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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high affinity and are together...

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Updated: Jul 8, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

G-protein-coupled receptors.

R D Sanders1, D Brian, M Maze

  • 1Academic Anaesthetics, Imperial College, Chelsea & Westminster Hospital, 369 Fulham Road, London, SW10 9NH, UK, m.maze@ic.ac.uk.

Handbook of Experimental Pharmacology
|January 5, 2008
PubMed
Summary
This summary is machine-generated.

G-Protein-coupled receptors are key targets for anesthetic drugs, including opioid and alpha(2) adrenoceptor agonists. Further research into receptors like orexin and GABA may advance anesthetic pharmacology.

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Area of Science:

  • Anesthesiology
  • Pharmacology
  • Neuroscience

Background:

  • G-Protein-coupled receptors (GPCRs) are crucial for mediating the effects of many anesthetic drugs.
  • Opioid agonists are highly effective analgesics, while alpha(2) adrenoceptor agonists offer both hypnotic and analgesic properties.

Purpose of the Study:

  • To review the molecular and neural network pharmacology of anesthetic agents targeting GPCRs.
  • To highlight the clinical significance of GPCRs in anesthesia and critical care.

Main Methods:

  • Literature review of anesthetic agents acting on GPCRs.
  • Discussion of molecular targets and neural pathways involved.

Main Results:

  • GPCRs, including opioid, alpha(2) adrenoceptor, orexin, GABA(B), and muscarinic cholinergic receptors, are central to anesthetic actions.
  • Opioid and alpha(2) adrenoceptor agonists are clinically established anesthetic targets.

Conclusions:

  • Understanding GPCR pharmacology is vital for advancing anesthetic drug development.
  • Exploiting ligands at novel GPCR targets like orexin and GABA(B) holds promise for future anesthetic innovations.