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Endogenous Cannabinoid Receptors and Medical Cannabis
Published in Sahar Swidan, Matthew Bennett, Advanced Therapeutics in Pain Medicine, 2020
Considerably more work is needed to fully describe the pharmacology of the orthosteric and allosteric modulators operating on the ECS, but much is already known. The endocannabinoid anandamide is a partial agonist, operating as a modulator more in the periphery, outside the CNS. Anandamide functions as a partial receptor agonist affecting the neurons that regulate pain signaling by controlling the chemical gates through which pain signals access the CNS. By contrast, the endocannabinoid 2-AG is a total agonist, fully activating the cannabinoid receptors. 2-AG has been referred to as the workhorse of the ECS, serving as a point-to-point retrograde messenger to provide fundamental brain and spinal cord functions. Major endocannabinoids are rapidly deactivated by reuptake mechanisms and degrading enzymes.11,12 Cannabinoid receptor activity is also selectively modified by the binding of ligands at allosteric sites on receptors.
Pharmacotherapy of Neurochemical Imbalances
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Rupali Patil, Aman Upaganlawar, Suvarna Ingale
The interesting fact observed was that though cannabinoids exist only naturally in plant with no biological connection in humans, many parts of brain, namely cerebral cortex, basal ganglia, cerebellum, and hippocampus express huge numbers of receptors for cannabinoids. This made scientific workers to think of endogenous substances which may be selectively interacting with CB and whose action is facilitated by Delta-9-tetrahydrocannabinol. Thus in 1992, the first endogenous ligand of CB1 receptors later labeled as Anandamide was discovered in porcine brain. The name, Anandamide was derived from the Sanskrit word ‘Ananda’ meaning ‘Bliss.’ With the discovery of anandamide, many other metabolites collectively termed as endocannabinoids, were characterized and discovered to act as useful agonists of CB in the brain, however they were not superior in efficacy than anandamide (Devane et al., 1992). The endocannabinoids are found in the brain or other tissues only in small amounts. Similar to other lipid mediators, they are formed and released locally on call. Anandamide and endocannabinoids are rapidly inactivated by reuptake through transporter and by metabolism through the enzyme fatty acid amide hydrolase. The anandamide is formed from the precursor N-arachidonic phosphatidyl ethanolamine by hydrolysis in presence of an enzyme phosphodiesterase enzyme phospholipase D (Iversen, 2003).
Scientific, Legal, and Regulatory Considerations for Cannabidiol
Published in Robert E.C. Wildman, Richard S. Bruno, Handbook of Nutraceuticals and Functional Foods, 2019
Jay Manfre, Rick Collins, Marielle Kahn Weintraub, Robert E.C. Wildman
Several studies of both the endocannabinoid system and endogenous cannabinoids have revealed their involvement in numerous physiological processes, including appetite,17 pain sensation, control of chronic pain,18–20 and regulation of immune cell functions.21 Endocannabinoid compounds, such as cannabidiol, have been shown to modulate various disease pathology and movement disorders.22–24There is little research available on the direct effects of CBD supplementation in conjunction with exercise in human subjects; however, it has been suggested that the endocannabinoid system partakes in adaptive responses to exercise. One theory of this adaptation is evident by the activation of the endogenous cannabinoid, anandamide, during exercise.25 Anandamide acts as a vasodilator, leading to hypertension and facilitating blood flow. Additionally, studies have demonstrated that both endocannabinoids and exogenous cannabinoids can act as bronchodilators,26 affecting the respiratory system and therefore possibly facilitating breathing during exercise. The degree to which endocannabinoids and phytocannabinoidsncrease regenerative properties, such as “healthy bone, tendon, ligament, muscular and connective tissue integrity27 is still being researched However, Dr. Hector Lopez theorizes how hemp-derived CBD products may help balance and optimize ECS physiology27. The addition of a CBD extract product may reduce anxiety levels, increase quality sleep, and contribute to an optimized diet.
Pharmacological Treatment of Generalised Anxiety Disorder: Current Practice and Future Directions
Published in Expert Review of Neurotherapeutics, 2023
Harry A. Fagan, David S. Baldwin
The endocannabinoid system is a widespread neurotransmitter system, consisting of endogenous ligands (anandamide and 2-AG) and two cannabinoid receptors (CB1 and CB2). Exogenous ligands for cannabinoid receptors are produced by the cannabis plant (Cannabis sativa) and these phytocannabinoids have been widely used throughout human history [136]. Identified phytocannabinoids include Δ9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD) [137]. Several synthetic cannabinoids have also been produced. CBD lacks the psychotomimetic effects of Δ9-THC and animal studies indicate a potential anxiolytic effect [138]. However, to date, there are limited clinical studies on the effect of cannabinoids in anxiety disorders [139]. No RCT has considered the effect of cannabinoids in GAD, although one small RCT demonstrated a single dose of CBD (600 mg) reduced anxiety induced by public speaking in patients with SAD [140]. In addition, a crossover RCT demonstrated the efficacy of 7 weeks of treatment with the synthetic cannabinoid nabilone on frequency of nightmares and quality of life in PTSD (albeit with a small sample size of 10 participants) [141].
A primer on sleeping, dreaming, and psychoactive agents
Published in Journal of Social Work Practice in the Addictions, 2023
The endocannabinoid system is a complicated biological system involved in regulating movement, mood, memory, appetite, fertility, pain, and physiological homeostasis. It consists of cannabinoid receptors and cannabinoid receptor proteins that are active throughout both the central and peripheral nervous systems. Two endogenous molecules that activate the endocannabinoid system have been found. The first, 2-arachidonoyl glycerol (2-AG), occurs in peripheral tissues, while anandamide (Sanskrit for ‘supreme joy’) is a neurotransmitter. The psychoactive component of cannabis, Δ9-tetrahydrocannabinol (THC), mimics the actions of anandamide, whereas the main therapeutic component of cannabis, cannabidiol (CBD), mimics 2-AG (Mechoulan & Parker, 2013). Data from the past 20 years indicates that the endocannabinoid system plays a role in modulating the human sleep-wake cycle and can play a part in the decrease in sleep disturbance or insomnia through the restoration of sleeping and dreaming through the regulation of how this occurs is not yet fully understood (Kesner & Lovinger, 2020; Prospéro-García et al., 2016).
Assessment of clinical outcomes of medicinal cannabis therapy for depression: analysis from the UK Medical Cannabis Registry
Published in Expert Review of Neurotherapeutics, 2022
Sajed Mangoo, Simon Erridge, Carl Holvey, Ross Coomber, Daniela A Riano Barros, Urmila Bhoskar, Gracia Mwimba, Kavita Praveen, Chris Symeon, Simmi Sachdeva-Mohan, James J Rucker, Mikael H Sodergren
(−)-trans-Δ9-tetrahydrocannabinol (Δ9-THC) and/or cannabidiol (CBD) are the main active pharmaceutical ingredients in cannabis-based medicinal products (CBMPs) [11]. Δ9-THC is mainly responsible for the psychotropic properties of cannabis, such as euphoria, and acts as a partial CB1 and CB2 receptor agonist [9]. CBD may act as a negative allosteric modulator of CB1 receptors, although there is controversy about the exact mechanism of CBD on cannabinoid receptors [12]. However, it is accepted that CBD primarily acts through the inhibition of fatty acid binding ligands [13]. This reduces the transportation of anandamide, an endogenous partial CB1 agonist, to fatty acid amide hydrolase, which leads to increased levels of anandamide and increased constitutive activation of CB1 receptors [13]. By increasing endocannabinoid signaling via interaction with CB1 and CB2 receptors in the endocannabinoid system, CBMPs have been proposed as potential therapeutic compounds for the treatment of depression.