Related Experiment Video

Updated: Aug 18, 2026

Drug-Induced Sleep Endoscopy (DISE) with Target Controlled Infusion (TCI) and Bispectral Analysis in Obstructive Sleep Apnea
07:54

Drug-Induced Sleep Endoscopy (DISE) with Target Controlled Infusion (TCI) and Bispectral Analysis in Obstructive Sleep Apnea

Published on: December 6, 2016

Drug targets: turning the channel (on) for sedation

David J Sandstrom1, Howard Nash

  • 1NIH, NIMH, Bldg 36, Rm 1B08, MSC 4034, 9000 Rockville Pike Bethesda, Maryland 20892, USA.

Current Biology : CB
|March 19, 2004
PubMed

Insights

Genetic studies reveal that specific ion channels are key targets for anesthetics and ethanol. These drugs hyperactivate these ion channels, leading to sedation.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Sedative-hypnotic drugs, including ethanol and intravenous anesthetics, induce central nervous system depression.
  • The precise molecular mechanisms underlying sedation remain incompletely understood.

Purpose of the Study:

  • To identify the molecular targets responsible for the sedative effects of ethanol and intravenous anesthetics.
  • To elucidate the mechanism by which these drugs interact with their targets.

Main Methods:

  • Utilized genetic techniques to probe the function of ion channels.
  • Investigated the interaction between drugs and identified ion channel targets.

Main Results:

  • Identified two distinct ion channels as critical molecular targets for sedative drugs.
  • Demonstrated that these identified ion channels are hyperactivated by ethanol and anesthetics.

Conclusions:

  • Ion channels are crucial molecular targets mediating the sedative actions of ethanol and intravenous anesthetics.
  • Drug-induced hyperactivation of specific ion channels is a key mechanism of sedation.

More Related Videos

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Optogenetic Activation of Afferent Pathways in Brain Slices and Modulation of Responses by Volatile Anesthetics08:16

Optogenetic Activation of Afferent Pathways in Brain Slices and Modulation of Responses by Volatile Anesthetics

Published on: July 23, 2020

Related Concept Videos

Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Sedatives and Hypnotics: Overview01:23

Sedatives and Hypnotics: Overview

Sedatives are drugs that alleviate anxiety, while hypnotics induce sleep. Both classes of medication suppress neuronal activity, leading to a calming effect for sedatives and facilitating sleep for hypnotics.
Sedative-hypnotics are categorized into barbiturates, benzodiazepines (BZDs), and non-benzodiazepines or Z-drugs. These drugs work by suppressing central nervous system activity, and this suppression is dose-dependent. Older sedative medications, like barbiturates, follow a linear curve in...
Sedatives and Hypnotics Drugs: Barbiturates01:20

Sedatives and Hypnotics Drugs: Barbiturates

Sedatives and hypnotics encompass a drug class that acts on the central nervous system (CNS) to alleviate anxiety, promote relaxation and induce sleep.These drugs function by amplifying the actions of the neurotransmitter γ-aminobutyric acid (GABA), resulting in reduced neuronal activity. Barbiturates, a subset of sedatives and hypnotics first synthesized in the late 1800s, are categorized into ultra-short, short, intermediate, and long-acting groups based on their duration of effect. A key...
Sedatives and Hypnotics Drugs: Benzodiazepines01:19

Sedatives and Hypnotics Drugs: Benzodiazepines

Benzodiazepines have both sedative and hypnotic properties. They include compounds such as diazepam (Valium) and alprazolam (Xanax). Structurally, their cores are similar, consisting of the fusion of a benzene ring and a diazepine ring, but they share a common mechanism of action in the central nervous system (CNS).
Benzodiazepines work by enhancing the effects of the inhibitory neurotransmitter GABA. They bind to the GABAA receptor, increasing its affinity for GABA, which opens chloride...
Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...