Pachymatisma johnstonii extract opens ATP-sensitive potassium channels in cardiac myocytes of the frog heart.
The effects of a proteic extract (PachyTX), isolated from the sponge Pachymatisma johnstonii, were studied respectively with intracellular microelectrode and the "whole cell" patch clamp techniques on fibers and myocytes isolated from the sinoatrial region of frog heart. PachyTX significantly and reversibly shortened the action potential duration and decreased the stimulated peak contraction. Under voltage clamp, PachyTX increased, in a dose-dependent manner, a tetraethylammonium-insensitive but glibenclamide-inhibited outward current. This current failed to develop when adenosine 5'-triphosphate (ATP) was intracellularly applied to the cell by diffusion through the patch electrode. PachyTX mimics the effect of the ATP-sensitive K channel opener SR 44866 on frog atrial action potential and peak contraction. From this evidence, it can be concluded that PachyTX is a new natural potent opener of ATP-sensitive K channels in frog atrial heart muscle and that the opening of these channels is associated with the inhibition of the contraction of cardiac muscle.
Sauviat
M P
MP
Laboratoire de Physiologie Cellulaire, ERS CNRS F0100, Université de Paris XI, Orsay, France.
Moré
M T
MT
Verbist
J F
JF
D000255:Adenosine Triphosphate / Q000494:pharmacology*; D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology; D004095:Dihydropyridines / Q000494:pharmacology; D066298:In Vitro Techniques; D008387:Marine Toxins / Q000494:pharmacology*; D009200:Myocardial Contraction / Q000187:drug effects; D009206:Myocardium / Q000166:cytology / Q000378:metabolism*; D011161:Porifera / Q000737:chemistry*; D015221:Potassium Channels / Q000187:drug effects* / Q000378:metabolism*; D011893:Rana esculenta
D001578:Benzopyrans; D004095:Dihydropyridines; D008387:Marine Toxins; D015221:Potassium Channels; C061050:bimakalim; D000255:Adenosine Triphosphate