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Titolo:
SPECIFIC BETA-ADRENERGIC-RECEPTOR BINDING OF CARAZOLOL MEASURED WITH PET
Autore:
BERRIDGE MS; NELSON AD; ZHENG L; LEISURE GP; MIRALDI F;
Indirizzi:
UNIV CLEVELAND HOSP,DIV NUCL RADIOL,2074 ABINGTON RD CLEVELAND OH 44106 CASE WESTERN RESERVE UNIV,SCH MED,DEPT RADIOL CLEVELAND OH 00000 CASE WESTERN RESERVE UNIV,SCH MED,DEPT CHEM CLEVELAND OH 00000
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 10, volume: 35, anno: 1994,
pagine: 1665 - 1676
SICI:
0161-5505(1994)35:10<1665:SBBOCM>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
LIVING HUMAN-BRAIN; INVIVO; SUBTYPES; HEART; RAT; METAIODOBENZYLGUANIDINE; IODOPINDOLOL; SYSTEM; MODEL;
Keywords:
PET; BETA-ADRENOCEPTORS; HEART; CARAZOLOL;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
M.S. Berridge et al., "SPECIFIC BETA-ADRENERGIC-RECEPTOR BINDING OF CARAZOLOL MEASURED WITH PET", The Journal of nuclear medicine, 35(10), 1994, pp. 1665-1676

Abstract

Carazolol is a promising high-affinity beta-adrenergic receptor ligand for the noninvasive determination of beta receptor status using PET. Earlier investigations demonstrated specific receptor binding of carazolol in mice. These PET studies with S(-)--[2''-C-11]carazolol in pigs were performed to explore the utility of the tracer for PET receptorstudies. Methods: Tracer uptake in the heart and lung was measured byPET as a function of time. Receptors were blocked with propranolol and different doses of ICI 118,551 to estimate specific binding. Fluorine-18-1''-Fluorocarazolol and the less active R-enantiomer of [C-11]-carazolol were also studied. Results: Specific receptor binding was 75% of the total uptake in the heart, preventable and displaceable by propranolol. Dose-dependent competition showed that carazolol binds in vivo to beta(1) and to beta(2) subtypes. Uptake of the labeled R(+) enantiomer of carazolol was not receptor-specific. Conclusions: Carazolol labeled with C-11 or F-18 is a strong candidate for use in receptor estimation with PET. The in vivo observations were consistent with its known high affinity and slow receptor dissociation rate. Its high specific receptor uptake and low metabolism allow existing kinetic models tobe applied for receptor measurements. The C-11 label is convenient for repeated administrations, though F-18 allowed the long observation periods necessary for measurement of the receptor dissociation rate. Ifneeded, nonspecific uptake can be estimated without pharmacologic intervention by using the labeled R enantiomer.

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Documento generato il 19/09/20 alle ore 14:27:33