The interaction of beta-adrenoceptor blocking drugs with platelet aggregation, calcium displacement and fluidization of the membrane.
beta-Adrenoceptor blocking drugs interfere with adenosine diphosphate-stimulated platelet aggregation. Alprenolol, exaprolol, Kö 1124 and propranolol inhibited the aggregation, metipranolol decreased the extent and rate of aggregation significantly. Atenolol potentiated the aggregation measured by amplitude significantly. The interaction of beta-adrenoceptor blocking drugs with aggregation correlated with the displacement of calcium ions from binding sites in isolated platelets and the fluidization of the whole platelets and isolated platelet membrane as measured with electron spin resonance of the spin probe. The most potent were highly liposoluble drugs alprenolol, exaprolol, metipranolol and propranolol which increased the calcium displacement and membrane fluidity, the least active was atenolol decreasing these phenomena. The inhibition by beta-adrenoceptor blocking drugs of stimulated platelet aggregation is rather a result of unspecific than specific receptor interaction.
Nosál
R
R
Jancinová
V
V
Ondrias
K
K
Jakubovský
J
J
Balgavý
P
P
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000526:Alprenolol / Q000494:pharmacology; D000818:Animals; D001262:Atenolol / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D004578:Electron Spin Resonance Spectroscopy; D008297:Male; D008433:Mathematics; D008560:Membrane Fluidity; D014290:Metipranolol / Q000494:pharmacology; D008854:Microscopy, Electron; D010974:Platelet Aggregation / Q000187:drug effects*; D011412:Propanolamines / Q000494:pharmacology; D011433:Propranolol / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013696:Temperature
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; C031472:Ko 1124; D001262:Atenolol; D000244:Adenosine Diphosphate; D000526:Alprenolol; D011433:Propranolol; C012969:exaprolol; D002118:Calcium; D014290:Metipranolol