Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
EVALUATION OF CEREBRAL PHARMACOKINETICS OF THE NOVEL ANTIDEPRESSANT DRUG, BMS-181101, BY POSITRON EMISSION TOMOGRAPHY
Autore:
CHRISTIAN BT; LIVNI E; BABICH JW; ALPERT NM; DISCHINO DD; RUEDIGER E; SALAZAR DE; FORD NF; FISCHMAN AJ;
Indirizzi:
MASSACHUSETTS GEN HOSP,DIV NUCL MED,32 FRUIT ST BOSTON MA 02114 MASSACHUSETTS GEN HOSP,DIV NUCL MED BOSTON MA 02114 MASSACHUSETTS GEN HOSP,DEPT RADIOL BOSTON MA 02114 HARVARD UNIV,SCH MED,DEPT RADIOL BOSTON MA 02115 BRISTOL MYERS SQUIBB CO PRINCETON NJ 08543
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 279, anno: 1996,
pagine: 325 - 331
SICI:
0022-3565(1996)279:1<325:EOCPOT>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
D2-DOPAMINE RECEPTOR OCCUPANCY; F-18 LABELED FLUCONAZOLE; HEALTHY-HUMAN SUBJECTS; C-11 RACLOPRIDE; PET; INVIVO; D1-DOPAMINE; BINDING; QUANTIFICATION; NEUROLEPTICS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
27
Recensione:
Indirizzi per estratti:
Citazione:
B.T. Christian et al., "EVALUATION OF CEREBRAL PHARMACOKINETICS OF THE NOVEL ANTIDEPRESSANT DRUG, BMS-181101, BY POSITRON EMISSION TOMOGRAPHY", The Journal of pharmacology and experimental therapeutics, 279(1), 1996, pp. 325-331

Abstract

BMS-181101 is a novel antidepressant drug that is currently under clinical investigation. The goal of this study was to evaluate the pharmacokinetics and receptor binding of this agent in the brains of healthyhuman volunteers. BMS-181101 was radiolabeled with C-11 by methylation with [C-11]CH3I of the 5-hydroxypiperazine precursor and the productwas purified by high-performance liquid chromatography. Cerebral pharmacokinetics of [C-11]BMS-181101 were studied by dynamic positron emission tomography imaging in six healthy volunteers. Two studies were performed in each subject. For the first study the subject was injected with 10 mCi of high specific activity [C-11]BMS-181101 (similar to 1700 mCi/mu mol) and serial positron emission tomography images and arterial blood samples were collected over 90 min. Thirty minutes after acquiring the final image, each subject was coinjected with a second dose, 10 mCi of [C-11]BMS-181101 plus 3 mg of unlabeled drug (final specific activity similar to 1.5 mCi/mu mol), and imaging/blood collection was repeated. The data were analyzed by calculating regional tracer accumulation (percent injected dose/g) at 60 min after injection and compartmental modeling. Measurements of percent injected dose/g yielded similar values for all brain regions, independent of specific activity. Kinetic modeling of time activity curves for cerebellum, caudate, putamen, thalamus, pens and temporal, occipital and frontal cortex demonstrated that tissue distribution can be described by a simple two-compartment flow model. Statistical comparisons of the apparent distributionvolumes for each region failed to reveal significant differences between the high and low specific activity studies. These results indicatethat the central nervous system distribution of [C-11]BMS-181101 is dominated by blood flow and significant receptor-specific localization does not occur in any brain region.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/04/20 alle ore 19:09:30