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Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
In several studies, antidepressant-like effects were noted. Salvinorin A reduced immobility in the forced swim test with rats, and in the tail suspension test with mice. These effects could be blocked by either the κ-opioid receptor antagonist nor-binaltorphimine or the CB1 cannabinoid receptor antagonist AM251. Treatment with Salvinorin A also suggested anxiolytic effects in rats in the elevated plus maze.11 Chronic treatment of rats with salvinorin A also reversed the reduction in preference for sucrose – considered a form of depression-like anhedonia – that was induced by chronic unpredictable stress.12
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
Esposito et al. have described the development of a method to encapsulate cannabinoid drugs (precisely the inverse agonist of the CB1 receptor (AM251 and Rimonabant) and the URB597 fatty acid amide hydrolase inhibitor) in NLC [122]. In this circumstance, the lipid phase was composed of tristearin/tricaprylin 2:1 while Poloxamer 188 was added to the water phase. Nanoparticles of around 100 nm with high encapsulation efficiency were obtained.
Micronutrients for Improved Management of Huntington’s Disease
Published in Kedar N. Prasad, Micronutrients in Health and Disease, 2019
Cannabinoid receptors CB1 and CB2 are reduced in the key areas of the HD brain, such as the striatum and cortex. Loss of CB1 receptors was observed at the early stage of HD in the autopsied brain samples of patients with HD.25 This was confirmed by the PET, using a novel CB1 ligand N- [2-(3-cyano-phenyl)-3-(4-(2-18F-fluorethoxy)phenyl)-1-methylpropyl-2-(5-methyl-2-pyridyloxyl)-2-methylproponamide in 20 symptomatic HD patients and 14 healthy subjects. Levels of CB1 receptors decreased throughout the gray matter of the cerebellum, cerebellum, and brainstem.26 Thus, upregulation of CB1 receptors may be of protective value. Indeed, upregulation of CB1 receptors slowed progression of the disease in transgenic R6/1 HD mice.27 Deletion of CB1 receptors aggravated the symptoms and caused neurodegeneration in transgenic HD mice.28 Furthermore, administration of an endogenous cannabinoid receptor agonist delta-9-tetrahydrocannabinol prevented the effect of deletion of CB1 receptors in these mice. Therefore agonists of CB1 receptors may be useful in improving the symptoms of HD. Indeed, administration of CB1 agonist WIN 55,212-2 prevented the development of HD phenotype in quinolinate rat model of HD. This effect of a CB1 receptor agonist was blocked by the corresponding antagonist AM251.29
Endocannabinoid signaling as an intrinsic component of the circuits mediating adaptive responses to repeated stress exposure in adult male sprague dawley rats
Published in Stress, 2020
Ryan J. Newsom, Jacob Stafford, Robert J. Garcia, Serge Campeau
The current study does not include non-stressed comparisons of vehicle treatment to CB1 receptor antagonism with AM251. We have previously reported systemic AM251 administration to have direct stimulatory effect on basal activity in some of the measures utilized in the current study, which are specifically dependent on dose and location of neural/endocrine tissue (Newsom et al., 2012) such that some limbic and neuroendocrine tissues are devoid of direct stimulation by CB1 receptor antagonist AM251, and some predictably display the pattern of CB1 receptor antagonist-stimulated basal activity only at 2.0 mg/kg but not at 1.0 mg/kg AM251 (Newsom et al., in review). It is thus unlikely that the potentiation of stress-induced plasma CORT and c-fos mRNA (in LS, PVN, and rPH) measured in repeatedly stressed rats in Experiment 3 resulted from stimulations of basal activity by the lowest dose of AM251 (0.5 mg/kg). Given the widespread expression of CB1 receptors and ligands in the brain and body, careful selection of agonist/antagonist dose and administration strategies will continue to be important for distinction of specific eCB system activities in future research.
Cannabinoids and bone regeneration
Published in Drug Metabolism Reviews, 2019
Dragos Apostu, Ondine Lucaciu, Alexandru Mester, Horea Benea, Daniel Oltean-Dan, Florin Onisor, Mihaela Baciut, Simion Bran
CB-1 selective inverse agonist (AM251 or Rimonabant®) has shown to inhibit osteoclast differentiation and function, as well as to limit osteoporosis in ovariectomized animal model (Idris et al. 2005, 2008; Idris 2010, 2012). The effect of AM251 is dependent on age, according to Samir and Malek (2014). It decreases RANKL/OPG ratio in skeletally immature rats and increases it in older rats (Samir and Malek 2014). Decrease in RANKL/OPG ratio is important factor in down-regulating osteoclastogenesis. AM 251 has also been shown to inhibit bone nodule formation (Idris et al. 2009). Another potential mechanism of action is represented by the inhibition of WNT signaling pathway, which could lead to an increased osteoblast formation and decreased osteoblast apoptosis (Figure 1) (Proto et al. 2017). Due to its physchiatric side effect including anxiety and depression, AM251 has been withdrawn by both United States Food and Drug Administration and European Medicines Agency (Moreira and Crippa 2009; Idris 2010).
The function of the endocannabinoid system in the pancreatic islet and its implications on metabolic syndrome and diabetes
Published in Islets, 2023
Edgardo Cortes-Justo, Sergio H Garfias-Ramírez, Alonso Vilches-Flores
In the last decade, AM251, AM281 and LY320135 were proposed as synthetic antagonists or reverse agonists for cannabinoid receptors. Isolated human and mouse islets short-term exposed to AM251 increased beta-cell proliferation after cytokines stimulation.46,47,71 As a CB1 receptor antagonist AM251 exerts stimulatory effect on glucose-stimulated insulin secretion in isolated islets from mice and human, but as GPR55 agonist enhances GLP-1 receptor activity, and therefore, potentiates insulin secretion.