Cannabinoid receptor type 2 ligands: an analysis of granted patents since 2010

Author(s):  
Benjamin Brennecke ◽  
Thais Gazzi ◽  
Kenneth Atz ◽  
Jürgen Fingerle ◽  
Pascal Kuner ◽  
...  

The G-protein-coupled cannabinoid receptor type 2 (CB2R) is a key element of the endocannabinoid (EC) system. EC/CB2R signaling has significant therapeutic potential in major pathologies affecting humans such as allergies, neurodegenerative disorders, inflammation or ocular diseases. CB2R agonism exerts anti-inflammatory and tissue protective effects in preclinical animal models of cardiovascular, gastrointestinal, liver, kidney, lung and neurodegenerative disorders. Existing ligands can be subdivided into endocannabinoids, cannabinoid-like and synthetic CB2R ligands that possess various degrees of potency on and selectivity against the cannabinoid receptor type 1. This review is an account of granted CB2R ligand patents from 2010 up to the present, which were surveyed using Derwent Innovation®.

2021 ◽  
Vol 5 (1) ◽  
pp. 034-047
Author(s):  
Rajib Dutta

Medical benefits of cannabis and related compounds is widely known. Discovery of psychotropic plant cannabinoid Δ9-tetrahydrocannabinol have urged researchers to study more about the cannabinoid system and related therapeutics in the field of neurology and medicine. Where activation of cannabinoid receptor type 1 (CB1R) yielded in unwanted and serious side effects, discovery of cannabinoid receptor type 2 (CB2R) and its ligands gave a new hope. Till now there is limited success in this field because of complex expanded endocannabinoid system comprising of receptors, ligands and enzymes. In this review we will update about the role of endocannabinoidome relevant to neurological disorders.


2005 ◽  
Vol 14 (22) ◽  
pp. 3389-3396 ◽  
Author(s):  
Meliha Karsak ◽  
Martine Cohen-Solal ◽  
Jan Freudenberg ◽  
Agnes Ostertag ◽  
Caroline Morieux ◽  
...  

Author(s):  
Andrea Mastinu ◽  
Marika Premoli ◽  
Giulia Ferrari-Toninelli ◽  
Simone Tambaro ◽  
Giuseppina Maccarinelli ◽  
...  

Abstract The use of different natural and/or synthetic preparations of Cannabis sativa is associated with therapeutic strategies for many diseases. Indeed, thanks to the widespread diffusion of the cannabinoidergic system in the brain and in the peripheral districts, its stimulation, or inhibition, regulates many pathophysiological phenomena. In particular, central activation of the cannabinoidergic system modulates the limbic and mesolimbic response which leads to food craving. Moreover, cannabinoid agonists are able to reduce inflammatory response. In this review a brief history of cannabinoids and the protagonists of the endocannabinoidergic system, i.e. synthesis and degradation enzymes and main receptors, will be described. Furthermore, the pharmacological effects of cannabinoids will be outlined. An overview of the involvement of the endocannabinoidergic system in neuroinflammatory and metabolic pathologies will be made. Finally, particular attention will also be given to the new pharmacological entities acting on the two main receptors, cannabinoid receptor type 1 (CB1) and cannabinoid receptor type 2 (CB2), with particular focus on the neuroinflammatory and metabolic mechanisms involved.


2015 ◽  
Vol 3 (2) ◽  
pp. 53-63 ◽  
Author(s):  
Douglas Thewke ◽  
◽  
Courtney Netherland-Van Dyke ◽  
Ward Rodgers ◽  
Makenzie Fulmer ◽  
...  

2020 ◽  
Vol 21 (11) ◽  
pp. 3809 ◽  
Author(s):  
Francesca Rossi ◽  
Chiara Tortora ◽  
Maura Argenziano ◽  
Alessandra Di Paola ◽  
Francesca Punzo

In late December 2019, a novel coronavirus (SARS-CoV-2 or CoV-19) appeared in Wuhan, China, causing a global pandemic. SARS-CoV-2 causes mild to severe respiratory tract inflammation, often developing into lung fibrosis with thrombosis in pulmonary small vessels and causing even death. COronaVIrus Disease (COVID-19) patients manifest exacerbated inflammatory and immune responses, cytokine storm, prevalence of pro-inflammatory M1 macrophages and increased levels of resident and circulating immune cells. Men show higher susceptibility to SARS-CoV-2 infection than women, likely due to estrogens production. The protective role of estrogens, as well as an immune-suppressive activity that limits the excessive inflammation, can be mediated by cannabinoid receptor type 2 (CB2). The role of this receptor in modulating inflammation and immune response is well documented in fact in several settings. The stimulation of CB2 receptors is known to limit the release of pro-inflammatory cytokines, shift the macrophage phenotype towards the anti-inflammatory M2 type and enhance the immune-modulating properties of mesenchymal stromal cells. For these reasons, we hypothesize that CB2 receptor can be a therapeutic target in COVID-19 pandemic emergency.


2020 ◽  
Vol 57 (6) ◽  
pp. 2830-2845 ◽  
Author(s):  
Ying Yu ◽  
Lexiao Li ◽  
Davis T. Nguyen ◽  
Suni M. Mustafa ◽  
Bob M. Moore ◽  
...  

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