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Titolo: ADENOSINE A(1)RECEPTOR OCCUPANCY PREDICTS A(1)RECEPTOR ANTAGONIST EFFECTS OF N0861
Autore: YASUDA SU; NAGASHIMA S; DOUYON E; BENTON RE; WOOSLEY RL; BARBEY JT;
 Indirizzi:
 GEORGETOWN UNIV,MED CTR,DEPT PHARMACOL,MED DENT BLDG,SE404 WASHINGTONDC 20007 GEORGETOWN UNIV,MED CTR,DEPT MED,DIV CLIN PHARMACOL WASHINGTON DC 20007
 Titolo Testata:
 Clinical pharmacology and therapeutics
fascicolo: 5,
volume: 64,
anno: 1998,
pagine: 536  541
 SICI:
 00099236(1998)64:5<536:AAOPAA>2.0.ZU;23
 Fonte:
 ISI
 Lingua:
 ENG
 Soggetto:
 MYOCARDIALINFARCTION; PLASMACONCENTRATION; BINDING; HEART; RECEPTORS; INVIVO;
 Tipo documento:
 Article
 Natura:
 Periodico
 Settore Disciplinare:
 Science Citation Index Expanded
 Citazioni:
 20
 Recensione:
 Indirizzi per estratti:



 Citazione:
 S.U. Yasuda et al., "ADENOSINE A(1)RECEPTOR OCCUPANCY PREDICTS A(1)RECEPTOR ANTAGONIST EFFECTS OF N0861", Clinical pharmacology and therapeutics, 64(5), 1998, pp. 536541
Abstract
Objective: To evaluate the relationship between dose of N0861 ([+/]N6endonorbornan2yl9methyladenine), N0861 plasma concentrations, and antagonism of adenosineinduced slowing of atrioventricular nodal conduction and to evaluate A(1)receptor occupancy by antagonist present in plasma of subjects after administration of N0861 to determineA(1)selectivity of these effects. Methods: The study was conducted in patients undergoing a clinically indicated electrophysiology study to evaluate atrioventricular nodal conduction, Nineteen subjects were enrolled in the study and received adenosine (60 to 140 mu g/kg) beforeor during a bolus dose and maintenance infusion of specific doses of N0861, Adenosineinduced slowing of atrioventricular nodal conductionwas determined by measuring AH intervals on the intracardiac electrocardiograms, Plasma concentrations of N0861 were determined with an HPLC method, A(1)Receptor occupancy by antagonist present in plasma from identical time points was determined with use of a radioreceptor assay. Results: A Linear relationship was shown between plasma concentration and dose of N0861. AH interval lengthening by 60 mu g/kg adenosine was reduced by administration of N0861. A linear relationship wasobserved between A(1) occupancy and N0861 concentration and between occupancy and antagonism of adenosineinduced AH prolongation, Conclusion: The results suggest that the effect of N0861 on antagonism of adenosineinduced prolongation of AH interval, at the doses used in this study, were the result of effects at the A(1) receptor.
ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/04/20 alle ore 05:46:39