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Oxa-adamantyl cannabinoids.

Thanh C Ho1, Marcus A Tius1, Spyros P Nikas2

  • 1Department of Chemistry, University of Hawaii at Manoa, 2545 The Mall, Honolulu, HI 96822, United States.

Bioorganic & Medicinal Chemistry Letters
|February 26, 2021
PubMed
Summary
This summary is machine-generated.

Researchers developed novel oxa-adamantyl cannabinoids, finding they are high-affinity ligands for CB1 and CB2 receptors. These compounds act as potent CB1 receptor agonists, with one analog irreversibly labeling both receptors.

Keywords:
Binding affinityCB1 cannabinoid receptorCB2 cannabinoid receptorClassical cannabinoidDesignHexahydrocannabinolNovel classOxa-adamantyl cannabinoidSynthesis

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Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Organic Synthesis

Background:

  • Previous research focused on classical cannabinoids with bulky side chains.
  • Cannabinergic ligands are crucial for understanding endocannabinoid system functions.

Purpose of the Study:

  • To design, synthesize, and biologically evaluate novel 3'-functionalized oxa-adamantyl cannabinoids.
  • To explore a new class of cannabinergic ligands with potential therapeutic applications.

Main Methods:

  • Nucleophilic addition/transannular cyclization of aryllithium to epoxyketone using cerium chloride.
  • Stereoselective construction of the tricyclic cannabinoid nucleus.
  • In vitro evaluation of synthesized oxa-adamantyl cannabinoid analogs.

Main Results:

  • A convenient and scalable synthesis route for oxa-adamantyl cannabinoids was established.
  • The novel compounds demonstrated high affinity for both CB1 and CB2 cannabinoid receptors.
  • In cyclase assays, these compounds proved to be potent and efficacious CB1 receptor agonists.
  • The isothiocyanate analog AM10504 was shown to irreversibly label CB1 and CB2 receptors.

Conclusions:

  • 3'-functionalized oxa-adamantyl cannabinoids represent a novel class of cannabinergic ligands.
  • These compounds exhibit significant potential as pharmacological tools for studying cannabinoid receptors.
  • The developed synthetic methodology is amenable to scale-up for further research and development.