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Related Concept Videos

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...
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.
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...
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...

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Related Experiment Video

Updated: Jun 21, 2026

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

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Is GPR55 an anandamide receptor?

Andrew J Brown1, C Robin Hiley

  • 1Department of Screening and Compound Profiling, Molecular Discovery Research, GlaxoSmithKline, New Frontiers Science Park, GlaxoSmithKline, Essex, UK.

Vitamins and Hormones
|August 4, 2009
PubMed
Summary

Anandamide, an endocannabinoid, activates CB1 receptors but also affects vasculature via the GPR55 receptor. While GPR55 responds to anandamide, it is not primarily a cannabinoid receptor.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Endocannabinoid System Research

Background:

  • Anandamide activates CB1 cannabinoid receptors.
  • Vascular effects of anandamide are not fully explained by CB1 or CB2 receptors.
  • A novel G protein-coupled receptor (GPCR) is suspected to mediate these effects.

Purpose of the Study:

  • Investigate the role of GPR55 as a potential target for anandamide.
  • Clarify the pharmacological relationship between anandamide, CB1, and GPR55.
  • Elucidate the signaling pathways activated by GPR55 in response to anandamide.

Main Methods:

  • Pharmacological profiling of GPR55.
  • Analysis of GPR55 signaling pathways, including G(alpha12/13) and RhoA activation.
  • Assessment of intracellular calcium (Ca2+) signaling.

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  • Investigation of potential interactions between CB1 and GPR55.

    • Main Results:

    • GPR55 is primarily a receptor for lysophosphatidylinositol.
    • GPR55 exhibits biased agonism, responding to anandamide.
    • Anandamide activation of GPR55 leads to G(alpha12/13) and RhoA activation, causing oscillatory Ca2+ signals.
    • Complex interactions may exist between CB1 and GPR55.

    Conclusions:

    • GPR55 possesses multiple signaling modalities.
    • Anandamide can activate GPR55-containing systems.
    • GPR55 cannot be definitively classified as an endocannabinoid receptor for anandamide.