Chemical probes for the recognition of cannabinoid receptors in native systems

Angew Chem Int Ed Engl. 2012 Jul 9;51(28):6896-9. doi: 10.1002/anie.201200467. Epub 2012 Jun 11.

Abstract

Receptors made visible: The described biotin-tagged small-molecule probes with excellent affinities for the CB(1) and CB(2) cannabinoid receptors (CB(1)R and CB(2)R) enable direct visualization of these receptors in native cellular systems, including neurons, microglia, and immune cells. This method could overcome some of the limitations of current methodologies and may help to dissect the complexity of the endogenous cannabinoid system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biotin / chemistry
  • Cannabinoids / pharmacology*
  • Cells, Cultured
  • Dronabinol / analogs & derivatives*
  • Dronabinol / pharmacology
  • Flow Cytometry
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Humans
  • Microglia / cytology
  • Microglia / drug effects
  • Microglia / metabolism
  • Molecular Dynamics Simulation
  • Molecular Probes / metabolism*
  • Monocytes / cytology
  • Monocytes / drug effects
  • Monocytes / metabolism
  • Neurons / cytology
  • Neurons / drug effects
  • Neurons / metabolism
  • Neuroprotective Agents / pharmacology
  • Protein Conformation
  • Rats
  • Receptor, Cannabinoid, CB1 / chemistry
  • Receptor, Cannabinoid, CB1 / metabolism*
  • Receptor, Cannabinoid, CB2 / chemistry
  • Receptor, Cannabinoid, CB2 / metabolism*

Substances

  • Cannabinoids
  • Molecular Probes
  • Neuroprotective Agents
  • Receptor, Cannabinoid, CB1
  • Receptor, Cannabinoid, CB2
  • Biotin
  • Dronabinol
  • HU 308
  • HU 211