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Insulin: The Receptor and Signaling Pathways01:28

Insulin: The Receptor and Signaling Pathways

Insulin action is mediated through a receptor tyrosine kinase, akin to the IGF-1 receptor. The number of receptors per cell varies significantly, from 40 on erythrocytes to 300,000 on adipocytes and hepatocytes. The insulin receptor consists of linked α/β subunit dimers, forming a heterotetramer glycoprotein with two extracellular α subunits and two β subunits spanning the membrane. The α subunits inhibit the inherent tyrosine kinase activity of the β subunits, but this inhibition is released...
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Intracellular Signaling Cascades01:24

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Once a ligand binds to a receptor, the signal is transmitted through the membrane and into the cytoplasm. The continuation of a signal in this manner is called signal transduction. Signal transduction only occurs with cell-surface receptors, which cannot interact with most components of the cell, such as DNA. Only internal receptors can interact directly with DNA in the nucleus to initiate protein synthesis. When a ligand binds to its receptor, conformational changes occur that affect the...

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Related Experiment Video

Updated: May 8, 2026

Human Pseudoislet System for Synchronous Assessment of Fluorescent Biosensor Dynamics and Hormone Secretory Profiles
08:04

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Published on: November 3, 2023

Islet cannabinoid receptors: cellular distribution and biological function.

Luis E Flores1, María E Alzugaray, Marisa A Cubilla

  • 1From the *CENEXA - Centro de Endocrinología Experimental y Aplicada (UNLP-CONICET LA PLATA, Centro Colaborador OPS/OMS para Diabetes), Facultad de Ciencias Médicas, UNLP, La Plata; and †Facultad de Ciencias Biomédicas, Universidad Austral, Pilar, Buenos Aires, Argentina.

Pancreas
|September 6, 2013
PubMed
Summary
This summary is machine-generated.

Cannabinoid receptors (CBs) in islet alpha cells modulate metabolic homeostasis. Blocking CB1 receptors with rimonabant (R) prevented fructose-induced metabolic dysfunction in rats, suggesting therapeutic potential.

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Area of Science:

  • Endocrinology
  • Metabolic Research
  • Pharmacology

Background:

  • Cannabinoid receptors (CBs) are implicated in metabolic regulation.
  • The role of islet CBs in diet-induced metabolic changes is not fully understood.
  • Fructose-rich diets are known to induce metabolic disturbances.

Purpose of the Study:

  • To investigate the cellular localization of islet CBs.
  • To determine the involvement of islet CBs in fructose-induced metabolic and hormonal alterations in rats.
  • To evaluate the therapeutic potential of a CB1 antagonist.

Main Methods:

  • Immunofluorescence and RT-PCR were used to identify CBs in rat islets.
  • Glucose-stimulated insulin secretion (GSIS) was measured in vitro with CB agonists and antagonists.
  • In vivo effects of rimonabant (R) were assessed in rats fed a fructose-rich diet (F), measuring metabolic parameters and gene expression.

Main Results:

  • CBs were exclusively found in islet alpha cells.
  • Fructose-fed rats exhibited increased triglycerides, insulin levels, and insulin resistance, which were ameliorated by rimonabant.
  • Rimonabant modulated gene expression of CBs and insulin receptor substrate in fructose-fed rats.

Conclusions:

  • Islet CBs play a significant role in maintaining metabolic homeostasis.
  • Rimonabant administration prevented fructose-induced metabolic impairment.
  • Selective CB1 receptor blockers may offer a strategy for treating metabolic disorders linked to unhealthy diets.