Review
Neurosciences
Sai Varshini Magham, Praveen Thaggikuppe Krishnamurthy, Neenu Shaji, Lalithkumar Mani, Shivaramakrishnan Balasubramanian
Summary: The endocannabinoid system, particularly the CB2 receptor, has unique neuroprotective properties in neuroinflammation, making it a significant focus of research in neurodegenerative disorders like Alzheimer's disease.
JOURNAL OF NEUROSCIENCE RESEARCH
(2021)
Review
Neurosciences
Andrea S. Heimann, Camila S. Dale, Francisco S. Guimaraes, Ricardo A. M. Reis, Ami Navon, Michal A. Shmuelov, Vanessa Rioli, Ivone Gomes, Lakshmi L. Devi, Emer S. Ferro
Summary: Hemopressin, derived from hemoglobin alpha-chain, exhibits diverse cannabinoid receptor activities and may have pharmacological effects by interacting with intracellular mitochondrial cannabinoid receptors. The peptide influences physiological processes such as pain, inflammation, appetite, learning, and memory, and shows potential applications in drug delivery systems.
Review
Biochemistry & Molecular Biology
Kangtai Xu, Yifei Wu, Zhuangzhuang Tian, Yuanfan Xu, Chaoran Wu, Zilong Wang
Summary: Pain, especially chronic pain, has a significant impact on patients' quality of life. Cannabinoids have shown potent analgesic effects in preclinical pain models by acting as agonists of CB1 and CB2 receptors. While the activation of CB1 receptors is associated with psychotropic adverse effects, the promising target for pain treatment is the CB2 receptors primarily expressed in immune cells. Microglia, as resident immune cells in the central nervous system, play a critical role in chronic pain, and CB2 receptors regulate their activity and function. This review focuses on the role of microglial CB2 receptors in spinal nociceptive circuitry and their implications for selective CB2 receptor agonist-mediated analgesia.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Cell Biology
Fabio Arturo Iannotti, Rosa Maria Vitale
Summary: PPARs are a family of nuclear receptors that regulate the expression of target genes involved in metabolism, immune reaction, cell differentiation, and other cellular changes. They are activated by various lipid molecules, including cannabinoids, and interact with the endocannabinoid system to modulate physiological and pathophysiological functions.
Review
Pharmacology & Pharmacy
Jian-Yu Chen, Xiao-Yun Tian, Shan-Shan Wei, Ying-Jie Yang, Shan Deng, Chun-Jie Jiao, Can-Jian Wang, Ke-Dan Chu, Xue-Qin Ma, Wei Xu
Summary: JAK/STAT signaling pathways play a critical role in regulating various biological processes and their abnormal activation is associated with disease progression. FDA-approved JAK/STAT inhibitors, such as tofacitinib and baricitinib, have shown promising results in rheumatology treatment.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Barbara Vuic, Tina Milos, Lucija Tudor, Marcela Konjevod, Matea Nikolac Perkovic, Maja Jazvinscak Jembrek, Gordana Nedic Erjavec, Dubravka Svob Strac
Summary: Neurodegenerative diseases, characterized by protein aggregation in the brain, can be influenced by the activation of CB2 receptors in the endocannabinoid system. Studies suggest that activating CB2 receptors has potential benefits in reducing protein aggregation-based pathology, attenuating inflammation, and alleviating dementia-related symptoms.
Article
Chemistry, Medicinal
Daniel Gundel, Winnie Deuther-Conrad, Lea Ueberham, Sarandeep Kaur, Elina Otikova, Rodrigo Teodoro, Magali Toussaint, Thu Hang Lai, Oliver Clauss, Matthias Scheunemann, Guy Bormans, Michael Bachmann, Klaus Kopka, Peter Brust, Rares-Petru Moldovan
Summary: The cannabinoid receptor type 2 (CB2R) is an ideal target for the diagnosis and therapy of neurodegenerative diseases and cancer. This study introduces a novel F-18-labeled radioligand that can efficiently image upregulated CB2R expression.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Cell Biology
Nuchjira Takheaw, Kanyaruck Jindaphun, Supansa Pata, Witida Laopajon, Watchara Kasinrerk
Summary: Cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) are important components of the endocannabinoid system, which regulate immune responses. This study investigated the effects of CB1 selective agonist ACEA and CB2 selective agonist GW833972A on T cell responses. The results showed that both agonists inhibited T cell proliferation and down-regulated activation markers and co-stimulatory molecules on T cells, B cells, and monocytes in different ways. GW833972A also suppressed the cytotoxic activities of CD8(+) T cells without affecting CD4(+) T cells and NK cells. Moreover, only the CB2 agonist caused a reduction in Th1 cytokine production. These findings suggest that the CB1 and CB2 agonists may have therapeutic potential in modulating T cell function in inflammatory and autoimmune diseases.
Editorial Material
Neurosciences
Arnau Busquets-Garcia, Miriam Melis, Luigi Bellocchio, Giovanni Marsicano
Summary: This article introduces the wide expression and regulatory functions of the endocannabinoid system in both the brain and the periphery. It discusses the distribution of cannabinoid receptors in different cell types and compartments, and highlights the different cellular or molecular effects mediated by these receptors. The article also mentions the expression of the endocannabinoid system throughout the body and its role in modulating the connection between the brain and the periphery. Lastly, it emphasizes the importance of understanding the cannabinoid receptors structure and pharmacology for the development of novel allosteric modulators.
EUROPEAN JOURNAL OF NEUROSCIENCE
(2022)
Review
Medicine, Research & Experimental
Hebaallah Mamdouh Hashiesh, Charu Sharma, Sameer N. Goyal, Bassem Sadek, Niraj Kumar Jha, Juma Al Kaabi, Shreesh Ojha
Summary: BCP is a natural compound with selective agonist properties that activate CB2R and have various pharmacological effects. BCP shows protective effects in the heart, liver, nervous system, kidneys, gastrointestinal tract, cancer, with antioxidant, anti-inflammatory, and immunomodulatory actions.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Medicine, General & Internal
Saki Sultana, Geraint Berger, Christian Lehmann
Summary: Interstitial cystitis/bladder pain syndrome (IC/BPS) is a chronic condition with unknown etiology and limited treatment options. Modulating the endogenous cannabinoid system (ECS) has shown benefits in alleviating pain and inflammation associated with IC/BPS.
Review
Pharmacology & Pharmacy
Raphael Mechoulam
Summary: After experiencing a traumatic childhood in Europe during the Second World War, the author discovers the joy of scientific research in Israel. Over the past 65 years, the author has focused on studying the chemistry and pharmacology of natural products, particularly plant cannabinoids and endogenous anandamide-like compounds. Despite the approval of certain cannabinoids as drugs, the effects of endogenous cannabinoids and anandamide-like compounds in humans remain poorly researched. Intellectual freedom, the ability to pursue scientific interests, has been the most fulfilling aspect of the author's career. Looking back on their 91 years of life, the author considers themselves fortunate both personally and scientifically.
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY
(2023)
Article
Chemistry, Medicinal
Florian Mohr, Thomas Hurrle, Lindsey Burggraaff, Lukas Langer, Martijn P. Bemelmans, Maximilian Knab, Martin Nieger, Gerard J. P. van Westen, Laura H. Heitman, Stefan Braese
Summary: The study reports the development and evaluation of structure-activity relationship of a series of modified coumarins as cannabinoid receptor ligands. The most potent coumarins showed a CB2 selective agonistic profile with low nanomolar affinities, and several crucial structural requirements were identified through the research.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Jun-Fan Xie, Lin-Xin Wang, Wen-Ting Ren, Can Wang, Jin-Xian Gao, Hai-Lin Chen, Xue-Qi Zhao, Yan-Li Ren, Yu-Ping Xie, Yu-Feng Shao, Yi-Ping Hou
Summary: Hemopressin and related peptides act as endogenous ligands or regulators of cannabinoid receptors. This study investigates the effects of mVD-HPa on the sleep-wake cycle and cortical EEG in rats, and identifies the brain neurons activated by mVD-HPa. The results show that mVD-HPa promotes NREM sleep through CB1 receptors and activates VLPO GABAergic neurons, while inhibiting the activity of LH, LC, and TMN neurons.
FRONTIERS IN PHARMACOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Harmeet Gurm, Jeremy A. Hirota, Sandeep Raha
Summary: Despite its intricate involvement in various physiological processes, the endocannabinoid system remains one of the most under-studied biological systems in the human body. Cannabinoid receptors are widely distributed in reproductive tissues and are crucial for regulating immune-reproductive interactions, while excessive cannabis use during pregnancy may lead to clinical complications.