Cannabinoid subtype 1 receptors (CB1Rs) are an important class of G protein-coupled
receptors (GPCRs) belonging to the endocannabinoid system. CB1Rs play a crucial …

Cannabinoid subtype 2 receptors (CB2Rs) are G protein‐coupled receptors (GPCRs)
belonging to the endocannabinoid system, a complex network of signalling pathways …

We report the development of novel cannabinergic probes that can stabilize the cannabinoid
receptors (CBRs) through tight binding interactions. Ligand design involves the introduction …

There has been an expanding public interest towards the notion that modulation of the
sophisticated endocannabinoid system can lead to various therapeutic benefits that are yet …

Detailed characterization of the ligand-binding motifs and structure–function correlates of the
principal GPCRs of the endocannabinoid-signaling system, the cannabinoid 1 (CB1R) and …

A9-Tetrahydrocannabinol (THC) 1, the psychoactive ingredient of Cannabis sativa, was
isolated in 1964 (see Scheme 4.1). 1 In 1988, a specific brain receptor for THC, cannabinoid …

X-ray crystallography and cryogenic electronic microscopy have provided significant
advancement in the knowledge of GPCR structure and have allowed the rational design of …

The fatty acid amide hydrolase (FAAH, EC 3.5. 1.99) is an integral intracellular membrane-
bound enzyme that was properly characterized in the mid-1980s, 1 although an N …

Cannabinoid receptor type 1 and 2 (CB1 and CB2) are two G i/o-protein-coupled
cannabinoid receptors (CBRs), which showed promise in various conditions including pain …

Covalent probes, or affinity labels, are pharmacological tools that can be used to study the
structural and functional properties of GPCRs [1]. As illustrated in Chapter 2, these ligands …