ISSN:
1432-1912
Schlagwort(e):
Key words Ferret heart tissues
;
β1- and putative
;
β4-adrenoceptors* Carvedilol
;
(
;
)-Isoprenaline
;
(±)-CGP 12177
Quelle:
Springer Online Journal Archives 1860-2000
Thema:
Medizin
Notizen:
Abstract The putative β4-adrenoceptor mediates positive inotropic effects, action potential shortening and arrhythmias in ferret ventricle. Here we compared the affinity of carvedilol at the putative β4-adrenoceptor and β1-adrenoceptor, activated by (±)-CGP 12177 and (–)-isoprenaline, respectively. In paced right ventricular preparations, carvedilol (0.01–10 μmol/l) was a simple competitive antagonist of the positive inotropic effects of (±)-CGP 12177 (slope of Schild-plot = 1.02, pK B = 6.8) and (–)-isoprenaline (slope of Schild-plot = 0.98, pK B = 8.1). Carvedilol also blocked putative β4- and β1-adrenoceptors of left ventricle, left atrium and sino-atrial pacemaker. Carvedilol therefore interacts with the putative β4-adrenoceptor according to the law of mass action and may provide a lead in the development of putative β4-adrenoceptor-selective antagonists.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1007/PL00005367
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