Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Sedatives and Hypnotics: Overview01:23

Sedatives and Hypnotics: Overview

1.9K
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...
1.9K
Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

778
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...
778
Sedatives and Hypnotics Drugs: Benzodiazepines01:19

Sedatives and Hypnotics Drugs: Benzodiazepines

1.1K
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...
1.1K
Sedatives and Hypnotics Drugs: Barbiturates01:20

Sedatives and Hypnotics Drugs: Barbiturates

1.3K
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...
1.3K
Anxiolytic Drugs: Benzodiazepines and Buspirone01:29

Anxiolytic Drugs: Benzodiazepines and Buspirone

2.9K
Benzodiazepines are a class of anxiolytic drugs known for their rapid efficacy and high therapeutic-to-lethal dose ratio, but with a potential risk of drug dependence. These drugs are lipophilic, allowing for rapid absorption after oral administration, eventually reaching the central nervous system (CNS). Once in the CNS, benzodiazepines bind to the allosteric site of the GABAA receptor. This binding enhances the inhibitory effects of the neurotransmitter GABA. By doing so, they prevent...
2.9K
Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics01:11

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

893
All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...
893

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Low-dose radiotherapy synergizes with PD-1 blockade to achieve durable survival in advanced NSCLC through antitumor neutrophil programming.

Signal transduction and targeted therapy·2026
Same author

Association between low-density lipoprotein cholesterol and frailty in adults aged ≥70 years: a cross-sectional study from Beijing, China.

Frontiers in endocrinology·2026
Same author

Mechanistic study of compound Muniziqi granule on lupus nephritis in MRL/lpr mice: insights from transcriptomics and experimental validation.

Lupus science & medicine·2026
Same author

Effects of ultrasound-guided nerve block combined with PCIA analgesia on postoperative pain, inflammatory response, hospital stay, and adverse reactions in breast cancer surgery.

African health sciences·2026
Same author

ZNF683<sup>+</sup> NK cells govern chemotherapy sensitivity in advanced HPSCC via reshaping immune microenvironment.

Nature communications·2026
Same author

Genomic characterization of <i>Klebsiella pneumoniae</i> clinical isolates from cancer patients: resistance profiles, virulence factors, and sequence typing.

Frontiers in microbiology·2025

Related Experiment Video

Updated: Mar 16, 2026

Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets
10:16

Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets

Published on: March 12, 2019

47.2K

Sedative-hypnotic Binding to 11β-hydroxylase.

Ervin Pejo1, Xiaojuan Zhou, S Shaukat Husain

  • 1From the Department of Anesthesia, Critical Care, and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts.

Anesthesiology
|August 20, 2016
PubMed
Summary
This summary is machine-generated.

Etomidate and its metabolite cyclopropyl methoxycarbonyl metomidate (CPMM) bind to 11β-hydroxylase, but other sedatives only inhibit binding at high concentrations. This explains why etomidate causes more adrenal suppression than CPMM.

More Related Videos

Polygraphic Recording Procedure for Measuring Sleep in Mice
08:45

Polygraphic Recording Procedure for Measuring Sleep in Mice

Published on: January 25, 2016

25.6K
Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

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

Published on: August 16, 2018

14.3K

Related Experiment Videos

Last Updated: Mar 16, 2026

Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets
10:16

Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets

Published on: March 12, 2019

47.2K
Polygraphic Recording Procedure for Measuring Sleep in Mice
08:45

Polygraphic Recording Procedure for Measuring Sleep in Mice

Published on: January 25, 2016

25.6K
Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

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

Published on: August 16, 2018

14.3K

Area of Science:

  • Pharmacology
  • Endocrinology
  • Anesthesiology

Background:

  • Etomidate suppresses steroid synthesis by inhibiting 11β-hydroxylase.
  • This study investigated if other sedative-hypnotics or their metabolites inhibit 11β-hydroxylase at clinically relevant concentrations.

Purpose of the Study:

  • To determine the binding affinity of etomidate to 11β-hydroxylase.
  • To assess the potency of other sedative-hypnotics and their metabolites in inhibiting etomidate binding to 11β-hydroxylase.

Main Methods:

  • Used a filtration assay to characterize H-etomidate binding to rat adrenal membranes.
  • Determined half-inhibitory concentrations (IC50) of various sedative-hypnotics and metabolites for etomidate binding.

Main Results:

  • Etomidate's dissociation constant (Kd) for 11β-hydroxylase was 40 nM.
  • Cyclopropyl methoxycarbonyl metomidate (CPMM) had a significantly lower affinity (Kd=143 nM) than etomidate (Kd=26 nM).
  • Metabolites etomidate-CA and CPMM-CA showed >1000x lower potency than their parent drugs; other sedatives inhibited binding only at supraphysiologic concentrations.

Conclusions:

  • Etomidate's in vitro binding affinity correlates with its in vivo effects on adrenal steroid synthesis.
  • CPMM causes less adrenal suppression than etomidate due to faster metabolism and lower 11β-hydroxylase affinity.
  • Other tested sedative-hypnotics and metabolites do not significantly inhibit 11β-hydroxylase at therapeutic concentrations.