Spin-labeled ouabain as a probe for cardiac glycoside receptor/Na, K-ATPase
Biochemical and Biophysical Research Communications
|October 15, 1984
Abstract:
We have synthesized a nitroxide spin-label derivative of the cardiac glycoside, ouabain. It has been tested on purified Na,K-ATPase from dog kidney as a probe to study the physico-chemical interactions of this class of drugs with receptor(s). Spin-labeled ouabain retained the biochemical properties of native ouabain as judged by dose response curves for inhibition of Na,K-ATPase activity and inhibition of [3H]-ouabain binding to receptor. Electron paramagnetic resonance spectra of the spin-labeled ouabain-Na,K-ATPase complex revealed the presence of two types of bound label with differing degrees of immobilization.
Related Concept Videos
01:21G-Protein Gated Ion Channels
GPCRs are primarily responsible for our sense of smell, taste, and vision. The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory organs,...
Sensory organs,...
01:26Heart Failure Drugs: Inotropic Agents
Positive inotropic agents are commonly used as the first line of treatment for heart failure. One such agent is digoxin, derived from the genus Digitalis, which has been known for centuries but effectively utilized since 1785. However, these cardiac glycosides can have potentially toxic effects due to their mechanism of action, which involves inhibiting Na+/K+-ATPase and increasing contractility. Digoxin is absorbed orally and distributed in various tissues, including the CNS. It has a long...