Antamanide antagonizes the phalloidin-induced negative inotropic effect and blocks voltage dependently the fast outward K+ current in voltage-clamped frog muscle fibres.
The effects of antamanide (10(-14)-10(-5) M) and N-acetyl-secophalloidin (10(-7)-5 X 10(-3) M) a neutral non-toxic derivative of phalloidin, were tested on voltage-clamped single frog muscle fibres. Antamanide protected muscle fibres against the negative inotropic effect of phalloidin but blocked the fast potassium permeability in the same concentration range and the same voltage-dependent manner as did phalloidin. N-Acetyl-secophalloidin exhibited a strongly attenuated blocking effect on K+ permeability in a 1,000-fold higher concentration range than phalloidin. Neither antamanide nor N-acetyl-secophalloidin affected the contractile properties. These results suggest the existence in the frog muscle membrane of a receptor with two sites for phalloidin and antamanide which acts on potassium conductance.
D000818:Animals; D003864:Depression, Chemical; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects*; D008564:Membrane Potentials / Q000187:drug effects; D009132:Muscles / Q000187:drug effects / Q000378:metabolism*; D009200:Myocardial Contraction / Q000187:drug effects*; D009842:Oligopeptides / Q000037:antagonists & inhibitors*; D010456:Peptides, Cyclic / Q000494:pharmacology*; D010539:Permeability; D010590:Phalloidine / Q000037:antagonists & inhibitors*; D011895:Rana ridibunda
D007473:Ion Channels; D009842:Oligopeptides; D010456:Peptides, Cyclic; C100265:antamanide; D010590:Phalloidine