COMPOUNDS; PHENOLS; POLYPHENOLS; RADIOACTIVE MATERIALS; RADIOISOTOPES; RODENTS; SECONDS LIVING RADIOISOTOPES; STEROIDS; SYMPATHOMIMETICS; SYNTHESIS; TOMOGRAPHY; VERTEBRATES