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Titolo:
IMAGING OF DELTA-OPIOID RECEPTORS IN HUMAN BRAIN BY N1'-([C-11]METHYL)NALTRINDOLE AND PET
Autore:
MADAR I; LEVER JR; KINTER CM; SCHEFFEL U; RAVERT HT; MUSACHIO JL; MATHEWS WB; DANNALS RF; FROST JJ;
Indirizzi:
JOHNS HOPKINS UNIV,SCH MED,DEPT RADIOL,DIV NUCL MED,600 N WOLFE ST,ROOM B1-130 BALTIMORE MD 21287 JOHNS HOPKINS UNIV,SCH MED,DEPT RADIOL,DIV NUCL MED BALTIMORE MD 21287 JOHNS HOPKINS UNIV,DEPT NEUROSCI BALTIMORE MD 21287 JOHNS HOPKINS UNIV,DEPT ENVIRONM HLTH SCI BALTIMORE MD 21287
Titolo Testata:
Synapse
fascicolo: 1, volume: 24, anno: 1996,
pagine: 19 - 28
SICI:
0887-4476(1996)24:1<19:IODRIH>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; TEMPORAL-LOBE EPILEPSY; NALORPHINE-LIKE DRUGS; MU-OPIATE RECEPTORS; CHRONIC SPINAL DOG; C-11 DIPRENORPHINE; ANATOMICAL LOCALIZATION; INVIVO BINDING; MORPHINE-LIKE; MOUSE-BRAIN;
Keywords:
METHYLNALTRINDOLE; DELTA OPIOID RECEPTORS; HUMAN BRAIN; POSITRON EMISSION TOMOGRAPHY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
45
Recensione:
Indirizzi per estratti:
Citazione:
I. Madar et al., "IMAGING OF DELTA-OPIOID RECEPTORS IN HUMAN BRAIN BY N1'-([C-11]METHYL)NALTRINDOLE AND PET", Synapse, 24(1), 1996, pp. 19-28

Abstract

Recently, we have developed the positron emitting radiotracer N1'([C-11]methyl)naltrindole ([C-11]MeNTI) and demonstrated its high selectivity for delta opioid receptors in the mouse brain [Lever et al. (1992)fur. J. Pharmacol., 216:449-450]. In the present study, we examined the selectivity of [C-11]MeNTI for the 6 opioid receptor in the human brain, using positron emission tomography (PET). The regional kinetics and distribution as well as the pharmacology confirmed the selectivityof [C-11]MeNTI for delta opioid receptor in the human brain. First, the regional kinetics of [C-11]MeNTI are in accordance with the densityof the delta opioid receptor. Rapid washout in receptor-poor areas and prolonged retention in receptor-rich areas were observed. Second, the regional distribution of [C-11]MeNTI correlated well (r = 0.91) withthe in vitro distribution of delta opioid sites but not with mu or kappa site densities (r less than or equal to 0.008 or r less than or equal to 0.014, respectively). [C-11]MeNTI binding was highest in regions of the neocortex (insular, parietal, frontal, cingulate, and occipital), caudate nucleus, and putamen. Binding was intermediate in the amygdala and lowest in the cerebellum and thalamus. Third, studies using the competitive antagonist naltrexone demonstrated the inhibition of [C-11]MeNTI binding. Naltrexone inhibition of [C-11]MeNTI binding was most effective in delta receptor-rich regions, and its inhibitory potency correlated well (r = 0.88) with the regional distribution of delta opioid sites. [C-11]MeNTI is the first radioligand which selectively labels delta opioid receptors in vivo in the human brain following systemic administration. The availability of [C-11]MeNTI will enable a receptor specific analysis of the role of [C-11]MeNTI receptors in normaland abnormal human brain. (C) 1996 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/10/20 alle ore 20:02:44