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Titolo:
INVESTIGATION OF ANGIOTENSIN-II AT(1) RECEPTORS WITH CARBON-11-L-159,884 - A SELECTIVE AT(1) ANTAGONIST
Autore:
SZABO Z; KAO PF; BURNS HD; GIBSON RE; HAMILL TG; RAVERT HT; KIM SE; MATHEWS WB; MUSACHIO JL; SCHEFFEL U; DANNALS RF;
Indirizzi:
JOHNS HOPKINS MED INST,DIV NUCL MED,NELSON BLDG B1-119,600 N WOLFE STBALTIMORE MD 21030 MERCK RES LABS,DEPT PHARMACOL W POINT PA 00000
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 7, volume: 39, anno: 1998,
pagine: 1209 - 1213
SICI:
0161-5505(1998)39:7<1209:IOAARW>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
BRAIN TRANSFER CONSTANTS; TIME UPTAKE DATA; ESSENTIAL-HYPERTENSION; GRAPHICAL EVALUATION; PHARMACOLOGY; POTENT; MK-996;
Keywords:
PET; KIDNEY; C-11; SUBSTITUTED BENZOYL SULFONAMIDES; DOGS; ANGIOTENSIN RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
Z. Szabo et al., "INVESTIGATION OF ANGIOTENSIN-II AT(1) RECEPTORS WITH CARBON-11-L-159,884 - A SELECTIVE AT(1) ANTAGONIST", The Journal of nuclear medicine, 39(7), 1998, pp. 1209-1213

Abstract

Antagonists of the angiotensin II AT(1) receptor subtype have been recently introduced for treatment of arterial hypertension and for pharmacological studies of these receptors, The purpose of this work was tolabel such an antagonist with C-11 and test the applicability of the radioligand for PET studies. Methods: The potent and selective nonpeptide AT(1) antagonist L-159,884 was labeled with C-11 and injected intravenously into six dogs. Renal accumulation and kinetics of the radioligand were imaged with PET at baseline and after receptor blockade with 1 mg/kg MK-996. Time-activity curves were derived from the renal cortex and were analyzed by the Gjedde-Patlak plot to obtain the influx rate constant of the radioligand. Results: There was selective radioligand binding in the kidneys, mainly located in the cortex, Within the time interval between 95 and 115 min postinjection, the radioactivity retained in the kidneys was 109 +/- 27 and 42 +/- 4 nCi/ml/mCi of the injected dose for the control and inhibition studies, respectively. Theinflux rate constant of the radioligand decreased from a baseline of 0.0298 +/- 0.0156 to a post-MK-996 value of 0.0098 +/- 0.0052, Conclusion: These results demonstrate distinct binding of C-11-L-159,884 in the renal cortex with a specific binding component suitable for quantitative PET imaging of angiotensin II/AT1 receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/09/20 alle ore 22:28:53