[Changes of affinity and capacity of cardiac glycoside receptors].
The receptor for cardiac glycosides probably is identical with the (Na+ + K+)-ATPase (approximately 250 000 Daltons). Its affinity for the therapeutically used glycosides is extremely different in different species (KD approximately 10(-9)M (human heart) - approximately 10(-7)M (rat heart]. In the latter, two distinct receptor types have been demonstrated (high- and low-affinity receptors) with different effects. In the human heart, there may be two cardiac glycoside receptors as well, although this has not been proved as yet. The number of cardiac glycoside receptors and their affinity is regulated in certain states and diseases. An increased receptor density is found in hyperthyroid states, in chronic hypokalaemia and in chronic digitalis treatment. A decreased number is measured in ischemic heart disease, in dilated cardiomyopathy and in hypothyroidism. Parallel to the decreased receptor density the maximal cardiac glycoside induced positive inotropy is reduced. Pronounced toxicity occurs, if the digitalis dose is increased in spite of missing effects.
D000375:Aging; D000818:Animals; D002301:Cardiac Glycosides / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D006801:Humans; D009200:Myocardial Contraction / Q000187:drug effects; D009206:Myocardium / Q000378:metabolism*; D011955:Receptors, Drug / Q000378:metabolism*; D000254:Sodium-Potassium-Exchanging ATPase
D002301:Cardiac Glycosides; D011955:Receptors, Drug; C028996:cardiac glycoside receptors; C027082:digitalis receptor; D000254:Sodium-Potassium-Exchanging ATPase
Veränderung der Affinität und der Kapazität des Herzglykosidrezeptors.