Pharmacological evaluation of new constituents of “Spice”: synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds Clara T. Schoeder, Cornelius Hess, Burkhard Madea, Jens Meiler, Christa E. Müller Forensic Toxicology, 2018, 36, 385-403. Doi : 10.1007/s11419-018-0415-z Abstract Purpose : In the present study we characterized a series of synthetic cannabinoids containing various heterocyclic scaffolds that had been identified as constituents of “Spice”, a preparation sold on the illicit drug market. All compounds were further investigated as potential ligands of the orphan receptors GPR18 and GPR55 that interact with some cannabinoids. Methods : The compounds were studied in radioligand binding assays to determine their affinity for [...]
Lire la suite5-HT1A receptors are involved in the cannabidiol-induced attenuation of behavioural and cardiovascular responses to acute restraint stress in rats Leonardo B.M. Resstel, Rodrigo F. Tavares, Sabrina F.S. Lisboa, Sâmia R.L. Joca, Fernando M.A. Corrêa and Francisco S. Guimarães British Journal of Pharmacology, 2009, 156, 181–188; doi : 10.1111/j.1476-5381.2008.00046.x Background and purpose : Cannabidiol (CBD) is a non-psychotomimetic compound from Cannabis sativa which induces anxiolytic- and antipsychotic-like effects in rodents. These effects could be mediated by facilitation of the endocannabinoid system or by the activation of 5-HT1A receptors. As either of these mechanisms could promote adaptation to inescapable stress, the aim of the present work [...]
Lire la suiteActivation of CB1R Promotes Lipopolysaccharide-Induced IL-10 Secretion by Monocytic Myeloid-Derived Suppressive Cells and Reduces Acute Inflammation and Organ Injury Jérémie Joffre, Che-Chung Yeh, Erika Wong, Mayuri Thete, Fengyun Xu, Ivana Zlatanova, Elliot Lloyd, Lester Kobzik, Matthieu Legrand, and Judith Hellman The Journal of Immunology, 2020, 204: 1–20. doi : 10.4049/jimmunol.2000213 Cannabis sativa and its principal components, D9-tetrahydrocannabinol (D9-THC) and cannabidiol, are increasingly being used to treat a variety of medical problems, including inflammatory conditions. Although studies suggest that the endocannabinoid system has immunomodulatory properties, there remains a paucity of information on the effects of cannabinoids on immunity and on outcomes of infection and injury. [...]
Lire la suiteBeneficial effects of the phytocannabinoid Δ9-THCV in L-DOPA-induced dyskinesia in Parkinson's disease Isabel Espadas, Ettel Keifman, Cristina Palomo-Garo Sonia Burgaz, Concepción García, Javier Fernández-Ruiz, Rosario Moratalla Neurobiology of Disease, 2020, 141, 104892 doi : 10.1016/j.nbd.2020.104892 A B S T R A C T The antioxidant and CB2 receptor agonist properties of Δ9-tetrahydrocannabivarin (Δ9-THCV) afforded neuroprotection in experimental Parkinson's disease (PD), whereas its CB1 receptor antagonist profile at doses lower than 5 mg/kg caused anti-hypokinetic effects. In the present study, we investigated the anti dyskinetic potential of Δ9-THCV (administered i.p. at 2 mg/kg for two weeks), which had not been investigated before. This objective was investigated [...]
Lire la suiteBIBLIOGRAPHIE : Système endocannabinoïdes et récepteurs aux cannabinoïdes Dr Christian Sueur, GRECC, avril 2020. 1 - Système endocannabinoïde : 1 - 7 2 - Récepteurs des cannabinoïdes : 8 - 13 3 - THC et récepteurs non-cannabinoïdes : 14 4 - CBD et récepteurs non cannabinoïdes : 15 5 - Neurophysiologie des endocannabinoïdes : 16 - 19 6 - Neuropharmacologie des cannabinoïdes de synthèse : 20 - 21 7 - Neuropharmacologie des Phytocannabinoïdes : 22 - 29
Lire la suitePlant cannabinoids : a neglected pharmacological treasure trove Raphael Mechoulam British Journal of Pharmacology, 2005, 146, 913–915 doi : 10.1038/sj.bjp.0706415 Most of the cannabinoids in Cannabis sativa L. have not been fully evaluated for their pharmacological activity. A publication in this issue presents evidence that a plant cannabinoid, D9-tetrahydro-cannabivarin is a potent antagonist of anandamide, a major endogenous cannabinoid. It seems possible that many of the non-psychoactive constituents of this plant will be of biological interest. Keywords : Anandamide; CB1 receptor antagonist; CB2 receptor antagonist; mouse vas deferens; D9 tetrahydrocannabinol; D9-tetrahydrocannabivarin; -(þ)-(R)- WIN55212 Cannabis sativa L. produces more than 60 terpeno-phenols that have not been detected [...]
Lire la suiteCannabidiol regulates behavioural alterations and gene expression changes induced by spontaneous cannabinoid withdrawal Francisco Navarrete, Auxiliadora Aracil-Fernández and Jorge Manzanares British Journal of Pharmacology, 2018. Doi : 10.1111/bph.14226 BACKGROUND AND PURPOSE Cannabidiol (CBD) represents a promising therapeutic tool for treating cannabis use disorder (CUD). This study aimed to evaluate the effects of CBD on the behavioural and gene expression alterations induced by spontaneous cannabinoid withdrawal. EXPERIMENTAL APPROACH Spontaneous cannabinoid withdrawal was evaluated 12 h after cessation of CP-55,940 treatment (0.5 mg·kg1 every 12 h, i.p.; 7 days) in C57BL/6J mice. The effects of CBD (5, 10 and 20 mg·kg1, i.p.) on withdrawal-related behavioural signs were evaluated by [...]
Lire la suiteCannabinoid receptor expression in non-small cell lung cancer. Effectiveness of tetrahydrocannabinol and cannabidiol inhibiting cell proliferation and epithelial mesenchymal transition in vitro Lara Milian, Manuel Mata, Javier Alcacer, Marıa Oliver, Marıa Sancho-Tello, Jose Javier Martın de Llano, Carlos Camps, Jose Galbis, Julian Carretero, Carmen Carda PLoS ONE, 2020, 15, (2): e0228909. Doi : 10.1371/journal.pone.0228909 Abstract Background/Objective : Patients with non-small cell lung cancer (NSCLC) develop resistance to antitumor agents by mechanisms that involve the epithelial-to-mesenchymal transition (EMT). This necessitates the development of new complementary drugs, e.g., cannabinoid receptors (CB1 and CB2) agonists including tetrahydro-cannabinol (THC) and cannabidiol (CBD). The combined use of THC and CBD [...]
Lire la suiteAntidepressant-like effects of β-caryophyllene on restraint plus stress-induced depression Eun-Sang Hwang, Hyun-Bum Kim, Seok Lee, Min-Jeong Kim, Kwan-Joong Kim, Gaeul Han, Se-Young Han, Eun-A Lee, Jeong-Hee Yoon, Dae-Ok Kim, Sungho Maeng, Ji-Ho Park Behavioural Brain Research, 2020, 380, 112439 doi : 10.1016/j.bbr.2019.112439 A B S T R A C T Chronic stress is depressogenic by altering neurotrophic and neuroinflammatory environments of the organism. The endocannabinoid system controls cognitive and emotional responses related with stress through the interaction with endocannabinoid receptors. β-Caryophyllene (BCP) is a CB2 agonist that exhibited anti-inflammatory, analgesic effects but minimal psychoactive effects. To test if BCP exhibits antidepressant-like action, animals were chronically restrained with additional [...]
Lire la suiteBeta-Caryophyllene, a CB2-Receptor-Selective Phytocannabinoid, Suppresses Mechanical Allodynia in a Mouse Model of Antiretroviral-Induced Neuropathic Pain Esraa Aly, Maitham A. Khajah and Willias Masocha Molecules, 2020, 25, 106; doi:10.3390/molecules25010106 Abstract : Neuropathic pain associated with nucleoside reverse transcriptase inhibitors (NRTIs), therapeutic agents for human immunodeficiency virus (HIV), responds poorly to available drugs. Smoked cannabis was reported to relieve HIV-associated neuropathic pain in clinical trials. Some constituents of cannabis (Cannabis sativa) activate cannabinoid type 1 (CB1) and cannabinoid type 2 (CB2) receptors. However, activation of the CB1 receptor is associated with side eects such as psychosis and physical dependence. Therefore, we investigated the effect of B-caryophyllene (BCP), [...]
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