Anesthetics and ion channels: molecular models and sites of action.

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Yamakura T, Bertaccini E, Trudell JR, Harris RA

Anesthetics and ion channels: molecular models and sites of action.

Annu Rev Pharmacol Toxicol. 2001;41:23-51.

PubMed ID

11264449 [ View in PubMed

]

Abstract

The mechanisms of general anesthesia in the central nervous system are finally yielding to molecular examination. As a result of research during the past several decades, a group of ligand-gated ion channels have emerged as plausible targets for general anesthetics. Molecular biology techniques have greatly accelerated attempts to classify ligand-gated ion channel sensitivity to general anesthetics, and have identified the sites of receptor subunits critical for anesthetic modulation using chimeric and mutated receptors. The experimental data have facilitated the construction of tenable molecular models for anesthetic binding sites, which in turn allows structural predictions to be tested. In vivo significance of a putative anesthetic target can now be examined by targeted gene manipulations in mice. In this review, we summarize from a molecular perspective recent advances in our understanding of mechanisms of action of general anesthetics on ligand-gated ion channels.

DrugBank Data that Cites this Article

Drugs

Butabarbital

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Amobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Amobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Amobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Aprobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Aprobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Aprobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Barbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Barbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Barbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Barbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	GABA(A) Receptor (Protein Group)	Protein group	Humans	Yes	Positive allosteric modulator	Details
Butabarbital	Glutamate receptor 1	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor 3	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor 4	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor ionotropic, kainate 1	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor ionotropic, kainate 3	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor ionotropic, kainate 4	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Glutamate receptor ionotropic, kainate 5	Protein	Humans	Unknown	Antagonist	Details
Butabarbital	Neuronal Acetylcholine (nACh) Receptor Subunits (Protein Group)	Protein group	Humans	Unknown	Inhibitor	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Butalbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Butalbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Butalbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Butalbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Butobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Butobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Butobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Heptabarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Heptabarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Heptabarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Hexobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Hexobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Hexobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Metharbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Metharbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Metharbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Metharbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Methylphenobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Methylphenobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Methylphenobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Pentobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Pentobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Pentobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Phenobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Phenobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Phenobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Phenobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Phenobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Primidone	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Primidone	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Primidone	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Primidone	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Quinidine barbiturate	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Quinidine barbiturate	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Quinidine barbiturate	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Secobarbital	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Secobarbital	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Secobarbital	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Talbutal	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Talbutal	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Talbutal	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Talbutal	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details
Thiamylal	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Agonist	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Thiopental	Glutamate receptor 2	Protein	Humans	Unknown	Antagonist	Details
Thiopental	Glutamate receptor ionotropic, kainate 2	Protein	Humans	Unknown	Antagonist	Details
Thiopental	Neuronal acetylcholine receptor subunit alpha-4	Protein	Humans	Unknown	Antagonist	Details
Thiopental	Neuronal acetylcholine receptor subunit alpha-7	Protein	Humans	Unknown	Antagonist	Details