A Fluorescent Probe to Unravel Functional Features of Cannabinoid Receptor CB1 in Human Blood and Tonsil Immune System Cells



Downloads per month over past year

Martín Fontecha, María del Mar and Angelina Querencias, Alba and Rückert, Beate and Rueda Zubiaurre, Ainoa and Martín Cruz, Leticia and Veen, Willem van de and Akdis, Mübeccel and Ortega Gutiérrez, Silvia and López Rodríguez, María Luz and Akdis, Cezmi A. and Palomares, Oscar (2018) A Fluorescent Probe to Unravel Functional Features of Cannabinoid Receptor CB1 in Human Blood and Tonsil Immune System Cells. Bioconjugate Chemistry, 29 (2). pp. 382-389. ISSN 1043-1802

[thumbnail of Martin Fontecha_2018-acs.bioconjchem.7b00680.pdf] PDF
Restringido a Repository staff only


Official URL: https://doi.org/10.1021/acs.bioconjchem.7b00680


The human endogenous cannabinoid system (ECS) regulates key physiological processes and alterations in its signaling pathways, and endocannabinoid levels are associated with diseases such as neurological and neuropsychiatric conditions, cancer, pain and inflammation, obesity, and metabolic and different immune related disorders. Immune system cells express the G-protein coupled cannabinoid receptor 1 (CB1), but its functional role has not been fully understood, likely due to the lack of appropriate tools. The availability of novel tools to investigate the role of CB1 in immune regulation might contribute to identify CB1 as a potential novel therapeutic target or biomarker for many diseases. Herein, we report the development and validation of the first fluorescent small molecule probe to directly visualize and quantify CB1 in blood and tonsil immune cells by flow cytometry and confocal microscopy. We coupled the cannabinoid agonist HU210 to the fluorescent tag Alexa Fluor 488, generating a fluorescent probe with high affinity for CB1 and selectivity over CB2. We validate HU210-Alexa488 for the rapid, simultaneous, and reproducible identification of CB1 in human monocytes, T cells, and B cells by multiplexed flow cytometry. This probe is also suitable for the direct visualization of CB1 in tonsil tissues, allowing the in vivo identification of tonsil CB1-expressing T and B cells. This study provides the first fluorescent chemical tool to investigate CB1 expression and function in human blood and tonsil immune cells, which might well pave the way to unravel essential features of CB1 in different immune and ECS-related diseases.

Item Type:Article
Additional Information:

Received 9 November 2017; Published online 9 January 2018; Published in print 21 February 2018

Uncontrolled Keywords:Inmune system cells; Human blood; Cannabinoid receptor B1; Endogenous cannabinoid system; Disorders; Neurological disorders; CB1; Biomarker
Subjects:Sciences > Chemistry > Biochemistry
Medical sciences > Medicine > Physiology
Medical sciences > Medicine > Immunology
ID Code:47251
Deposited On:19 Apr 2018 13:41
Last Modified:20 Apr 2018 07:47

Origin of downloads

Repository Staff Only: item control page