scholarly journals Difference and Influence of Inactive and Active States of Cannabinoid Receptor Subtype CB2: From Conformation to Drug Discovery

2016 ◽  
Vol 56 (6) ◽  
pp. 1152-1163 ◽  
Author(s):  
Jianping Hu ◽  
Zhiwei Feng ◽  
Shifan Ma ◽  
Yu Zhang ◽  
Qin Tong ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cannabinoid Receptor ◽  
Receptor Subtype

Toxicological profiles of selected synthetic cannabinoids showing high binding affinities to the cannabinoid receptor subtype CB1

2013 ◽  
Vol 87 (7) ◽  
pp. 1287-1297 ◽  
Author(s):  
Verena J. Koller ◽  
Gerhard J. Zlabinger ◽  
Volker Auwärter ◽  
Sabine Fuchs ◽  
Siegfried Knasmueller
Keyword(s):  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Receptor Subtype ◽  
Binding Affinities ◽  
High Binding

scholarly journals Molecular Dynamics Simulations of the Activated Cannabinoid Receptor Subtype 2/Gi Protein Complex

2013 ◽  
Vol 104 (2) ◽  
pp. 537a
Author(s):  
Jagjeet Singh ◽  
Diane Lynch ◽  
Alan Grossfield ◽  
Michael Pitman ◽  
Patricia Reggio
Keyword(s):  
Molecular Dynamics ◽  
Molecular Dynamics Simulations ◽  
Protein Complex ◽  
Cannabinoid Receptor ◽  
Receptor Subtype ◽  
Gi Protein ◽  
Dynamics Simulations

Cannabinoid Receptor Subtype-1 Regulates Allergic Airway Eosinophilia During Lung Helminth Infection

2021 ◽  
Author(s):  
Mark B. Wiley ◽  
Sarah D. Bobardt ◽  
Tara M. Nordgren ◽  
Meera G. Nair ◽  
Nicholas V. DiPatrizio
Keyword(s):  
Helminth Infection ◽  
Cannabinoid Receptor ◽  
Receptor Subtype ◽  
Airway Eosinophilia

Interplay Between Endocannabinoid System and Neurodegeneration: Focus on Polypharmacology

2021 ◽  
Vol 28 ◽  
Author(s):  
Francesca Seghetti ◽  
Silvia Gobbi ◽  
Federica Belluti ◽  
Angela Rampa ◽  
Alessandra Bisi
Keyword(s):  
Neurodegenerative Diseases ◽  
Cannabinoid Receptor ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Endocannabinoid System ◽  
Receptor Subtype ◽  
Disease Development ◽  
Therapeutic Approaches ◽  
Promising Therapeutic Target ◽  
Amide Hydrolase

: Pharmacological treatment of complex pathologies such as neurodegenerative diseases still represents a major challenge, due to the networked pathways involved in their onset and progression that may require equally complex therapeutic approaches. Polypharmacology, based on the simultaneous modulation of multiple targets involved in the disease, may offer the potential to increase effectiveness and reduce the drawbacks related to the use of drug combinations. Clearly, this approach requires both the knowledge of the systems responsible for disease development and the discovery of new attractive targets to be exploited to design a multitarget drug. Over the last years, an ever increasing interest has focused on the endocannabinoid system, implicated in the modulation of several physiological functions, among which neuroinflammation, a crucial process for most neurodegenerative diseases. In this respect, the cannabinoid receptor subtype 2 represents a promising therapeutic target, being overexpressed in microglia cells and thus involved in neuroinflammation. The indirect modulation of this system through the inhibition of the main enzymes responsible for endocannabinoids metabolism, namely fatty acid amide hydrolase and monoacylglycerol lipase, may also significantly affect neurodegenerative processes. The aim of this review is to give an overview of the opportunities posed by the endocannabinoid system for neurodegenerative diseases management, mainly focusing on the potential for a multitarget strategy.

scholarly journals Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies

2018 ◽  
Vol 146 ◽  
pp. 409-422 ◽  
Author(s):  
Dominik Heimann ◽  
Frederik Börgel ◽  
Henk de Vries ◽  
Marius Patberg ◽  
Eliot Jan-Smith ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Metabolic Stability ◽  
Receptor Subtype

scholarly journals Assessment of select synthetic cannabinoid receptor agonist bias and selectivity between the type 1 and type 2 cannabinoid receptor

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Ayat Zagzoog ◽  
Asher L. Brandt ◽  
Tallan Black ◽  
Eunhyun D. Kim ◽  
Riley Burkart ◽  
...  
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Partial Agonist ◽  
Synthetic Cannabinoid ◽  
Receptor Subtype ◽  
Service Agency ◽  
Subtype Selectivity ◽  
Insight Into

AbstractThe first synthetic cannabinoid receptor agonists (SCRAs) were designed as tool compounds to study the endocannabinoid system’s two predominant cannabinoid receptors, CB1R and CB2R. Unfortunately, novel SCRAs now represent the most rapidly proliferating novel psychoactive substances (NPS) of abuse globally. Unlike ∆9-tetrahydrocannabinol, the CB1R and CB2R partial agonist and the intoxicating constituent of Cannabis, many SCRAs characterized to date are full agonists of CB1R. Gaining additional insight into the pharmacological activity of these SCRAs is critical to assess and regulate NPSs as they enter the marketplace. The purpose of this study was to assess select SCRAs recently identified by Canadian police, border service agency, private companies and the illicit market as potential CB1R and CB2R agonists. To this end, fifteen SCRAs were screened for in vitro activity and in silico interactions at CB1R and CB2R. Several SCRAs were identified as being highly biased for cAMP inhibition or βarrestin2 recruitment and receptor subtype selectivity between CB1R and CB2R. The indazole ring and halogen-substituted butyl or pentyl moieties were identified as two structural features that may direct βarrestin2 bias. Two highly-biased SCRAs—JWH-018 2′-napthyl-N-(3-methylbutyl) isomer (biased toward cAMP inhibition) and 4-fluoro MDMB-BINACA (biased toward βarrestin2 recruitment) displayed unique and differential in vivo activity in mice. These data provide initial insight into the correlations between structure, signalling bias, and in vivo activity of the SCRAs.

scholarly journals Erratum to: Toxicological profiles of selected synthetic cannabinoids showing high binding affinities to the cannabinoid receptor subtype CB1

2013 ◽  
Vol 87 (7) ◽  
pp. 1299-1299
Author(s):  
Verena J. Koller ◽  
Gerhard J. Zlabinger ◽  
Volker Auwärter ◽  
Sabine Fuchs ◽  
Siegfried Knasmueller
Keyword(s):  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Receptor Subtype ◽  
Binding Affinities ◽  
High Binding
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