Voltage-dependent aminoglycoside blockade of the sarcoplasmic reticulum K+ channel.
Single-channel conductance of the K+ channel from sarcoplasmic reticulum (SR) was reduced by aminoglycoside antibiotics such as neomycin and ribostamycin and also by n-hexylamine from either side of the membrane in a dose- and voltage-dependent manner. K+ channels were incorporated into an artificial phospholipid bilayer. This inhibition follows a single-site titration curve. The voltage dependence of the inhibition is explained by assuming that these drugs bind to the open state of a single channel on one site located approximately 40% of the way through the membrane from the cis side (the side to which SR vesicles are added) when drugs are added to the cis side and bind on another site located approximately 40% of the way through the membrane from the trans side (the opposite side to the cis side) when drugs are added to the trans side.
Oosawa
Y
Y
Sokabe
M
M
D000588:Amines / Q000494:pharmacology; D000617:Aminoglycosides / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D001693:Biological Transport, Active / Q000187:drug effects; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects* / Q000378:metabolism; D009355:Neomycin / Q000494:pharmacology; D011188:Potassium / Q000378:metabolism*; D011817:Rabbits; D012271:Ribostamycin / Q000494:pharmacology; D012519:Sarcoplasmic Reticulum / Q000187:drug effects* / Q000378:metabolism
D000588:Amines; D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D007473:Ion Channels; D012271:Ribostamycin; C007940:hexylamine; D009355:Neomycin; D011188:Potassium