Interactions of general anesthetics within the pore of an ion channel. 1998

M Barann, and I Wenningmann, and J P Dilger
Klinik für Anästhesiologie, Universität Bonn, Germany.

(1) We review the electrophysiological evidence that the ion channel pore is the site at which general anesthetics bind to inhibit muscle-type acetylcholine receptor channels. (2) The amphipathic character of a pore certainly offers a suitable environment for the binding of amphipathic anesthetics. (3) The absence of direct information about the binding sites of these rather non-specific drugs, forces us to rely on indirect information provided by kinetic experiments. (4) We also discuss the implications of these findings for the interaction of general anesthetics with other ion channels.

UI MeSH Term Description Entries
D007473 Ion Channels Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS. Membrane Channels,Ion Channel,Ionic Channel,Ionic Channels,Membrane Channel,Channel, Ion,Channel, Ionic,Channel, Membrane,Channels, Ion,Channels, Ionic,Channels, Membrane
D011950 Receptors, Cholinergic Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology. ACh Receptor,Acetylcholine Receptor,Acetylcholine Receptors,Cholinergic Receptor,Cholinergic Receptors,Cholinoceptive Sites,Cholinoceptor,Cholinoceptors,Receptors, Acetylcholine,ACh Receptors,Receptors, ACh,Receptor, ACh,Receptor, Acetylcholine,Receptor, Cholinergic,Sites, Cholinoceptive
D004594 Electrophysiology The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D018680 Cholinergic Antagonists Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists. Acetylcholine Antagonist,Acetylcholine Antagonists,Anti-Cholinergic,Anticholinergic,Anticholinergic Agent,Anticholinergic Agents,Cholinergic Receptor Antagonist,Cholinergic-Blocking Agent,Cholinergic-Blocking Agents,Cholinolytic,Cholinolytics,Anti-Cholinergics,Anticholinergics,Cholinergic Antagonist,Cholinergic Receptor Antagonists,Agent, Anticholinergic,Agent, Cholinergic-Blocking,Agents, Anticholinergic,Agents, Cholinergic-Blocking,Antagonist, Acetylcholine,Antagonist, Cholinergic,Antagonist, Cholinergic Receptor,Antagonists, Acetylcholine,Antagonists, Cholinergic,Antagonists, Cholinergic Receptor,Anti Cholinergic,Anti Cholinergics,Cholinergic Blocking Agent,Cholinergic Blocking Agents,Receptor Antagonist, Cholinergic,Receptor Antagonists, Cholinergic
D018681 Anesthetics, General Agents that induce various degrees of analgesia; depression of consciousness, circulation, and respiration; relaxation of skeletal muscle; reduction of reflex activity; and amnesia. There are two types of general anesthetics, inhalation and intravenous. With either type, the arterial concentration of drug required to induce anesthesia varies with the condition of the patient, the desired depth of anesthesia, and the concomitant use of other drugs. (From AMA Drug Evaluations Annual, 1994, p.173) General Anesthetic,General Anesthetics,Anesthetic, General

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