Chemical probes for the recognition of cannabinoid receptors in native systems.
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.
Department of Organic Chemistry, Universidad Complutense de Madrid, Spain.
Lidia
L
Martín-Couce
Mar
M
Martín-Fontecha
Oscar
O
Palomares
Leyre
L
Mestre
Arnau
A
Cordomí
Miriam
M
Hernangomez
Sara
S
Palma
Leonardo
L
Pardo
Carmen
C
Guaza
María L
ML
López-Rodríguez
Silvia
S
Ortega-Gutiérrez
D000818:Animals; D001710:Biotin / Q000737:chemistry; D002186:Cannabinoids / Q000494:pharmacology*; D002478:Cells, Cultured; D013759:Dronabinol / Q000031:analogs & derivatives* / Q000494:pharmacology; D005434:Flow Cytometry; D006624:Hippocampus / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D017628:Microglia / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D056004:Molecular Dynamics Simulation; D015335:Molecular Probes / Q000378:metabolism*; D009000:Monocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D009474:Neurons / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D018696:Neuroprotective Agents / Q000494:pharmacology; D011487:Protein Conformation; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000737:chemistry / Q000378:metabolism*; D043885:Receptor, Cannabinoid, CB2 / Q000737:chemistry / Q000378:metabolism*
D002186:Cannabinoids; D015335:Molecular Probes; D018696:Neuroprotective Agents; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; D001710:Biotin; D013759:Dronabinol; C402416:HU 308; C062018:HU 211