The cloning and characterization of the cannabinoid type 1 receptor

2018 ◽  
Author(s):  
Mary E. Abood ◽  
Thomas Gamage
Keyword(s):  
Chronic Pain ◽  
Cannabinoid Receptor ◽  
Functional Characterization ◽  
Endocannabinoid System ◽  
Cb1 Receptor ◽  
Cannabinoid Type 1 Receptor ◽  
Endogenous Cannabinoid ◽  
Endogenous Cannabinoid System

The cloning and characterization of the first cannabinoid receptor (now known as the cannabinoid type 1 (CB1) receptor) by Matsuda et al. in the landmark paper discussed in this chapter was a seminal discovery in 1990. While the analgesic properties of marijuana had been known for thousands of years, the mechanisms through which marijuana produces analgesia were not understood. The identification and functional characterization of the CB1 receptor led to the discovery of an endogenous cannabinoid system (the endocannabinoid system), which has now been shown to be important not only for acute and chronic pain states, but also for a whole host of physiological and pathophysiological disorders.

scholarly journals Type 2 Diabetes Alters Vascular Cannabinoid Receptor 1 Expression, Phosphorylation Status, and Vasorelaxation in Rat Aorta

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4948
Author(s):  
Enrique Sánchez-Pastor ◽  
Xóchitl Trujillo ◽  
Christian Ramos-Flores ◽  
Mónica Ríos-Silva ◽  
Felipa Andrade ◽  
...  
Keyword(s):  
Metabolic Diseases ◽  
Cannabinoid Receptor ◽  
Endocannabinoid System ◽  
Rat Aorta ◽  
Cardiovascular Complications ◽  
Cb1 Receptor ◽  
Receptor Expression ◽  
Vasorelaxant Effect

Previous studies have suggested a role of the endocannabinoid system in metabolic diseases, such as diabetes. We investigated the effect of diabetes on cannabinoid receptor type 1 (CB1) expression and cannabinoid-induced vasorelaxation in rat aorta rings. Aortas from healthy rats and from rats with experimentally induced diabetes were used to compare the vasorelaxant effect of the cannabinoid agonist arachidonylcyclopropylamide (ACPA) and CB1 expression and localization. After 4–8 weeks of diabetes induction, CB1 receptor expression and CB1 phosphorylation were higher in aortic rings, in association with greater vasorelaxation induced by the CB1 agonist ACPA compared to healthy rats. The vasorelaxant effect observed in healthy rats is similar throughout the study. Further studies are needed to elucidate the implications of CB1 receptor overexpression in diabetes and its influence on the progression of the cardiovascular complications of this metabolic disease.

Functional characterization of putative cholesterol binding sequence (CRAC) in human type-1 cannabinoid receptor

2011 ◽  
Vol 116 (5) ◽  
pp. 858-865 ◽  
Author(s):  
Sergio Oddi ◽  
Enrico Dainese ◽  
Filomena Fezza ◽  
Mirko Lanuti ◽  
Daniela Barcaroli ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Functional Characterization ◽  
Human Type ◽  
Binding Sequence ◽  
Type 1 Cannabinoid Receptor ◽  
Cholesterol Binding

scholarly journals Identification and functional characterization of CD8+ T regulatory cells in type 1 diabetes patients

PLoS ONE ◽  
2019 ◽  
Vol 14 (1) ◽  
pp. e0210839 ◽  
Author(s):  
Marsha Pellegrino ◽  
Antonino Crinò ◽  
Manuela M. Rosado ◽  
Alessandra Fierabracci
Keyword(s):  
Type 1 Diabetes ◽  
T Regulatory Cells ◽  
Functional Characterization ◽  
Regulatory Cells ◽  
Diabetes Patients

scholarly journals Cannabinoid Receptors: An Update on Cell Signaling, Pathophysiological Roles and Therapeutic Opportunities in Neurological, Cardiovascular, and Inflammatory Diseases

2020 ◽  
Vol 21 (20) ◽  
pp. 7693
Author(s):  
Dhanush Haspula ◽  
Michelle A. Clark
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Inflammatory Diseases ◽  
Endocannabinoid System ◽  
Future Directions ◽  
The Past ◽  
Health And Disease ◽  
Made In

The identification of the human cannabinoid receptors and their roles in health and disease, has been one of the most significant biochemical and pharmacological advancements to have occurred in the past few decades. In spite of the major strides made in furthering endocannabinoid research, therapeutic exploitation of the endocannabinoid system has often been a challenging task. An impaired endocannabinoid tone often manifests as changes in expression and/or functions of type 1 and/or type 2 cannabinoid receptors. It becomes important to understand how alterations in cannabinoid receptor cellular signaling can lead to disruptions in major physiological and biological functions, as they are often associated with the pathogenesis of several neurological, cardiovascular, metabolic, and inflammatory diseases. This review focusses mostly on the pathophysiological roles of type 1 and type 2 cannabinoid receptors, and it attempts to integrate both cellular and physiological functions of the cannabinoid receptors. Apart from an updated review of pre-clinical and clinical studies, the adequacy/inadequacy of cannabinoid-based therapeutics in various pathological conditions is also highlighted. Finally, alternative strategies to modulate endocannabinoid tone, and future directions are also emphasized.

scholarly journals Positron Emission Tomographic Imaging of the Cannabinoid Type 1 Receptor System with [11C]OMAR ([11C]JHU75528): Improvements in Image Quantification Using Wild-Type and Knockout Mice

2011 ◽  
Vol 10 (6) ◽  
pp. 7290.2011.00019 ◽  
Author(s):  
Raúl Herance ◽  
Santiago Rojas ◽  
Sergio Abad ◽  
Xavier Jiménez ◽  
Juan Domingo Gispert ◽  
...  
Keyword(s):  
Cb1 Receptor ◽  
New Drugs ◽  
Wild Type ◽  
Receptor System ◽  
Cannabinoid Type 1 Receptor ◽  
Positron Emission ◽  
Study Support ◽  
Genetically Manipulated ◽  
The Brain

In this study, we assessed the feasibility of using positron emission tomography (PET) and the tracer [11C]OMAR ([11C]JHU75528), an analogue of rimonabant, to study the brain cannabinoid type 1 (CB1) receptor system. Wild-type (WT) andCB1 knockout (KO) animals were imaged at baseline and after pretreatment with blocking doses of rimonabant. Brain uptake in WT animals was higher (50%) than in KO animals in baseline conditions. After pretreatment with rimonabant, WT uptake lowered to the level of KO animals. The results of this study support the feasibility of using PET with the radiotracer [11C]JHU75528 to image the brain CB1 receptor system in mice. In addition, this methodology can be used to assess the effect of new drugs in preclinical studies using genetically manipulated animals.

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