[Apamin--a highly specific and effective blockader of calcium-dependent potassium conductance].
Apamin is a toxic polypeptide extracted from bee venom. It has been considered as a neurotoxin with central action, but its low concentrations (10(-8)-10(-7) M) were shown to reversibly block the nonadrenergic inhibition and effects of externally applied ATP, noradrenaline and caffeine in smooth muscles of the gastrointestinal tract. All these processes are related to the activation of Ca-dependent potassium permeability. Current-clamp, voltage-clamp and patch-clamp experiments have also shown that apamin blocks specifically some types of these conductances in other tissues: skeletal muscles, mammalian neurons and neuroblastoma, hepatocytes. Nowadays apamin is the most specific but not a universal blocker of the Ca-activated potassium conductance.
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D000818:Animals; D001030:Apamin / Q000494:pharmacology*; D001514:Bee Venoms / Q000494:pharmacology*; D002118:Calcium / Q000502:physiology*; D004305:Dose-Response Relationship, Drug; D004553:Electric Conductivity; D008099:Liver / Q000187:drug effects / Q000502:physiology; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D009474:Neurons / Q000187:drug effects / Q000502:physiology; D015221:Potassium Channels / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship
D001514:Bee Venoms; D015221:Potassium Channels; D001030:Apamin; D002118:Calcium
Apamin--vysokospetsificheskiĭ i éffektivnyĭ blokator nekotorykh kal'tsiĭzavisimykh kalievykh provodimosteĭ.