AUTHOR=Amenta Arianna , Caprioglio Diego , Minassi Alberto , Panza Luigi , Passarella Daniele , Fasano Valerio , Imperio Daniela 

TITLE=Recent advances in the development of CB1R selective probes

JOURNAL=Frontiers in Natural Products

VOLUME=2

YEAR=2023

URL=https://www.frontiersin.org/journals/natural-products/articles/10.3389/fntpr.2023.1196321

DOI=10.3389/fntpr.2023.1196321

ISSN=2813-2602

ABSTRACT=<p>Cannabinoid subtype 1 receptors (CB<sub>1</sub>Rs) are an important class of G protein-coupled receptors (GPCRs) belonging to the endocannabinoid system. CB<sub>1</sub>Rs play a crucial modulatory role in the functioning of other neurotransmitter systems and are involved in a wide range of physiological functions and dysfunctions; thus, they are considered one of the most important targets for drug development, as well as diagnostic purposes. Despite this, only a few molecules targeting this receptor are available on the pharmaceutical market, thus emphasizing the need to gain a deeper understanding of the complex activation pathways of CB<sub>1</sub>Rs and how they regulate diseases. As part of this review, we provide an overview of pharmacological and imaging tools useful for detecting CB<sub>1</sub>Rs. Herein, we summarize the derivations of cannabinoids and terpenoids with fluorescent compounds, radiotracers, or photochromic motifs. CB<sub>1</sub>Rs’ molecular probes may be used <italic>in vitro</italic> and, in some cases, <italic>in vivo</italic> for investigating and exploring the roles of CB<sub>1</sub>Rs together with the starting point for the development of CB<sub>1</sub>R-targeted drugs.</p>