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Endocannabinoids and Their Pharmacological Actions.

Roger G Pertwee1

  • 1School of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen, Scotland, UK. rgp@abdn.ac.uk.

Handbook of Experimental Pharmacology
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Summary

This review identifies 13 potential orthosteric endocannabinoids and three allosteric endocannabinoids, detailing their interactions with cannabinoid receptors (CB1 and CB2) and other targets in vitro.

Keywords:
2-ArachidonoylglycerolAnandamideCannabinoid receptorsDihomo-γ-linolenoylethanolamideDocosahexaenoylethanolamideDocosatetraenoylethanolamideEicosapentaenoylethanolamideEndocannabinoid pharmacologyHaemopressinLipoxin A4N-arachidonoyldopamineN-oleoyldopamineNoladin etherOleamidePepcan-12PregnenoloneSphingosineVirodhamine

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Area of Science:

  • Endocrinology
  • Neuroscience
  • Pharmacology

Background:

  • The endocannabinoid system comprises cannabinoid receptors (CB1, CB2), endogenous ligands (endocannabinoids), and associated enzymes and uptake mechanisms.
  • Understanding the full spectrum of endocannabinoids and their receptor interactions is crucial for deciphering system function.

Purpose of the Study:

  • To review in vitro evidence identifying potential orthosteric and allosteric endocannabinoids.
  • To characterize the binding and functional activity of these compounds at cannabinoid receptors (CB1, CB2).
  • To explore potential off-target interactions with non-cannabinoid receptors and ion channels.

Main Methods:

  • Literature review of in vitro studies investigating endocannabinoid compounds.
  • Analysis of binding assays and functional assays for receptor activation, antagonism, and modulation.
  • Examination of data on interactions with non-cannabinoid targets.

Main Results:

  • Identified 13 probable orthosteric endocannabinoids detected in mammalian tissues and binding to cannabinoid receptors.
  • Eight of these compounds activate CB1 and/or CB2 receptors; two act as antagonists/inverse agonists.
  • Evidence presented for three allosteric endocannabinoids, including negative and positive modulators of CB1 and CB2 receptors.
  • Some endocannabinoids exhibit in vitro activity at non-cannabinoid receptors and ion channels.

Conclusions:

  • A broad range of endogenous compounds function as orthosteric and allosteric endocannabinoids.
  • These compounds exhibit diverse activities, including agonism, antagonism, and allosteric modulation at CB1 and CB2 receptors.
  • Potential for off-target effects necessitates further investigation into the pharmacology of endocannabinoids.