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Recent Cannabinoid Delivery Systems
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Natascia Bruni, Carlo Della Pepa, Simonetta Oliaro-Bosso, Daniela Gastaldi, Franco Dosio, Enrica Pessione
Although phytocannabinoids have similar chemical structures, they can elicit different pharmacological action. The identification of THC paved the way for the discovery, in 1988, of cannabinoid receptor type 1 (CB1) [4], and, later, of cannabinoid receptor type 2 (CB2) [5]. CB1 and CB2, belong to a family of seven transmembrane guanosine binding protein-coupled receptors, are widely expressed and distinguished by their specific functions, localization, and signaling mechanisms. They are one of the important endogenous lipid signaling pathways, named the “endocannabinoid system,” which consists of cannabinoid receptors, the endogenous ligands of cannabinoid receptors (endocannabinoids), and the enzymes that regulate the biosynthesis and inactivation of endocannabinoids. This lipid signaling system is involved in many important physiological functions in the central and peripheral nervous system and in the endocrine and immune systems [6,7].
Herbal Cannabinomimetics
Published in Amritpal Singh Saroya, Reverse Pharmacology, 2018
(E)-p-caryophyllene is a major constituent in Cannabis. The constituent has selective binding to cannabinoid receptor type 2. Upon binding, the constituent has inhibitory action on adenylate cyclase. This results in transition on calcium inside the cell.
Evaluation of COMT (rs4680), CNR2 (rs2501432), CNR2 (rs2229579), UCP2 (rs659366), and IL-17 (rs763780) gene variants in synthetic cannabinoid use disorder patients
Published in Journal of Addictive Diseases, 2020
Sacide Pehlivan, Hasan Mervan Aytac, Selin Kurnaz, Mustafa Pehlivan, Pinar Cetinay Aydin
Catechol-O-methyltransferase (COMT) is an enzyme found in the central nervous system that inactivates dopamine, epinephrine, and norepinephrine. A variation in the COMT gene exchanging valine to the methionine amino acid at position 108/158 results in two common enzyme variants: Val and Met. While the Met allele of COMT is associated with low enzymatic activity, the Val allele is associated with increased enzymatic activity.5 COMT (rs4680) variants may affect COMT activity in the brain, altering dopamine neurotransmission known to play a prominent role in reward and addiction.6 Cannabinoid receptors that bind to both exogenous and endogenous cannabinoids are seven-transmembrane domain G-protein-coupled receptors. The cannabinoid receptor-1 (CB1) is encoded by the cannabinoid receptor type 1 (CNR1) gene, while the cannabinoid receptor-2 (CB2) is encoded by the cannabinoid receptor type 2 gene (CNR2), which has been actively investigated for its role in osteoporosis, inflammation, leukemia, several types of cancer, and addiction.7
Effects of hypertension and FAAH inhibitor treatment of rats with primary and secondary hypertension considering the physicochemical properties of erythrocytes
Published in Toxicology Mechanisms and Methods, 2020
Izabela Dobrzyńska, Barbara Szachowicz-Petelska, Anna Pędzińska-Betiuk, Zbigniew A. Figaszewski, Elżbieta Skrzydlewska
The level of ROS depends on the functioning of the endocannabinoid system. Through the activation of their receptors (cannabinoid receptor type 1 – CB1 and cannabinoid receptor type 2 – CB2), endocannabinoids modulate ROS levels and inflammation directly and indirectly (Luo et al. 2015; Biernacki, Malinowska, et al. 2018; Biernacki et al. 2019). Endocannabinoids and their receptors are also present in the human circulatory system and are involved in the regulation of blood flow (Baranowska-Kuczko et al. 2016; Toczek et al. 2016; Harasim-Symbor et al. 2019). Increasing endocannabinoid levels promote blood pressure decrease, and the levels of endocannabinoids, especially anandamide, are regulated mainly by fatty-acid amide hydrolase (FAAH), which is responsible primarily for anandamide degradation (Biernacki et al. 2019). Thus, FAAH inhibitors are potential antihypertensive agents. Acute blockade of FAAH (e.g. by URB597) in hypertensive rats raised endocannabinoid levels and normalized the blood pressure (Godlewski et al. 2010).
Analysis of endocannabinoid receptors and enzymes in the post-mortem motor cortex and spinal cord of amyotrophic lateral sclerosis patients
Published in Amyotrophic Lateral Sclerosis and Frontotemporal Degeneration, 2018
Francisco Espejo-Porras, Javier Fernández-Ruiz, Eva de Lago
Rilutek® and Radicava® are the only FDA approved drugs for slowing disease progression in ALS, but they have modest efficacy (8–10). Recently cannabinoids have been shown to provide neuroprotection in ALS, specifically in the SOD-1G93A transgenic mice (11,12), and the issue has reached the clinical scenario with the first trial with cannabinoid-based therapies in ALS (13). Neuroprotective effects have been found with Δ9-tetrahydrocannabinol (14), cannabinol (15), the synthetic agonist WIN55,212-2 (16), and the cannabinoid receptor type-2 (CB2) agonist AM1241 (17,18). The fact that neuroprotective effects were reached with nonselective cannabinoids (14–16) suggests that different endocannabinoid mechanisms, for example, the cannabinoid receptor type-1 (CB1) and also the CB2 receptor, and even targets outside this system, may be involved (12). However, activating selectively the CB2 receptor with AM1241 led to levels of neuroprotection (17,18) similar to treatments with nonselective agonists (14–16), which supports a major role for the CB2 receptor. This may be facilitated by the CB2 receptor up-regulation found in lesioned structures in neurodegenerative disorders (12,19,20). In ALS, such up-regulation has been found in spinal tissues from patients (21), SOD1G93A transgenic mice (18,22), dogs affected by an ALS-related canine disease (23), and TDP-43 transgenic mice (24), and implied reactive microglia and/or activated astrocytes. These studies have situated the CB2 receptor in a prominent position for the development of disease modifying therapies, given its effective control of glial influence on neurons (19,20,25). In fact, this could be one of the mechanisms involved in the effects of palmitoylethanolamide in the clinical trial initiated in Europe (13), given its activity at the CB2-like receptors (26). On the other hand, all studies showing CB2 receptor up-regulation in ALS, including Yiangou et al. (21), investigated exclusively the spinal cord, not including the motor cortex where cell bodies of upper motor neurons are located. In the present study, we investigated the motor cortex to confirm that CB2 receptors are also elevated, to identify the cell substrates in which this response takes place, and to explore whether other cannabinoid receptors (e.g. CB1 receptor) or endocannabinoid enzymes (e.g. FAAH, MAGL) are also altered in this structure in patients.