Étiquette : CB1 recepteur

Cannabinoid CB1 and CB2 Receptor Signaling and Bias, Mikkel Soes Ibsen et al., 2017

Cannabinoid CB1 and CB2 Receptor Signaling and Bias Mikkel Soes Ibsen, Mark Connor, Michelle Glass Cannabis and Cannabinoid Research, 2017, Volume 2.1, 48-60 https://doi.org/10.1089/can.2016.0037   Abstract An agonist that acts through a single receptor can activate numerous signaling pathways. Recent studies have suggested that different ligands can differentially activate these pathways by stabilizing a limited range of receptor conformations, which in turn preferentially drive different downstream signaling cascades. This concept, termed “biased signaling” represents an exciting therapeutic opportunity to target specific pathways that elicit only desired effects, while avoiding undesired effects mediated by different signaling cascades. The cannabinoid receptors CB1 and CB2 each activate multiple pathways, [...]

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An Update on Non-CB1, Non-CB2 Cannabinoid Related G-Protein-Coupled Receptors, Paula Morales and Patricia H. Reggio, 2017

An Update on Non-CB1, Non-CB2 Cannabinoid Related G-Protein-Coupled Receptors Paula Morales and Patricia H. Reggio Cannabis and Cannabinoid Research, 2017, Volume 2.1, 265-273 DOI: 10.1089/can.2017.0036   Abstract The endocannabinoid system (ECS) has been shown to be of great importance in the regulation of numerous physiological and pathological processes. To date, two Class A G-protein-coupled receptors (GPCRs) have been discovered and validated as the main therapeutic targets of this system: the cannabinoid receptor type 1 (CB1), which is the most abundant neuromodulatory receptor in the brain, and the cannabinoid receptor type 2 (CB2), predominantly found in the immune system among other organs and tissues. Endogenous cannabinoid receptor [...]

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Endocannabinoid Signaling and Synaptic Function, Pablo E. Castillo et al., 2012

Endocannabinoid Signaling and Synaptic Function Pablo E. Castillo, Thomas J. Younts, Andres E. Chavez, and Yuki Hashimotodani Neuron, Cell Press, 2012. http://dx.doi.org/10.1016/j.neuron.2012.09.020   Endocannabinoids are key modulators of synaptic function. By activating cannabinoid receptors expressed in the central nervous system, these lipid messengers can regulate several neural functions and behaviors. As experimental tools advance, the repertoire of known endocannabinoid-mediated effects at the synapse, and their underlying mechanism, continues to expand. Retrograde signaling is the principal mode by which endocannabinoids mediate short- and long-term forms of plasticity at both excitatory and inhibitory synapses. However, growing evidence suggests that endocannabinoids can also signal in a nonretrograde manner. [...]

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N-Arachidonoyl Dopamine : A Novel Endocannabinoid and Endovanilloid with Widespread Physiological and Pharmacological Activities, Urszula Grabiec and Faramarz Dehghan, 2017

N-Arachidonoyl Dopamine : A Novel Endocannabinoid and Endovanilloid with Widespread Physiological and Pharmacological Activities Urszula Grabiec and Faramarz Dehghani Cannabis and Cannabinoid Research, 2017, 2, (1), 183-196 DOI: 10.1089/can.2017.0015   Abstract N-arachidonoyl dopamine (NADA) is a member of the family of endocannabinoids to which several other N-acyldopamines belong as well. Their activity is mediated through various targets that include cannabinoid receptors or transient receptor potential vanilloid (TRPV)1. Synthesis and degradation of NADA are not yet fully understood. Nonetheless, there is evidence that NADA plays an important role in nociception and inflammation in the central and peripheral nervous system. The TRPV1 receptor, for which NADA is a [...]

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A Conversion of Oral Cannabidiol to Delta9-Tetrahydrocannabinol Seems Not to Occur in Humans, Gerhard Nahler et al., 2017

A Conversion of Oral Cannabidiol to Delta9-Tetrahydrocannabinol Seems Not to Occur in Humans Gerhard Nahler, Franjo Grotenhermen, Antonio Waldo Zuardi, and Jose´ A.S. Crippa3 Cannabis and Cannabinoid Research, 2017, 2, 1, 81-86 DOI: 10.1089/can.2017.0009 Abstract Cannabidiol (CBD), a major cannabinoid of hemp, does not bind to CB1 receptors and is therefore devoid of psychotomimetic properties. Under acidic conditions, CBD can be transformed to delta9 tetrahydro-cannabinol (THC) and other cannabinoids. It has been argued that this may occur also after oral administration in humans. However, the experimental conversion of CBD to THC and delta8-THC in simulated gastric fluid (SGF) is a highly artificial approach that deviates [...]

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The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids : D9-tetrahydrocannabinol, cannabidiol and D9-tetrahydrocannabivarin, R.G. Pertwee, 2008

The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids : D9-tetrahydrocannabinol, cannabidiol and D9-tetrahydrocannabivarin Roger G. Pertwee British Journal of Pharmacology, 2008, 153, 199–215 doi:10.1038/sj.bjp.0707442   Cannabis sativa is the source of a unique set of compounds known collectively as plant cannabinoids or phytocannabinoids. This review focuses on the manner with which three of these compounds, (-)-trans-D9-tetrahydrocannabinol (D9-THC), (-)- cannabidiol (CBD) and (-)-trans-D9-tetrahydrocannabivarin (D9-THCV), interact with cannabinoid CB1 and CB2 receptors. D9-THC, the main psychotropic constituent of cannabis, is a CB1 and CB2 receptor partial agonist and in line with classical pharmacology, the responses it elicits appear to be strongly influenced both by [...]

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Therapeutic Potential of Cannabinoids in Psychosis, Leweke F.M. et al., 2016

Therapeutic Potential of Cannabinoids in Psychosis. Leweke F.M., Mueller J.K., Lange B., Rohleder C. Biological Psychiatry, 2016, 79, (7) 604-612. doi: 10.1016/j.biopsych.2015.11.018.   Abstract Over recent years, the interest in the endocannabinoid system (ECS) as a new target for the treatment of schizophrenia has evolved. The ECS represents one of the most relevant neurotransmitter systems in the brain and mainly fulfills a homeostatic role in terms of neurotransmission but also with respect to inflammatory processes. Two main approaches to the modulation of endocannabinoid functioning have been chosen so far. First, the selective blockade or inverse agonism of the type 1 cannabinoid receptor has been tested for [...]

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Molecular Pharmacology of Phytocannabinoids, Sarah E. Turner et al., 2017

Molecular Pharmacology of Phytocannabinoids Sarah E. Turner, Claire M. Williams, Leslie Iversen, and Benjamin J. Whalley © Springer International Publishing Switzerland 2017 A.D. Kinghorn, H. Falk, S. Gibbons, J. Kobayashi (eds.), Phytocannabinoids, Progress in the Chemistry of Organic Natural Products 103, 61-100. DOI 10.1007/978-3-319-45541-9_3 Contents 1 Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . [...]

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Cannabinoids and Neuropathic Pain, P.W. Brownjohn and J.C. Ashton, 2012

Cannabinol and Neuropathic Pain P.W. Brownjohn and J.C. Ashton Neuropathic Pain, 2012, chap. 4, 79-102   1. Introduction Cannabinoids are drugs that are either derived from cannabis or that induce similar behavioural and physiological effects to cannabis. They fall into three classes: those that are produced by plants of the Cannabis genus, termed phytocannabinoids (plant cannabinoids); those that are produced within the body, termed endocannabinoids (endogenous cannabinoids); and those that are produced synthetically to mimic the pharmacology of naturally occurring cannabinoids. Cannabinoids stand in relation to cannabis as opioids such as codeine, pethidine, fentanyl, and methadone stand in relation to opium. While opium and opioids [...]

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Cannabinoids : potential antitumoral agents ?, Manuel Guzmán, 2006

Cannabinoids: potential antitumoral agents ? Manuel Guzmán Cannabinoids, 2006, 1, 2, 15-17 © International Association for Cannabis as Medicine Mini-review Abstract Cannabinoids, the active components of Cannabis sativa L., act in the body by mimicking endogenous substances - the endocannabinoids - that activate specific cell surface receptors. Cannabinoids exert palliative effects in cancer patients. For example, they inhibit chemotherapy-induced nausea and vomiting, stimulate appetite and inhibit pain. In addition, cannabinoids inhibit tumor growth in laboratory animals. They do so by modulating key cell signaling pathways, thereby inducing antitumoral actions such as the apoptotic death of tumor cells as well as the inhibition of tumor angiogenesis. Of [...]

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