Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
ADENOSINE A(1)-RECEPTOR OCCUPANCY PREDICTS A(1)-RECEPTOR ANTAGONIST EFFECTS OF N-0861
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:
0009-9236(1998)64:5<536:AAOPAA>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
MYOCARDIAL-INFARCTION; PLASMA-CONCENTRATION; 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 N-0861", Clinical pharmacology and therapeutics, 64(5), 1998, pp. 536-541

Abstract

Objective: To evaluate the relationship between dose of N-0861 ([+/-]N-6-endo-norbornan-2-yl-9-methyladenine), N-0861 plasma concentrations, and antagonism of adenosine-induced slowing of atrioventricular nodal conduction and to evaluate A(1)-receptor occupancy by antagonist present in plasma of subjects after administration of N-0861 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 N-0861, Adenosine-induced slowing of atrioventricular nodal conductionwas determined by measuring A-H intervals on the intracardiac electrocardiograms, Plasma concentrations of N-0861 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 N-0861. A-H interval lengthening by 60 mu g/kg adenosine was reduced by administration of N-0861. A linear relationship wasobserved between A(1) occupancy and N-0861 concentration and between occupancy and antagonism of adenosine-induced A-H prolongation, Conclusion: The results suggest that the effect of N-0861 on antagonism of adenosine-induced prolongation of A-H 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