scholarly journals Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors

1998 ◽  
Vol 124 (4) ◽  
pp. 619-622 ◽  
Author(s):  
S J MacLennan ◽  
P H Reynen ◽  
J Kwan ◽  
D W Bonhaus
Keyword(s):  
Inverse Agonism ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

The role of the peripheral cannabinoid system in the pathogenesis of detrusor overactivity evoked by increased intravesical osmolarity in rats

2015 ◽  
Vol 93 (8) ◽  
pp. 721-726 ◽  
Author(s):  
Kajetan Juszczak ◽  
Piotr Maciukiewicz
Keyword(s):  
Urinary Bladder ◽  
Detrusor Overactivity ◽  
Cannabinoid Receptors ◽  
Bladder Capacity ◽  
Pressure Profile ◽  
Intravesical Instillation ◽  
Motility Index ◽  
Urinary Bladder Dysfunction ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

The cannabinoid receptors CB1 and CB2 are localized in the urinary bladder and play a role in the regulation of its function. We investigated the pathomechanisms through which hyperosmolarity induces detrusor overactivity (DO). We compared urinary bladder activity in response to blockade of CB1 and CB2 receptors using AM281 and AM630, respectively, in normal rats and after hyperosmolar stimulation. Experiments were performed on 44 rats. DO was induced by intravesical instillation of hyperosmolar saline. Surgical procedures and cystometry were performed under urethane anaesthesia. The measurements represent the average of 5 bladder micturition cycles. We analysed basal, threshold, and micturition voiding pressure; intercontraction interval; compliance; functional bladder capacity; motility index; and detrusor overactivity index. The blockage of CB1 and CB2 receptors diminished the severity of hyperosmolar-induced DO. In comparison with naïve animals the increased frequency of voiding with no significant effect on intravesical voiding pressure profile was observed as a result of the blockage of CB1 and CB2 receptors. These results demonstrate that hyperosmolar-induced DO is mediated by CB1 and CB2 receptors. Therefore, the cannabinoid pathway could potentially be a target for the treatment of urinary bladder dysfunction.

Enhanced Humoral Immunity in Mice Lacking CB1 and CB2 Receptors (Cnr1 −/− /Cnr2 −/− Mice) is not Due to Increased Splenic Noradrenergic Neuronal Activity

2014 ◽  
Vol 9 (4) ◽  
pp. 544-557 ◽  
Author(s):  
Tyrell Simkins ◽  
Robert B. Crawford ◽  
John L. Goudreau ◽  
Keith J. Lookingland ◽  
Barbara L. F. Kaplan
Keyword(s):  
Neuronal Activity ◽  
Humoral Immunity ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

scholarly journals Minor Cannabinoids: Biosynthesis, Molecular Pharmacology and Potential Therapeutic Uses

2021 ◽  
Vol 12 ◽  
Author(s):  
Kenneth B. Walsh ◽  
Amanda E. McKinney ◽  
Andrea E. Holmes
Keyword(s):  
Transient Receptor Potential ◽  
Cannabis Sativa ◽  
Trp Channels ◽  
Current Knowledge ◽  
Synergistic Activity ◽  
Molecular Pharmacology ◽  
Isolation And Characterization ◽  
Therapeutic Uses ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

The medicinal use of Cannabis sativa L. can be traced back thousands of years to ancient China and Egypt. While marijuana has recently shown promise in managing chronic pain and nausea, scientific investigation of cannabis has been restricted due its classification as a schedule 1 controlled substance. A major breakthrough in understanding the pharmacology of cannabis came with the isolation and characterization of the phytocannabinoids trans-Δ9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD). This was followed by the cloning of the cannabinoid CB1 and CB2 receptors in the 1990s and the subsequent discovery of the endocannabinoid system. In addition to the major phytocannabinoids, Δ9-THC and CBD, cannabis produces over 120 other cannabinoids that are referred to as minor and/or rare cannabinoids. These cannabinoids are produced in smaller amounts in the plant and are derived along with Δ9-THC and CBD from the parent cannabinoid cannabigerolic acid (CBGA). While our current knowledge of minor cannabinoid pharmacology is incomplete, studies demonstrate that they act as agonists and antagonists at multiple targets including CB1 and CB2 receptors, transient receptor potential (TRP) channels, peroxisome proliferator-activated receptors (PPARs), serotonin 5-HT1a receptors and others. The resulting activation of multiple cell signaling pathways, combined with their putative synergistic activity, provides a mechanistic basis for their therapeutic actions. Initial clinical reports suggest that these cannabinoids may have potential benefits in the treatment of neuropathic pain, neurodegenerative diseases, epilepsy, cancer and skin disorders. This review focuses on the molecular pharmacology of the minor cannabinoids and highlights some important therapeutic uses of the compounds.

Virtual screening using Docking and Molecular Dynamics of cannabinoid analogues against CB1 and CB2 receptors

2021 ◽  
pp. 107590
Author(s):  
Antistio Avíz-Amador ◽  
Neyder Contreras-Puentes ◽  
Jairo Mercado-Camargo
Keyword(s):  
Molecular Dynamics ◽  
Virtual Screening ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

scholarly journals Cross-regulation of cannabinoid CB1 and CB2 receptors governs hepatic steatosis

2010 ◽  
Vol 30 (10) ◽  
pp. 1397-1399 ◽  
Author(s):  
Ying-Ying Yang ◽  
Han-Chieh Lin
Keyword(s):  
Hepatic Steatosis ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

Therapeutic Applications for Agents that Act at CB1 and CB2 Receptors

2009 ◽  
pp. 361-392 ◽  
Author(s):  
Roger G. Pertwee ◽  
Adèle Thomas
Keyword(s):  
Therapeutic Applications ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

Functional and Immunohistochemical Characterization of CB1 and CB2 Receptors in Rat Bladder

Urology ◽  
2008 ◽  
Vol 72 (5) ◽  
pp. 1174-1178 ◽  
Author(s):  
Matthew H. Hayn ◽  
Inmaculada Ballesteros ◽  
Fernando de Miguel ◽  
Christian H. Coyle ◽  
Shachi Tyagi ◽  
...  
Keyword(s):  
Rat Bladder ◽  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors

Expression of Cannabinoid Receptors on the Neoplastic Lymphocytes in Patients with Chronic Lymphocytic Leukemia.

Blood ◽  
2004 ◽  
Vol 104 (11) ◽  
pp. 4804-4804
Author(s):  
Jaroslaw A. Piszcz ◽  
Miroslawa Pietruczuk ◽  
Janusz S. Kloczko ◽  
Milena Dabrowska ◽  
Marzenna Galar ◽  
...  
Keyword(s):  
Chronic Lymphocytic Leukemia ◽  
Peripheral Blood ◽  
Cannabinoid Receptors ◽  
Lymphocytic Leukemia ◽  
Control Group ◽  
Neoplastic Cells ◽  
Fluorescent Intensity ◽  
Cb2 Receptors ◽  
Neoplastic Lymphocytes ◽  
Cb1 And Cb2 Receptors

Abstract Endocannabinoids take part in the physiology of neural and immune systems. The latest data showed that these compounds and their receptors play an important role in proliferation and apoptosis of various neoplastic cells. Cannabinoids were shown to increase apoptosis in human leukemia and lymphoma cell lines and culture of neoplastic cells obtained from patients with T-cell acute lymphoblastic leukemia. The aim of the study was an assessment of cannabinoid receptors expression on lymphocytes B derived from patients with CLL. The study group contains newly diagnosed, untreated adult patients with B-cell chronic lymphocytic leukemia; 13 male and 7 female, aged from 44 to 65. All of the patients were in B or C stage according to Binet. Peripheral blood samples from 10 healthy adult donors were used as the control group. The patients were hospitalized in the Department of Haematology, Medical University in Bialystok, Poland. Diagnosis of CLL in all cases was confirmed by routine immunophenotyping study. For flow cytometric analysis 1x105 – 1x106 of peripheral blood cells were incubated with 10ul of anty CB1 and anty CB2 polyclonal antibodies (American Diagnostics). Then 10ul of monoclonal antibodies IgG1-FITC and CD19-PE (Becton Dickinson) were added and the samples were incubated for 20 min in dark in 4°C. The samples were lysed, fixed and stabilized using Immuno-Prep (Coulter procedure) and assessed by flaw cytometry (Epics XL, Coulter). Statistical analysis was performed using non parametric U Mann-Whitney and Wilcoxon Tests. The conducted study revealed high expression of CB1 and CB2 receptors on the surface of neoplastic lymphocytes. The percentage of CB1/CD19 and CB2/CD19 positive cells in CLL patients were significantly higher, compared to the control group respectively (81.2±9,8% vs 12.0±9,3% p<0,05; 94,8±11,0 % vs 9,9±4,0%, p<0,05). No difference was noticed between the percentage of lymphocytes with CB1 and CB2 receptors expression in CLL and control group. Fluorescent intensity of CB2 receptors was about ten folds higher than CB1 receptors in both groups. The study demonstrated the presence of both types of cannabinoid receptors (CB1 and CB2) on neoplastic cells derived from patients with chronic lymphocytic leukemia. The higher percentage of B-lymphocytes expressing cannabinoid receptors in CLL patient suggests that the cannabinoid system may take part in CLL development. High intensity of CB2 receptor may be another target in CLL treatment.

scholarly journals Cannabinoid CB1 and CB2 Receptors and Fatty Acid Amide Hydrolase Are Specific Markers of Plaque Cell Subtypes in Human Multiple Sclerosis

2007 ◽  
Vol 27 (9) ◽  
pp. 2396-2402 ◽  
Author(s):  
C. Benito ◽  
J. P. Romero ◽  
R. M. Tolon ◽  
D. Clemente ◽  
F. Docagne ◽  
...  
Keyword(s):  
Multiple Sclerosis ◽  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Cb2 Receptors ◽  
Amide Hydrolase ◽  
Cb1 And Cb2 Receptors ◽  
Fatty Acid Amide

Capsaicin evokes hypothermia independent of cannabinoid CB1 and CB2 receptors

2005 ◽  
Vol 1065 (1-2) ◽  
pp. 147-151 ◽  
Author(s):  
Zhe Ding ◽  
Alan Cowan ◽  
Scott M. Rawls
Keyword(s):  
Cb2 Receptors ◽  
Cb1 And Cb2 Receptors
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