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Titolo:
IMAGING NICOTINIC ACETYLCHOLINE-RECEPTORS WITH FLUORINE-18-FPH, AN EPIBATIDINE ANALOG
Autore:
VILLEMAGNE VL; HORTI A; SCHEFFEL U; RAVERT HT; FINLEY P; CLOUGH DJ; LONDON ED; WAGNER HN; DANNALS RF;
Indirizzi:
JOHNS HOPKINS MED INST,DIV NUCL MED,615 N WOLFE ST,ROOM 2001 BALTIMORE MD 21205 JOHNS HOPKINS MED INST,DIV NUCL MED BALTIMORE MD 21205 JOHNS HOPKINS MED INST,DIV RADIAT HLTH SCI BALTIMORE MD 21205 NIDA,BRAIN IMAGING SECT,INTRAMURAL RES PROGRAM,NIH BALTIMORE MD 00000
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 11, volume: 38, anno: 1997,
pagine: 1737 - 1741
SICI:
0161-5505(1997)38:11<1737:INAWFA>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; LIVING HUMAN-BRAIN; BINDING-SITES; RAT-BRAIN; CHOLINERGIC RECEPTORS; ALZHEIMERS-DISEASE; CEREBRAL-CORTEX; H-3 EPIBATIDINE; AUTORADIOGRAPHIC LOCALIZATION; ALPHA-BUNGAROTOXIN;
Keywords:
NICOTINIC RECEPTORS; PET; NONHUMAN PRIMATE; BRAIN; EPIBATIDINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
42
Recensione:
Indirizzi per estratti:
Citazione:
V.L. Villemagne et al., "IMAGING NICOTINIC ACETYLCHOLINE-RECEPTORS WITH FLUORINE-18-FPH, AN EPIBATIDINE ANALOG", The Journal of nuclear medicine, 38(11), 1997, pp. 1737-1741

Abstract

Nicotinic acetylcholine receptors (nAChRs) have been implicated in a variety of central processes, such as learning and memory and analgesia. These receptors also mediate the reinforcing properties of nicotinein tobacco products and are increased in postmortem samples of brainsof smokers, On the other hand, brains of individuals who have died from dementia of the Alzheimer type show abnormally low densities of nAChRs. In this study, the distribution and kinetics of [(+/-)-exo-2-(2-[F-18] fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane (F-18-FPH), a high-affinity nAChR agonist, was evaluated in a baboon using PET. Methods: After intravenous injection of 5 mCi [185 MBq] F-18-FPH into a 25-kg anesthetized baboon, sequential quantitative tomographic data were acquired over a period of 150 min. Regions of interest were placed and time-activity curves were generated, Brain kinetics of the radiotracer were calculated, and the in vivo regional binding in the baboon brain was compared with the known in vitro regional distribution of nAChRs in the rat and human brain. Results: Brain activity reached a plateau within 60 min after injection of the tracer, and the binding was reversible. Elimination of F-18-FPH was relatively rapid from the cerebellum (clearance t(1/2) = 3 hr), intermediate from the hypothalamus/midbrain (t(1/2) = 7 hr) and slow from the thalamus (t(1/2) = 16 hr). Radioactivity due to F-18-FPH at 130 min postinjection was highest in the thalamus and hypothalamus/midbrain, intermediate in the neocortex and hippocampus and lowest in the cerebellum. Subcutaneous injection of 1 mg/kgcytisine 45 min after injection of the radiotracer reduced brain activity at 130 min by 67%, 64%, 56% and 52% of control values in the thalamus, hypothalamus/midbrain, hippocampus and cerebellum, respectively. The regional binding of F-18-FPH at 130 min was highly correlated with the known densities of nAChR measured in vitro in human (r = 0.81) and rat brain (r = 0.90). Conclusion: These results demonstrate the feasibility of imaging nAChRs in vivo. Fluorine-18-FPH appears to be a suitable tracer to study nAChRs in the human brain.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/09/20 alle ore 07:36:30