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Journal articles on the topic 'Cannabinoid CB1 receptor'

Author: Grafiati

Published: 11 March 2023

Last updated: 31 July 2025

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1

Soraya, hiva, Ruohollah Seddigh, Fatemeh Hadi, and Mohammad Faramarzi. "Chemical cannabis; The New Trend of addiction in Iran." Iranian Journal of Psychiatry and Clinical Psychology 28, no. 1 (2022): 10. http://dx.doi.org/10.32598/ijpcp.28.1.4010.1.

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Synthetic cannabinoids (SC) are a heterogeneous group of substances with a high affinity for cannabinoid receptors. Unlike Δ9-tetrahydrocannabinol (THC), synthetic cannabinoids are incredibly potent, highly productive, have more affinity for the Cannabinoid receptor type 1 (CB1), and Cannabinoid receptor type 2 (CB2), and are designed to accelerate the effects of tetrahydrocannabinol. Also, there is experimental evidence that SCs acts on non-cannabinoid receptors, such as the 5-HT2B receptor or dopaminergic receptors. (1, 2).

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Walsh, Kenneth B., and Andrea E. Holmes. "Pharmacology of Minor Cannabinoids at the Cannabinoid CB1 Receptor: Isomer- and Ligand-Dependent Antagonism by Tetrahydrocannabivarin." Receptors 1, no. 1 (2022): 3–12. http://dx.doi.org/10.3390/receptors1010002.

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(1) Background: In addition to the major phytocannabinoids, trans-Δ9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD), the cannabis plant (Cannabis sativa L.) synthesizes over 120 additional cannabinoids that are known as minor cannabinoids. These minor cannabinoids have been proposed to act as agonists and antagonists at numerous targets including cannabinoid type 1 (CB1) and type 2 (CB2) receptors, transient receptor potential (TRP) channels and others. The goal of the present study was to determine the agonist effects of the minor cannabinoids: cannabinol (CBN), cannabigerol (CBG), canna

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Li, Yong, and Jimok Kim. "CB2 Cannabinoid Receptor Knockout in Mice Impairs Contextual Long-Term Memory and Enhances Spatial Working Memory." Neural Plasticity 2016 (2016): 1–14. http://dx.doi.org/10.1155/2016/9817089.

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Neurocognitive effects of cannabinoids have been extensively studied with a focus on CB1 cannabinoid receptors because CB1 receptors have been considered the major cannabinoid receptor in the nervous system. However, recent discoveries of CB2 cannabinoid receptors in the brain demand accurate determination of whether and how CB2 receptors are involved in the cognitive effects of cannabinoids. CB2 cannabinoid receptors are primarily involved in immune functions, but also implicated in psychiatric disorders such as schizophrenia and depression. Here, we examined the effects of CB2 receptor knock

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SMALL-HOWARD, Andrea L., Lori M. N. SHIMODA, Chaker N. ADRA, and Helen TURNER. "Anti-inflammatory potential of CB1-mediated cAMP elevation in mast cells." Biochemical Journal 388, no. 2 (2005): 465–73. http://dx.doi.org/10.1042/bj20041682.

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Cannabinoids are broadly immunosuppressive, and anti-inflammatory properties have been reported for certain marijuana constituents and endogenously produced cannabinoids. The CB2 cannabinoid receptor is an established constituent of immune system cells, and we have recently established that the CB1 cannabinoid receptor is expressed in mast cells. In the present study, we sought to define a role for CB1 in mast cells and to identify the signalling pathways that may mediate the suppressive effects of CB1 ligation on mast cell activation. Our results show that CB1 and CB2 mediate diametrically op

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Dobovišek, Luka, Fran Krstanović, Simona Borštnar, and Nataša Debeljak. "Cannabinoids and Hormone Receptor-Positive Breast Cancer Treatment." Cancers 12, no. 3 (2020): 525. http://dx.doi.org/10.3390/cancers12030525.

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Breast cancer (BC) is the most common cancer in women worldwide. Approximately 70–80% of BCs express estrogen receptors (ER), which predict the response to endocrine therapy (ET), and are therefore hormone receptor-positive (HR+). Endogenous cannabinoids together with cannabinoid receptor 1 and 2 (CB1, CB2) constitute the basis of the endocannabinoid system. Interactions of cannabinoids with hypothalamic–pituitary–gonadal axis hormones are well documented, and two studies found a positive correlation between peak plasma endogenous cannabinoid anandamide with peak plasma 17β-estradiol, luteiniz

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GÓMEZ DEL PULGAR, Teresa, Guillermo VELASCO, and Manuel GUZMÁN. "The CB1 cannabinoid receptor is coupled to the activation of protein kinase B/Akt." Biochemical Journal 347, no. 2 (2000): 369–73. http://dx.doi.org/10.1042/bj3470369.

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Cannabinoids exert most of their effects in the central nervous system through the CB1 cannabinoid receptor. This G-protein-coupled receptor has been shown to be functionally coupled to inhibition of adenylate cyclase, modulation of ion channels and activation of extracellular-signal-regulated kinase. Using Chinese hamster ovary cells stably transfected with the CB1 receptor cDNA we show here that ∆9-tetrahydrocannabinol (THC), the major active component of marijuana, induces the activation of protein kinase B/Akt (PKB). This effect of THC was also exerted by the endogenous cannabinoid anandam

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Bow, Eric W., and John M. Rimoldi. "The Structure–Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation." Perspectives in Medicinal Chemistry 8 (January 2016): PMC.S32171. http://dx.doi.org/10.4137/pmc.s32171.

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The cannabinoids are members of a deceptively simple class of terpenophenolic secondary metabolites isolated from Cannabis sativa highlighted by (-)-Δ 9 -tetrahydrocannabinol (THC), eliciting distinct pharmacological effects mediated largely by cannabinoid receptor (CB1 or CB2) signaling. Since the initial discovery of THC and related cannabinoids, synthetic and semisynthetic classical cannabinoid analogs have been evaluated to help define receptor binding modes and structure–CB1/CB2 functional activity relationships. This perspective will examine the classical cannabinoids, with particular em

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Zibolka, Juliane, Anja Wolf, Lisa Rieger, et al. "Influence of Cannabinoid Receptor Deficiency on Parameters Involved in Blood Glucose Regulation in Mice." International Journal of Molecular Sciences 21, no. 9 (2020): 3168. http://dx.doi.org/10.3390/ijms21093168.

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Cannabinoids are known to influence hormone secretion of pancreatic islets via G protein-coupled cannabinoid receptor type 1 and 2 (CB1 and CB2). The present study was designed to further investigate the impact of cannabinoid receptors on the parameters involved in insulin secretion and blood glucose recognition. To this end, CB1 and CB2 receptor knockout mice (10–12 week old, both sexes) were characterised at basal state and compared to wild-type mice. The elimination of cannabinoid receptor signalling resulted in alterations of blood glucose concentrations, body weights and insulin levels. C

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Černe, Katarina. "Toxicological properties of Δ9-tetrahydrocannabinol and cannabidiol". Archives of Industrial Hygiene and Toxicology 71, № 1 (2020): 1–11. http://dx.doi.org/10.2478/aiht-2020-71-3301.

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AbstractCannabis sativa L. contains more than 100 phytocannabinoids that can interact with cannabinoid receptors CB1 and CB2. None of the cannabinoid receptor ligands is entirely CB1- or CB2-specific. The effects of cannabinoids therefore differ not just because of different potency at cannabinoid receptors but also because they can interact with other non-CB1 and non-CB2 targets, such as TRPV1, GPR55, and GPR119. The most studied phytocannabinoid is Δ9-tetrahydrocannabinol (THC). THC is a partial agonist at both cannabinoid receptors, but its psychotomimetic effect is produced primarily via a

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Barth, Francis, and Murielle Rinaldi-Carmona. "The Development of Cannabinoid Antagonists." Current Medicinal Chemistry 6, no. 8 (1999): 745–55. http://dx.doi.org/10.2174/0929867306666220401143808.

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The discovery of two distinct cannabinoid receptors (CB1 and C B 2 ) in the early 1990's has revived the research on cannabinoid antagonists. While the search for antagonists based on the structure of agonists (classical cannabinoids or aminoalkylindoles) appeared rather disappointing, the first potent cannabinoid antagonists were developed in a new chemical series: the diarylpyrazoles. Since its discovery in 1994, the selective CB1 antagonist SR 141716 has become a major pharmacological tool to elucidate the physiological role of the CB 1 cannabinoid receptor and its endogenous ligand. The se

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Simoneau, Isabelle I., Maged S. Hamza, Heriberto P. Mata, et al. "The Cannabinoid Agonist WIN55,212-2 Suppresses Opioid-induced Emesis in Ferrets." Anesthesiology 94, no. 5 (2001): 882–87. http://dx.doi.org/10.1097/00000542-200105000-00029.

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Background Cannabinoid receptor agonists reverse nausea and vomiting produced by chemotherapy and radiation therapy in animals and humans but have not been tested against opioid-induced emesis. This study tests the hypothesis that cannabinoid receptor agonists will prevent opioid-induced vomiting. Methods Twelve male ferrets were used. They weighed 1.2-1.6 kg at the beginning and 1.8-2.3 kg at the end of the experiments. All drugs were injected subcutaneously. WIN55,212-2, a mixed CB1-CB2 cannabinoid receptor agonist, was administered 25 min before morphine. Retches and vomits were counted at

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Wu, Yan-ran, Jia-qin Tang, Wan-nian Zhang, Chun-lin Zhuang, and Ying Shi. "Rational drug design of CB2 receptor ligands: from 2012 to 2021." RSC Advances 12, no. 54 (2022): 35242–59. http://dx.doi.org/10.1039/d2ra05661e.

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Senkiv, J., A. Kryshchyshyn-Dylevych, D. Khylyuk, et al. "Novel putative ligands of cannabinoid receptors: synthesis and effects on cell signaling and neuronal functions." Ukrainian Biochemical Journal 95, no. 1 (2023): 31–43. http://dx.doi.org/10.15407/ubj95.01.031.

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Cannabinoid ligands are known to possess neuroprotective actions and may have utility in the treatment of neurodegeneration. The major targets for cannabinoids include the classical CB1 cannabinoid receptor, as well as the novel cannabinoid receptor GPR55 which binds to many synthetic cannabinoid ligands. In this study, novel thiopyranothiazoles 1, 3, 4, 6, and 7 were synthesized and their pharmacological activity as potential cannabinoid-like ligands was evaluated in glioblastoma cells, cultured cortical neurons, and cells of HEK293 line expressing GPR55. Stimulation of protein kinase ERK1/2,

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Andrzejewska, Angelika, Klaudia Staszak, Marta Kaczmarek-Ryś, Ryszard Słomski, and Szymon Hryhorowicz. "Understanding cannabinoid receptors: structure and function." Folia Biologica et Oecologica 14 (December 30, 2018): 1–13. http://dx.doi.org/10.1515/fobio-2017-0004.

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The endocannabinoid system (ECS) consists of the endocannabinoids, cannabinoid receptors and the enzymes that synthesize and degrade endocannabinoids. The whole EC system plays an important role in the proper functioning of the central and autonomic nervous system. ECS is involved in the regulation of the body energy and in the functioning of the endocrine system. It can affect on the regulation of emotional states, motoric movement, operations of the endocrine, immune and digestive system. Many of the effects of cannabinoids are mediated by G coupled –protein receptors: CB1, CB2 and GPR55 but

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Gorberg, Victoria, Tamar Harpaz, Emilya Natali Shamir, et al. "A Tourette Syndrome/ADHD-like Phenotype Results from Postnatal Disruption of CB1 and CB2 Receptor Signalling." International Journal of Molecular Sciences 26, no. 13 (2025): 6052. https://doi.org/10.3390/ijms26136052.

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Cannabinoid receptor 1 (CB1) signalling is critical for weight gain and for milk intake in newborn pups. This is important as in humans, low birth weight increases the risk for attention-deficit hyperactivity disorder (ADHD). Moreover, some children with ADHD also have Tourette syndrome (TS). However, it remains unclear if insufficient CB1 receptor signalling may promote ADHD/TS-like behaviours. Here, ADHD/TS-like behaviours were studied from postnatal to adulthood by exposing postnatal wild-type CB1 and Cannabinoid receptor 2 (CB2) knockout mouse pups to SR141716A (rimonabant), a CB1 receptor

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Ye, Lingyan, Zheng Cao, Weiwei Wang, and Naiming Zhou. "New Insights in Cannabinoid Receptor Structure and Signaling." Current Molecular Pharmacology 12, no. 3 (2019): 239–48. http://dx.doi.org/10.2174/1874467212666190215112036.

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Background: Cannabinoid has long been used for medicinal purposes. Cannabinoid signaling has been considered the therapeutic target for treating pain, addiction, obesity, inflammation, and other diseases. Recent studies have suggested that in addition to CB1 and CB2, there are non-CB1 and non-CB2 cannabinoid-related orphan GPCRs including GPR18, GPR55, and GPR119. In addition, CB1 and CB2 display allosteric binding and biased signaling, revealing correlations between biased signaling and functional outcomes. Interestingly, new investigations have indicated that CB1 is functionally present with

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Ellert-Miklaszewska, Aleksandra, Iwona Anna Ciechomska, and Bozena Kaminska. "Synthetic Cannabinoids Induce Autophagy and Mitochondrial Apoptotic Pathways in Human Glioblastoma Cells Independently of Deficiency in TP53 or PTEN Tumor Suppressors." Cancers 13, no. 3 (2021): 419. http://dx.doi.org/10.3390/cancers13030419.

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Glioblastomas (GBMs) are aggressive brain tumors with frequent genetic alterations in TP53 and PTEN tumor suppressor genes rendering resistance to standard chemotherapeutics. Cannabinoid type 1 and 2 (CB1/CB2) receptor expression in GBMs and antitumor activity of cannabinoids in glioma cells and animal models, raised promises for a targeted treatment of these tumors. The susceptibility of human glioma cells to CB2-agonists and their mechanism of action are not fully elucidated. We determined CB1 and CB2 expression in 14 low-grade and 21 high-grade tumor biopsies, GBM-derived primary cultures a

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Rohbeck, Elisabeth, Juergen Eckel, and Tania Romacho. "Cannabinoid Receptors in Metabolic Regulation and Diabetes." Physiology 36, no. 2 (2021): 102–13. http://dx.doi.org/10.1152/physiol.00029.2020.

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There is an urgent need for developing effective drugs to combat the obesity and Type 2 diabetes mellitus epidemics. The endocannabinoid system plays a major role in energy homeostasis. It comprises the cannabinoid receptors 1 and 2 (CB1 and CB2), endogenous ligands called endocannabinoids and their metabolizing enzymes. Because the CB1 receptor is overactivated in metabolic alterations, pharmacological blockade of the CB1 receptor arose as a promising candidate to treat obesity. However, because of the wide distribution of CB1 receptors in the central nervous system, their negative central ef

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Potenzieri, Carl, Thaddeus S. Brink, Cholawat Pacharinsak та Donald A. Simone. "Cannabinoid Modulation of Cutaneous Aδ Nociceptors During Inflammation". Journal of Neurophysiology 100, № 5 (2008): 2794–806. http://dx.doi.org/10.1152/jn.90809.2008.

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Previous studies have demonstrated that locally administered cannabinoids attenuate allodynia and hyperalgesia through activation of peripheral cannabinoid receptors (CB1 and CB2). However, it is currently unknown if cannabinoids alter the response properties of nociceptors. In the present study, correlative behavioral and in vivo electrophysiological studies were conducted to determine if peripheral administration of the cannabinoid receptor agonists arachidonyl-2′-chloroethylamide (ACEA) or (R)-(+)-methanandamide (methAEA) could attenuate mechanical allodynia and hyperalgesia, and decrease m

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Howlett, Allyn C., Barbara Berglund, and Lawrence S. Melvin. "Cannabinoid Receptor Agonists and Antagonists." Current Pharmaceutical Design 1, no. 3 (1995): 343–54. http://dx.doi.org/10.2174/1381612801666220918164118.

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Research on the cannabinoid natural products and synthetic drugs has been bolstered recently by major breakthroughs in the understanding of the biochemical pathways and the production of significant new tools in the form of novel chemical structures. Cannabinoid receptors are now defined pharmacologically, anatomically, and at the molecular level as belonging to the seven transmembrane spanning G protein coupled receptor superfarnily. Currently recognized receptor subtypes include the CB1 and CBJ(a) splice variants, found predominantly in the brain, and the CB2 subtype, identified in cells of

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Asproni, Battistina, Gabriele Murineddu, Paola Corona, and Gérard A. Pinna. "Tricyclic Pyrazole-Based Compounds as Useful Scaffolds for Cannabinoid CB1/CB2 Receptor Interaction." Molecules 26, no. 8 (2021): 2126. http://dx.doi.org/10.3390/molecules26082126.

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Cannabinoids comprise different classes of compounds, which aroused interest in recent years because of their several pharmacological properties. Such properties include analgesic activity, bodyweight reduction, the antiemetic effect, the reduction of intraocular pressure and many others, which appear correlated to the affinity of cannabinoids towards CB1 and/or CB2 receptors. Within the search aiming to identify novel chemical scaffolds for cannabinoid receptor interaction, the CB1 antagonist/inverse agonist pyrazole-based derivative rimonabant has been modified, giving rise to several tricyc

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Zhang, Xuefeng, Jian Feng Wang, Yehoshua Maor, George Kunos, and Jerome E. Groopman. "Endogenous Cannabinoid-Like Arachidonoyl Serine Induces Angiogenesis through Novel Pathways." Blood 106, no. 11 (2005): 3690. http://dx.doi.org/10.1182/blood.v106.11.3690.3690.

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Abstract Cannabinoid effects on the central nervous system have been well-described and include altered cognition, memory, motor function, and concentration. Studies have also shown that marijuana and its primary active constituent, THC (Tetrahydrocannabinol), can be salubrious in treating diverse medical conditions such as chemotherapy-induced nausea, HIV cachexia, glaucoma, and chronic pain. Recently, cannabinoids have been shown in animal models to inhibit the growth and metastasis of certain tumors through their effects on angiogenesis. There are also animal data showing that cannabinoids

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Maslov, L. N., and R. S. Karpov. "Prospects for the Use of Cannabinoid Receptor Ligands for the Treatment of Metabolic Syndrome and Atherosclerosis: Analysis of Experimental and Clinical Data." Annals of the Russian academy of medical sciences 72, no. 1 (2017): 59–65. http://dx.doi.org/10.15690/vramn779.

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An antagonist of central cannabinoid CB1 receptors rimonabant causes weight loss in patients with obesity and metabolic syndrome, improves blood lipid parameters, increases the adiponectin level, decreases the rate of glucose and glycosylated hemoglobin in patients with diabetes mellitustype-2. However, rimonabant adverse effects include depression, anxiety, nausea, and dizziness which are apparently due to the blockade of central CB1 receptors. In mice with a high-calorie diet, we defined that the blockade of peripheral CB1 receptors prevents obesity, steatosis of the liver, improves lipid an

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Tang, Xinru, Zheng Liu, Xiaoqing Li, Jing Wang, and Liliang Li. "Cannabinoid Receptors in Myocardial Injury: A Brother Born to Rival." International Journal of Molecular Sciences 22, no. 13 (2021): 6886. http://dx.doi.org/10.3390/ijms22136886.

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Cannabinoid receptors typically include type 1 (CB1) and type 2 (CB2), and they have attracted extensive attention in the central nervous system (CNS) and immune system. Due to more in-depth studies in recent years, it has been found that the typical CB1 and CB2 receptors confer functional importance far beyond the CNS and immune system. In particular, many works have reported the critical involvement of the CB1 and CB2 receptors in myocardial injuries. Both pharmacological and genetic approaches have been used for studying CB1 and CB2 functions in these studies, revealing that the brother rec

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Sapundzhi, Fatima, Tatyana Dzimbova, Nevena Pencheva, and Peter Milanov. "Computer modeling of Cannabinoid receptor type 1." ITM Web of Conferences 16 (2018): 02008. http://dx.doi.org/10.1051/itmconf/20181602008.

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Cannabinoid receptors are important class of receptors as they are involved in various physiological processes such as appetite, pain-sensation, mood, and memory. It is important to design receptor-selective ligands in order to treat a particular disorder. The aim of the present study is to model the structure of cannabinoid receptor CB1 and to perform docking between obtained models and known ligands. Two models of CBR1 were prepared with two different methods (Modeller of Chimera and MOE). They were used for docking with GOLD 5.2. It was established a high correlation between inhibitory cons

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Ji, Xiaoyu, Yang Zeng, and Jie Wu. "The CB2 Receptor as a Novel Therapeutic Target for Epilepsy Treatment." International Journal of Molecular Sciences 22, no. 16 (2021): 8961. http://dx.doi.org/10.3390/ijms22168961.

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Epilepsy is characterized by repeated spontaneous bursts of neuronal hyperactivity and high synchronization in the central nervous system. It seriously affects the quality of life of epileptic patients, and nearly 30% of individuals are refractory to treatment of antiseizure drugs. Therefore, there is an urgent need to develop new drugs to manage and control refractory epilepsy. Cannabinoid ligands, including selective cannabinoid receptor subtype (CB1 or CB2 receptor) ligands and non-selective cannabinoid (synthetic and endogenous) ligands, may serve as novel candidates for this need. Cannabi

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Silva, Guillermo B., Douglas K. Atchison, Luis I. Juncos, and Néstor H. García. "Anandamide inhibits transport-related oxygen consumption in the loop of Henle by activating CB1 receptors." American Journal of Physiology-Renal Physiology 304, no. 4 (2013): F376—F381. http://dx.doi.org/10.1152/ajprenal.00239.2012.

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The energy required for active Na chloride reabsorption in the thick ascending limb (TAL) depends on oxygen consumption and oxidative phosphorylation (OXP). In other cells, Na transport is inhibited by the endogenous cannabinoid anandamide through the activation of the cannabinoid receptors (CB) type 1 and 2. However, it is unclear whether anandamide alters TAL transport and the mechanisms that could be involved. We hypothesized that anandamide inhibits TAL transport via activation of CB1 receptors and NO. For this, we measured oxygen consumption (QO2) in TAL suspensions to monitor the anandam

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Sun, Y., S. P. H. Alexander, D. A. Kendall та A. J. Bennett. "Cannabinoids and PPARα signalling". Biochemical Society Transactions 34, № 6 (2006): 1095–97. http://dx.doi.org/10.1042/bst0341095.

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Cannabinoids have been shown to possess anti-inflammatory and neuroprotective properties, which were proposed to occur mainly via activation of the G-protein-coupled receptor CB1 (cannabinoid receptor 1). Recently, certain cannabinoids have been reported to be ligands for members of the nuclear receptor transcription factor superfamily known as PPARs (peroxisome-proliferator-activated receptors). This review summarizes the evidence for cannabinoid activation of PPARs and identifies a new intracellular target for cannabinoids as therapeutic agents for neuroprotective treatment.

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Qhabibi, Faqrizal Ria. "THE MAIN ROLE OF DELTA-9-TETRAHYDROCANNABINOL (THC) TO DOWNREGULATE AN EXPRESSION OF CANNABINOID 1 (CB1) RECEPTOR IN CANNABIS WITHDRAWAL SYNDROME." Journal of Psychiatry Psychology and Behavioral Research 6, no. 1 (2025): 36–41. https://doi.org/10.21776/ub.jppbr.2025.006.01.8.

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Introduction – Cannabinoids from Cannabis sativa have derived compounds that are the best characterized like delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD) as the main psychogenic compounds from Cannabis sativa. In addition, THC is an important agonist for the CB1 receptors and has a responsibility to develop cannabis withdrawal. This paper aims to reveal the role of delta-9-tetrahydrocannabinol (THC) to downregulate an expression of cannabinoid 1 (CB1) receptor and their correlation to developing cannabis withdrawal syndrome. Methods – A literature review evaluating the role of delt

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Haddad, Mansour. "The Impact of CB1 Receptor on Nuclear Receptors in Skeletal Muscle Cells." Pathophysiology 28, no. 4 (2021): 457–70. http://dx.doi.org/10.3390/pathophysiology28040029.

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Cannabinoids are abundant signaling compounds; their influence predominantly arises via engagement with the principal two G-protein-coupled cannabinoid receptors, CB1 and CB2. One suggested theory is that cannabinoids regulate a variety of physiological processes within the cells of skeletal muscle. Earlier publications have indicated that expression of CB1 receptor mRNA and protein has been recognized within myotubes and tissues of skeletal muscle from both murines and humans, thus representing a potentially significant pathway which plays a role in the control of skeletal muscular activities

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Sachdev, Shivani, Rochelle Boyd, Natasha L. Grimsey, Marina Santiago, and Mark Connor. "Brodifacoum does not modulate human cannabinoid receptor-mediated hyperpolarization of AtT20 cells or inhibition of adenylyl cyclase in HEK 293 cells." PeerJ 7 (September 25, 2019): e7733. http://dx.doi.org/10.7717/peerj.7733.

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BackgroundSynthetic cannabinoids are a commonly used class of recreational drugs that can have significant adverse effects. There have been sporadic reports of co-consumption of illicit drugs with rodenticides such as warfarin and brodifacoum (BFC) over the past 20 years but recently, hundreds of people have been reported to have been poisoned with a mixture of synthetic cannabinoids and BFC. We have sought to establish whether BFC directly affects cannabinoid receptors, or their activation by the synthetic cannabinoid CP55940 or the phytocannabinoid Δ9-tetrahydrocannabinol (Δ9-THC).MethodsThe

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Rathod, Sumit S., Yogeeta O. Agrawal, Kartik T. Nakhate, M. F. Nagoor Meeran, Shreesh Ojha, and Sameer N. Goyal. "Neuroinflammation in the Central Nervous System: Exploring the Evolving Influence of Endocannabinoid System." Biomedicines 11, no. 10 (2023): 2642. http://dx.doi.org/10.3390/biomedicines11102642.

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Neuroinflammation is a complex biological process that typically originates as a protective response in the brain. This inflammatory process is triggered by the release of pro-inflammatory substances like cytokines, prostaglandins, and reactive oxygen and nitrogen species from stimulated endothelial and glial cells, including those with pro-inflammatory functions, in the outer regions. While neuronal inflammation is common in various central nervous system disorders, the specific inflammatory pathways linked with different immune-mediated cell types and the various factors influencing the bloo

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Tsotsokou, Giota, Ioanna-Maria Sotiropoulou, Klearchos Stampolitis, George D. Oikonomou, Aikaterini-Paraskevi Avdi, and Costas Papatheodoropoulos. "Cannabinoid Modulation of Excitability and Short-Term Neuronal Dynamics in the Dorsal and Ventral Hippocampus." Biology 14, no. 6 (2025): 642. https://doi.org/10.3390/biology14060642.

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Endocannabinoids, acting primarily through CB1 receptors, are critical modulators of neuronal activity, influencing cognitive functions and emotional processing. CB1 receptors are highly expressed in the hippocampus, primarily on GABAergic interneurons, modulating the excitation/inhibition balance. Previous evidence suggests the functional heterogeneity of CB1 receptors along the dorsoventral axis of the hippocampus. However, it is not known whether CB1 receptors differentially modulate basic aspects of the local neuronal network along the hippocampus. This study investigated how CB1 receptor

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Twitchell, W., S. Brown, and K. Mackie. "Cannabinoids Inhibit N- and P/Q-Type Calcium Channels in Cultured Rat Hippocampal Neurons." Journal of Neurophysiology 78, no. 1 (1997): 43–50. http://dx.doi.org/10.1152/jn.1997.78.1.43.

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Twitchell, W., S. Brown, and K. Mackie. Cannabinoids inhibit N- and P/Q-type calcium channels in cultured rat hippocampal neurons. J. Neurophysiol. 78: 43–50, 1997. Cannabinoids and their analogues have been found to inhibit N- and P/Q-type Ca2+ currents in cell lines and sympathetic neurons transfected with cannabinoid CB1 receptor. However, the effects of cannabinoids on Ca2+ currents in the CNS are largely unexplored. In this study we investigated whether these compounds inhibit Ca2+ channels in cultured rat hippocampal neurons. With the use of antibodies directed against the amino-terminus

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Orazbekov, Yerkebulan, Mohamed A. Ibrahim, Serjan Mombekov, et al. "Isolation and Biological Evaluation of Prenylated Flavonoids from Maclura pomifera." Evidence-Based Complementary and Alternative Medicine 2018 (2018): 1–8. http://dx.doi.org/10.1155/2018/1370368.

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Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds (I–IV) along with eleven known compounds (V–XV). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (−49.7 and −53.8% displacement, resp.). Compound I was found to be possibly allosteric for κ and μ opioid receptors (−88.4 and −27.2% displacement, resp.) and showed moderate activity (60.5% displacement) towards CB1 receptor. Compound II exhibited mod

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Xu, Kangtai, Yifei Wu, Zhuangzhuang Tian, Yuanfan Xu, Chaoran Wu, and Zilong Wang. "Microglial Cannabinoid CB2 Receptors in Pain Modulation." International Journal of Molecular Sciences 24, no. 3 (2023): 2348. http://dx.doi.org/10.3390/ijms24032348.

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Pain, especially chronic pain, can strongly affect patients’ quality of life. Cannabinoids ponhave been reported to produce potent analgesic effects in different preclinical pain models, where they primarily function as agonists of Gi/o protein-coupled cannabinoid CB1 and CB2 receptors. The CB1 receptors are abundantly expressed in both the peripheral and central nervous systems. The central activation of CB1 receptors is strongly associated with psychotropic adverse effects, thus largely limiting its therapeutic potential. However, the CB2 receptors are promising targets for pain treatment wi

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Takheaw, Nuchjira, Kanyaruck Jindaphun, Supansa Pata, Witida Laopajon, and Watchara Kasinrerk. "Cannabinoid Receptor 1 Agonist ACEA and Cannabinoid Receptor 2 Agonist GW833972A Attenuates Cell-Mediated Immunity by Different Biological Mechanisms." Cells 12, no. 6 (2023): 848. http://dx.doi.org/10.3390/cells12060848.

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Cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) are components in the endocannabinoid system that play significant roles in regulating immune responses. There are many agonists for the cannabinoid receptors; however, their effects on T cell regulation have not been elucidated. In the present study, we determined the effects of the CB1 selective agonist ACEA and the CB2 selective agonist GW833972A on T cell responses. It was found that both agonists impaired anti-CD3 monoclonal antibody induced T cell proliferation. However, ACEA and GW833972A agonists down-regulated the expressio

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Quartilho, Aline, Heriberto P. Mata, Mohab M. Ibrahim, et al. "Inhibition of Inflammatory Hyperalgesia by Activation of Peripheral CB2Cannabinoid Receptors." Anesthesiology 99, no. 4 (2003): 955–60. http://dx.doi.org/10.1097/00000542-200310000-00031.

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Background Cannabinoid receptor agonists inhibit inflammatory hyperalgesia in animal models. Nonselective cannabinoid receptor agonists also produce central nervous system (CNS) side effects. Agonists selective for CB2 cannabinoid receptors, which are not found in the CNS, do not produce the CNS effects typical of nonselective cannabinoid receptor agonists but do inhibit acute nociception. The authors used the CB2 receptor-selective agonist AM1241 to test the hypothesis that selective activation of peripheral CB2 receptors inhibits inflammatory hyperalgesia. Methods Rats were injected in the h

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Yang, Yi, Rupali Vyawahare, Melissa Lewis-Bakker, Hance A. Clarke, Albert H. C. Wong, and Lakshmi P. Kotra. "Bioactive Chemical Composition of Cannabis Extracts and Cannabinoid Receptors." Molecules 25, no. 15 (2020): 3466. http://dx.doi.org/10.3390/molecules25153466.

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Cannabis is widely used as a therapeutic drug, especially by patients suffering from psychiatric and neurodegenerative diseases. However, the complex interplay between phytocannabinoids and their targets in the human receptome remains largely a mystery, and there have been few investigations into the relationship between the chemical composition of medical cannabis and the corresponding biological activity. In this study, we investigated 59 cannabis samples used by patients for medical reasons. The samples were subjected to extraction (microwave and supercritical carbon dioxide) and chemical a

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Braile, Mariantonia, Simone Marcella, Gianni Marone, Maria Rosaria Galdiero, Gilda Varricchi, and Stefania Loffredo. "The Interplay between the Immune and the Endocannabinoid Systems in Cancer." Cells 10, no. 6 (2021): 1282. http://dx.doi.org/10.3390/cells10061282.

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The therapeutic potential of Cannabis sativa has been recognized since ancient times. Phytocannabinoids, endocannabinoids and synthetic cannabinoids activate two major G protein-coupled receptors, subtype 1 and 2 (CB1 and CB2). Cannabinoids (CBs) modulate several aspects of cancer cells, such as apoptosis, autophagy, proliferation, migration, epithelial-to-mesenchymal transition and stemness. Moreover, agonists of CB1 and CB2 receptors inhibit angiogenesis and lymphangiogenesis in vitro and in vivo. Low-grade inflammation is a hallmark of cancer in the tumor microenvironment (TME), which conta

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Hossain, Mohammad Zakir, Hiroshi Ando, Shumpei Unno, and Junichi Kitagawa. "Targeting Peripherally Restricted Cannabinoid Receptor 1, Cannabinoid Receptor 2, and Endocannabinoid-Degrading Enzymes for the Treatment of Neuropathic Pain Including Neuropathic Orofacial Pain." International Journal of Molecular Sciences 21, no. 4 (2020): 1423. http://dx.doi.org/10.3390/ijms21041423.

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Neuropathic pain conditions including neuropathic orofacial pain (NOP) are difficult to treat. Contemporary therapeutic agents for neuropathic pain are often ineffective in relieving pain and are associated with various adverse effects. Finding new options for treating neuropathic pain is a major priority in pain-related research. Cannabinoid-based therapeutic strategies have emerged as promising new options. Cannabinoids mainly act on cannabinoid 1 (CB1) and 2 (CB2) receptors, and the former is widely distributed in the brain. The therapeutic significance of cannabinoids is masked by their ad

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Huffman, J. W. "Cannabimimetic lndoles, Pyrroles and lndenes." Current Medicinal Chemistry 6, no. 8 (1999): 705–20. http://dx.doi.org/10.2174/0929867306666220401125055.

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In the course of efforts to develop new nonsteroidal antiinflammatory agents, it was discovered that 1-aminoalkyl-3-aroylindoles have affinity for the cannabinoid brain (CB1 ) receptor. This led to the synthesis of well over 100 cannabimimetic aminoalkylindoles by the group at Sterling Winthrop, and to the development of structure-activity relationships (SAR) for these compounds. These SAR require a heterocyclic aminoethyl group attached to the indole nitrogen, and a 1-naphthoyl group at C-3 for significant receptor affinity. Other workers subsequently demonstrated that an aminoalkyl group was

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Di MARZO, Vincenzo, Dominique MELCK, Pierangelo ORLANDO, et al. "Palmitoylethanolamide inhibits the expression of fatty acid amide hydrolase and enhances the anti-proliferative effect of anandamide in human breast cancer cells." Biochemical Journal 358, no. 1 (2001): 249–55. http://dx.doi.org/10.1042/bj3580249.

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Palmitoylethanolamide (PEA) has been shown to act in synergy with anandamide (arachidonoylethanolamide; AEA), an endogenous agonist of cannabinoid receptor type 1 (CB1). This synergistic effect was reduced by the CB2 cannabinoid receptor antagonist SR144528, although PEA does not activate either CB1 or CB2 receptors. Here we show that PEA potently enhances the anti-proliferative effects of AEA on human breast cancer cells (HBCCs), in part by inhibiting the expression of fatty acid amide hydrolase (FAAH), the major enzyme catalysing AEA degradation. PEA (1–10μM) enhanced in a dose-related manne

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Pagano Zottola, Antonio C., Ilenia Severi, Astrid Cannich, et al. "Expression of Functional Cannabinoid Type-1 (CB1) Receptor in Mitochondria of White Adipocytes." Cells 11, no. 16 (2022): 2582. http://dx.doi.org/10.3390/cells11162582.

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Via activation of the cannabinoid type-1 (CB1) receptor, endogenous and exogenous cannabinoids modulate important biochemical and cellular processes in adipocytes. Several pieces of evidence suggest that alterations of mitochondrial physiology might be a possible mechanism underlying cannabinoids’ effects on adipocyte biology. Many reports suggest the presence of CB1 receptor mRNA in both white and brown adipose tissue, but the detailed subcellular localization of CB1 protein in adipose cells has so far been scarcely addressed. In this study, we show the presence of the functional CB1 receptor

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Kelly, Sara, and Victoria Chapman. "Selective Cannabinoid CB1 Receptor Activation Inhibits Spinal Nociceptive Transmission In Vivo." Journal of Neurophysiology 86, no. 6 (2001): 3061–64. http://dx.doi.org/10.1152/jn.2001.86.6.3061.

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Cannabinoid1 (CB1) receptors are located at CNS sites, including the spinal cord, involved in somatosensory processing. Analgesia is one of the tetrad of behaviors associated with cannabinoid agonists. Here, effects of a potent cannabinoid CB1 receptor agonist arachidonyl-2-chloroethylamide (ACEA) on evoked responses of dorsal horn neurons in anesthetized rats were investigated. Extracellular recordings of convergent dorsal horn neurons were made in halothane anesthetized Sprague-Dawley rats ( n = 16). Effects of spinal application of ACEA on electrically evoked responses of dorsal horn neuron

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Benyó, Zoltán, Éva Ruisanchez, Miriam Leszl-Ishiguro, Péter Sándor, and Pál Pacher. "Endocannabinoids in cerebrovascular regulation." American Journal of Physiology-Heart and Circulatory Physiology 310, no. 7 (2016): H785—H801. http://dx.doi.org/10.1152/ajpheart.00571.2015.

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The cerebral blood flow is tightly regulated by myogenic, endothelial, metabolic, and neural mechanisms under physiological conditions, and a large body of recent evidence indicates that inflammatory pathways have a major influence on the cerebral blood perfusion in certain central nervous system disorders, like hemorrhagic and ischemic stroke, traumatic brain injury, and vascular dementia. All major cell types involved in cerebrovascular control pathways (i.e., smooth muscle, endothelium, neurons, astrocytes, pericytes, microglia, and leukocytes) are capable of synthesizing endocannabinoids a

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Marini, Pietro, Philip Cowie, Ahmet Ayar, et al. "M3 Receptor Pathway Stimulates Rapid Transcription of the CB1 Receptor Activation through Calcium Signalling and the CNR1 Gene Promoter." International Journal of Molecular Sciences 24, no. 2 (2023): 1308. http://dx.doi.org/10.3390/ijms24021308.

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In this study, we have investigated a possible mechanism that enables CB1/M3 receptor cross-talk, using SH-SY5Y cells as a model system. Our results show that M3 receptor activation initiates signaling that rapidly upregulates the CNR1 gene, resulting in a greatly potentiated CB1 receptor response to agonists. Calcium homeostasis plays an essential intermediary role in this functional CB1/M3 receptor cross-talk. We show that M3 receptor-triggered calcium release greatly increases CB1 receptor expression via both transcriptional and translational activity, by enhancing CNR1 promoter activity. T

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Hughes, Hallmon Victoria, and Victoria Hughes. "Effects of Cannabidiol on Dugesia Dorotocephala Head Regeneration." Athens Journal of Health and Medical Sciences 9, no. 2 (2022): 87–94. http://dx.doi.org/10.30958/ajhms.9-2-2.

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The endocannabinoid system regulates synaptic transmissions. It is comprised of two G protein-coupled receptors, cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2), a degradation system and the endocannabinoids, a group of lipidic ligands. The connection between JNK, cannabinoids, and regeneration has led to the hypothesis that cannabinoids impact both regeneration and the levels of the enzymes required for the regenerative process. Thus, by encouraging neoblasts to enter the M phase, cannabinoids would speed up effective regeneration. These regeneration pathways may have implicatio

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Vieira, Graziela, Juliana Cavalli, Elaine C. D. Gonçalves, et al. "Antidepressant-Like Effect of Terpineol in an Inflammatory Model of Depression: Involvement of the Cannabinoid System and D2 Dopamine Receptor." Biomolecules 10, no. 5 (2020): 792. http://dx.doi.org/10.3390/biom10050792.

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Depression has a multifactorial etiology that arises from environmental, psychological, genetic, and biological factors. Environmental stress and genetic factors acting through immunological and endocrine responses generate structural and functional changes in the brain, inducing neurogenesis and neurotransmission dysfunction. Terpineol, monoterpenoid alcohol, has shown immunomodulatory and neuroprotective effects, but there is no report about its antidepressant potential. Herein, we used a single lipopolysaccharide (LPS) injection to induce a depressive-like effect in the tail suspension test

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YAZULLA, STEPHEN, KEITH M. STUDHOLME, HELEN H. McINTOSH, and SHIH-FANG FAN. "Cannabinoid receptors on goldfish retinal bipolar cells: Electron-microscope immunocytochemistry and whole-cell recordings." Visual Neuroscience 17, no. 3 (2000): 391–401. http://dx.doi.org/10.1017/s0952523800173079.

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Cannabinoid CB1 receptors are distributed throughout the CNS and interact with GABA, glutamate, and dopamine systems. Cannabinoids have effects on the visual system, some of which may have a retinal component, particularly the enhancement of photosensitivity. We used immunocytochemistry and whole-cell recording to study cannabinoids in the goldfish retina. Immunoblots of an antiserum against amino acids (1-14) of the rat CB1 receptor produced a single band in goldfish retina at about 70 kDa. Light microscope immunocytochemistry of CB1 receptor immunoreactivity (CB1R-IR) revealed intense staini

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