scholarly journals Can Physical Activity Support the Endocannabinoid System in the Preventive and Therapeutic Approach to Neurological Disorders?

2020 ◽  
Vol 21 (12) ◽  
pp. 4221
Author(s):  
Tomasz Charytoniuk ◽  
Hubert Zywno ◽  
Karolina Konstantynowicz-Nowicka ◽  
Klaudia Berk ◽  
Wiktor Bzdega ◽  
...  
Keyword(s):  
Physical Activity ◽  
Neurodegenerative Disorders ◽  
Therapeutic Approach ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Endocannabinoid System ◽  
Antidepressant Effect ◽  
Brain Physiology ◽  
Current State ◽  
Neurological Effects

The worldwide prevalence of neurological and neurodegenerative disorders, such as depression or Alzheimer’s disease, has spread extensively throughout the last decades, becoming an enormous health issue. Numerous data indicate a distinct correlation between the altered endocannabinoid signaling and different aspects of brain physiology, such as memory or neurogenesis. Moreover, the endocannabinoid system is widely regarded as a crucial factor in the development of neuropathologies. Thus, targeting those disorders via synthetic cannabinoids, as well as phytocannabinoids, becomes a widespread research issue. Over the last decade, the endocannabinoid system has been extensively studied for its correlation with physical activity. Recent data showed that physical activity correlates with elevated endocannabinoid serum concentrations and increased cannabinoid receptor type 1 (CB1R) expression in the brain, which results in positive neurological effects including antidepressant effect, ameliorated memory, neuroplasticity development, and reduced neuroinflammation. However, none of the prior reviews presented a comprehensive correlation between physical activity, the endocannabinoid system, and neuropathologies. Thus, our review provides a current state of knowledge of the endocannabinoid system, its action in physical activity, as well as neuropathologies and a possible correlation between all those fields. We believe that this might contribute to finding a new preventive and therapeutic approach to both neurological and neurodegenerative disorders.

scholarly journals Cannabinoids on the Brain

2002 ◽  
Vol 2 ◽  
pp. 632-648 ◽  
Author(s):  
Andrew J. Irving ◽  
Mark G. Rae ◽  
Angela A. Coutts
Keyword(s):  
Cannabinoid Receptor ◽  
Endocannabinoid System ◽  
Medicinal Uses ◽  
Cellular Targets ◽  
Analgesic Effects ◽  
Current State ◽  
History Of ◽  
New Type ◽  
Reward Pathways ◽  
The Brain

Cannabis has a long history of consumption both for recreational and medicinal uses. Recently there have been significant advances in our understanding of how cannabis and related compounds (cannabinoids) affect the brain and this review addresses the current state of knowledge of these effects. Cannabinoids act primarily via two types of receptor, CB1and CB2, with CB1receptors mediating most of the central actions of cannabinoids. The presence of a new type of brain cannabinoid receptor is also indicated. Important advances have been made in our understanding of cannabinoid receptor signaling pathways, their modulation of synaptic transmission and plasticity, the cellular targets of cannabinoids in different central nervous system (CNS) regions and, in particular, the role of the endogenous brain cannabinoid (endocannabinoid) system. Cannabinoids have widespread actions in the brain: in the hippocampus they influence learning and memory; in the basal ganglia they modulate locomotor activity and reward pathways; in the hypothalamus they have a role in the control of appetite. Cannabinoids may also be protective against neurodegeneration and brain damage and exhibit anticonvulsant activity. Some of the analgesic effects of cannabinoids also appear to involve sites within the brain. These advances in our understanding of the actions of cannabinoids and the brain endocannabinoid system have led to important new insights into neuronal function which are likely to result in the development of new therapeutic strategies for the treatment of a number of key CNS disorders.

scholarly journals Overview of Synthetic Cannabinoids ADB-FUBINACA and AMB-FUBINACA: Clinical, Analytical, and Forensic Implications

2021 ◽  
Vol 14 (3) ◽  
pp. 186
Author(s):  
Carolina Lobato-Freitas ◽  
Andreia Machado Brito-da-Costa ◽  
Ricardo Jorge Dinis-Oliveira ◽  
Helena Carmo ◽  
Félix Carvalho ◽  
...  
Keyword(s):  
Scientific Literature ◽  
Cannabinoid Receptor ◽  
Biological Effects ◽  
Synthetic Cannabinoids ◽  
Detection Methods ◽  
Drug Candidate ◽  
Assessment And Treatment ◽  
Neurological Effects ◽  
Recreational Use ◽  
Harmful Effects

ADB-FUBINACA and AMB-FUBINACA are two synthetic indazole-derived cannabinoid receptor agonists, up to 140- and 85-fold more potent, respectively, than trans-∆9-tetrahydrocannabinol (∆9-THC), the main psychoactive compound of cannabis. Synthesised in 2009 as a pharmaceutical drug candidate, the recreational use of ADB-FUBINACA was first reported in 2013 in Japan, with fatal cases being described in 2015. ADB-FUBINACA is one of the most apprehended and consumed synthetic cannabinoid (SC), following AMB-FUBINACA, which emerged in 2014 as a drug of abuse and has since been responsible for several intoxication and death outbreaks. Here, we critically review the physicochemical properties, detection methods, prevalence, biological effects, pharmacodynamics and pharmacokinetics of both drugs. When smoked, these SCs produce almost immediate effects (about 10 to 15 s after use) that last up to 60 min. They are rapidly and extensively metabolised, being the O-demethylated metabolite of AMB-FUBINACA, 2-(1-(4-fluorobenzyl)-1H-indazole-3-carboxamide)-3-methylbutanoic acid, the main excreted in urine, while for ADB-FUBINACA the main biomarkers are the hydroxdimethylpropyl ADB-FUBINACA, hydroxydehydrodimethylpropyl ADB-FUBINACA and hydroxylindazole ADB-FUBINACA. ADB-FUBINACA and AMB-FUBINACA display full agonism of the CB1 receptor, this being responsible for their cardiovascular and neurological effects (e.g., altered perception, agitation, anxiety, paranoia, hallucinations, loss of consciousness and memory, chest pain, hypertension, tachycardia, seizures). This review highlights the urgent requirement for additional studies on the toxicokinetic properties of AMB-FUBINACA and ADB-FUBINACA, as this is imperative to improve the methods for detecting and quantifying these drugs and to determine the best exposure markers in the various biological matrices. Furthermore, it stresses the need for clinicians and pathologists involved in the management of these intoxications to describe their findings in the scientific literature, thus assisting in the risk assessment and treatment of the harmful effects of these drugs in future medical and forensic investigations.

scholarly journals Cannabinoids: Chemical Structure, Mechanisms of Action, Toxicity and Implications in Everyday Life

2019 ◽  
Vol 70 (2) ◽  
pp. 627-629
Author(s):  
Mary Nicoleta Lupu ◽  
Magdalena Miulescu ◽  
Madalina Nina Sandu ◽  
Iulia Filip ◽  
Laura Rebegea ◽  
...  
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Endocannabinoid System ◽  
Presynaptic Neuron ◽  
Cannabinoid System ◽  
Sensory Experiences ◽  
Increased Risk ◽  
Psychoactive Effects ◽  
Exogenous Substances

In the human body there is an endocannabinoid system consisting of cannabinoid receptors and endogenous transmitters - the endocannabinoids (anandamides).This cannabinoid system works by certain principles: the presynaptic neuron releases the neurotransmitter that reaches the postsynaptic neuron, activating it; at this level endocannabinoids are synthesized, whichhave retrograde transmission through the synaptic gap, reaching the cannabinoid receptors where they can inhibit the anterograde release of neurotransmitters. At the same level, certain exogenous substances, derived from plants and called phytocannabinoids may also work, the most known one being tetrahydrocannabinol. 9-D-Tetrahydrocannabinol is a component extracted from hemp plant with intense psychotic action but also with some medical applications. The result of the cannabinoid system activity is to obtain certain psychoactive effects, euphoria, relaxation, intense sensory experiences, pain relief but also changes in perception, attention deficit, etc. Synthetic cannabinoids are obtained to mimic the effects of marijuana, are major cannabinoid receptor agonists and are at increased risk of toxicity. Chronic consumption of such substances can cause memory disorders, pulmonary disorders and, most importantly, addiction.

scholarly journals Identification and Analytical Characterization of a Novel Synthetic Cannabinoid-Type Substance in Herbal Material in Europe

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 793
Author(s):  
Emmanouil D. Tsochatzis ◽  
Joao Alberto Lopes ◽  
Margaret V. Holland ◽  
Fabiano Reniero ◽  
Giovanni Palmieri ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Cannabinoid Receptor ◽  
Analytical Data ◽  
Synthetic Cannabinoids ◽  
Synthetic Cannabinoid ◽  
Gas Chromatography Mass Spectrometry ◽  
New Psychoactive Substances ◽  
Synthetic Cannabinoid Receptor Agonists ◽  
Analytical Laboratories

The rapid diffusion of new psychoactive substances (NPS) presents unprecedented challenges to both customs authorities and analytical laboratories involved in their detection and characterization. In this study an analytical approach to the identification and structural elucidation of a novel synthetic cannabimimetic, quinolin-8-yl-3-[(4,4-difluoropiperidin-1-yl) sulfonyl]-4-methylbenzoate (2F-QMPSB), detected in seized herbal material, is detailed. An acid precursor 4-methyl-3-(4,4-difluoro-1-piperidinylsulfonyl) benzoic acid (2F-MPSBA), has also been identified in the same seized material. After extraction from the herbal material the synthetic cannabimimetic, also referred to as synthetic cannabinoid receptor agonists or “synthetic cannabinoids”, was characterized using gas chromatography-mass spectrometry (GC-MS), 1H, 13C, 19F and 15N nuclear magnetic resonance (NMR) and high-resolution tandem mass spectrometry (HR-MS/MS) combined with chromatographic separation. A cheminformatics platform was used to manage and interpret the analytical data from these techniques.

scholarly journals CB1 antagonism increases excitatory synaptogenesis in a cortical spheroid model of fetal brain development

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Alexis Papariello ◽  
David Taylor ◽  
Ken Soderstrom ◽  
Karen Litwa
Keyword(s):  
Brain Development ◽  
Spontaneous Activity ◽  
Microelectrode Array ◽  
Cannabinoid Receptor ◽  
Fetal Brain ◽  
Endocannabinoid System ◽  
Autism Spectrum ◽  
Nervous System Development ◽  
Inhibitory Synapses ◽  
Fetal Brain Development

AbstractThe endocannabinoid system (ECS) plays a complex role in the development of neural circuitry during fetal brain development. The cannabinoid receptor type 1 (CB1) controls synaptic strength at both excitatory and inhibitory synapses and thus contributes to the balance of excitatory and inhibitory signaling. Imbalances in the ratio of excitatory to inhibitory synapses have been implicated in various neuropsychiatric disorders associated with dysregulated central nervous system development including autism spectrum disorder, epilepsy, and schizophrenia. The role of CB1 in human brain development has been difficult to study but advances in induced pluripotent stem cell technology have allowed us to model the fetal brain environment. Cortical spheroids resemble the cortex of the dorsal telencephalon during mid-fetal gestation and possess functional synapses, spontaneous activity, an astrocyte population, and pseudo-laminar organization. We first characterized the ECS using STORM microscopy and observed synaptic localization of components similar to that which is observed in the fetal brain. Next, using the CB1-selective antagonist SR141716A, we observed an increase in excitatory, and to a lesser extent, inhibitory synaptogenesis as measured by confocal image analysis. Further, CB1 antagonism increased the variability of spontaneous activity within developing neural networks, as measured by microelectrode array. Overall, we have established that cortical spheroids express ECS components and are thus a useful model for exploring endocannabinoid mediation of childhood neuropsychiatric disease.

scholarly journals Therapeutic Attributes of Endocannabinoid System against Neuro-Inflammatory Autoimmune Disorders

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3389
Author(s):  
Ishtiaq Ahmed ◽  
Saif Ur Rehman ◽  
Shiva Shahmohamadnejad ◽  
Muhammad Anjum Zia ◽  
Muhammad Ahmad ◽  
...  
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Therapeutic Potential ◽  
Endocannabinoid System ◽  
Cell Types ◽  
Autoimmune Disorders ◽  
Specific Receptors ◽  
Different Cell Types

In humans, various sites like cannabinoid receptors (CBR) having a binding affinity with cannabinoids are distributed on the surface of different cell types, where endocannabinoids (ECs) and derivatives of fatty acid can bind. The binding of these substance(s) triggers the activation of specific receptors required for various physiological functions, including pain sensation, memory, and appetite. The ECs and CBR perform multiple functions via the cannabinoid receptor 1 (CB1); cannabinoid receptor 2 (CB2), having a key effect in restraining neurotransmitters and the arrangement of cytokines. The role of cannabinoids in the immune system is illustrated because of their immunosuppressive characteristics. These characteristics include inhibition of leucocyte proliferation, T cells apoptosis, and induction of macrophages along with reduced pro-inflammatory cytokines secretion. The review seeks to discuss the functional relationship between the endocannabinoid system (ECS) and anti-tumor characteristics of cannabinoids in various cancers. The therapeutic potential of cannabinoids for cancer—both in vivo and in vitro clinical trials—has also been highlighted and reported to be effective in mice models in arthritis for the inflammation reduction, neuropathic pain, positive effect in multiple sclerosis and type-1 diabetes mellitus, and found beneficial for treating in various cancers. In human models, such studies are limited; thereby, further research is indispensable in this field to get a conclusive outcome. Therefore, in autoimmune disorders, therapeutic cannabinoids can serve as promising immunosuppressive and anti-fibrotic agents.

Oxidants and antioxidants in exercise

1995 ◽  
Vol 79 (3) ◽  
pp. 675-686 ◽  
Author(s):  
C. K. Sen
Keyword(s):  
Oxidative Stress ◽  
Physical Activity ◽  
Exercise Training ◽  
Animal Studies ◽  
Dietary Habits ◽  
Antioxidant Defenses ◽  
Current State ◽  
Strenuous Physical Exercise ◽  
Long Duration ◽  
Exercise Induced

There is consistent evidence from human and animal studies that strenuous physical exercise may induce a state wherein the antioxidant defenses of several tissues are overwhelmed by excess reactive oxygen. A wide variety of physiological and dietary antioxidants act in concert to evade such a stress. Submaximal long-duration exercise training may augment the physiological antioxidant defenses in several tissues; however, this enhanced protection may not be sufficient to completely protect highly fit individuals from exhaustive exercise-induced oxidative stress. Regular physical activity in association with dietary habits that ensure adequate supply of a combination of appropriate antioxidants may be expected to yield desirable results. The significance of this area of research, current state of information, and possibilities of further investigation are briefly reviewed.

scholarly journals Discordant Effects of Cannabinoid 2 Receptor Antagonism/Inverse Agonism During Adolescence on Pavlovian and Instrumental Reward Learning in Adult Male Rats

2021 ◽  
Vol 13 ◽  
Author(s):  
Danna Ellner ◽  
Bryana Hallam ◽  
Jude A. Frie ◽  
Hayley H. A. Thorpe ◽  
Muhammad Shoaib ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Critical Role ◽  
Behavioral Outcomes ◽  
Endocannabinoid System ◽  
Developmental Trajectory ◽  
Male Rats ◽  
Reward Learning ◽  
Adolescent Male ◽  
High Dose ◽  
Lever Pressing

The endocannabinoid system is responsible for regulating a spectrum of physiological activities and plays a critical role in the developing brain. During adolescence, the endocannabinoid system is particularly sensitive to external insults that may change the brain’s developmental trajectory. Cannabinoid receptor type 2 (CB2R) was initially thought to predominantly function in the peripheral nervous system, but more recent studies have implicated its role in the mesolimbic pathway, a network largely attributed to reward circuitry and reward motivated behavior, which undergoes extensive changes during adolescence. It is therefore important to understand how CB2R modulation during adolescence can impact reward-related behaviors in adulthood. In this study, adolescent male rats (postnatal days 28–41) were exposed to a low or high dose of the CB2R antagonist/inverse agonist SR144528 and Pavlovian autoshaping and instrumental conditional behavioral outcomes were measured in adulthood. SR144528-treated rats had significantly slower acquisition of the autoshaping task, seen by less lever pressing behavior over time [F(2, 19) = 5.964, p = 0.010]. Conversely, there was no effect of adolescent SR144528 exposure on instrumental conditioning. These results suggest that modulation of the CB2R in adolescence differentially impacts reward-learning behaviors in adulthood.

scholarly journals Influence of sports-type physical activity on the formation of predictors of stress and its consequences in adolescents of school age

2021 ◽  
Vol 100 (6) ◽  
pp. 623-628
Author(s):  
Ekaterina V. Bulycheva ◽  
Ilya A. Setko
Keyword(s):  
Physical Activity ◽  
Stress Resistance ◽  
Cognitive Activity ◽  
Educational Activity ◽  
Mental Condition ◽  
School Age ◽  
Emotional Experiences ◽  
Sports Activity ◽  
Current State ◽  
Resistance To Stress

Introduction. Physical activity in a sports mode can have a positive effect not only on physical health but also on mental condition. In this regard, sports motor activity can be considered a factor in increasing resistance to stress and protection from stressors in adolescents of school age. Materials and methods. 200 students aged 15-17 yrs, formed into two groups, a comparative assessment of the mental factors of the current state was carried out, which is determined by the action of stressors, including the level of anxiety, negative emotional experiences, cognitive activity, stress and stress resistance. The carried out correlation and factor analysis established the relationship between the studied mental factors of the mental state. Results. A significant decrease in the level of anxiety and negative emotional experiences in educational activity among athletes was determined in comparison with the data of adolescents who were not athletes, while in everyday activities these indicators practically did not differ among adolescents from the studied groups. The effective potential of adaptation to stressful situations in adolescents was evidenced by the data obtained on a decrease in the stress level by 1.4 times and an increase in the level of stress resistance by 1.5 times relative to these adolescents who are not athletes. Correlation analysis indicates the level of resistance to stress and stress to be associated with the level of anxiety and negative emotional experiences. At the same time, it was determined that athletes during the formation of stress, anxiety and negative emotional experiences were chosen to account for only 18% of the variance (F = 12.68, p≤0.0001), while in non-athletes - 44% (F = 42.59, p≤0.0001). Conclusion. Organized sports activity of adolescents plays an essential role in improving and maintaining mental factors of the current state, such as anxiety, negative emotional experiences, stress and stress resistance.

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