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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/28641003/synthesis-and-anti-inflammatory-evaluation-of-2-aminobenzaldehydes-via-ir-iii-catalyzed-c-h-amidation-of-aldimines-with-acyl-azides
#1
Saegun Kim, Prashant Chakrasali, Hyo Sun Suh, Neeraj Kumar Mishra, Taeyoung Kim, Sang Hoon Han, Hyung Sik Kim, Byung-Moo Lee, Soo Bong Han, In Su Kim
The aldimine-directed C-H amidation of various arenes with N-acyl azides as amidation surrogates under cationic iridium(III) catalysis is described. This transformation efficiently provides a range of 2-aminobenzaldehydes derivatives with excellent site-selectivity and functional group compatibility. The resulting 2-aminobenzaldehyde framework provides facile access to a range of biologically interesting heterocycles. In addition, all synthetic compounds were screened for anti-inflammatory activity against interleukin-1β (IL-1β) and tumor necrosis factor alpha (TNF-α) with lipopolysaccharide (LPS)-induced RAW264...
June 22, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28637216/qualitative-analysis-and-detection-of-the-pyrolytic-products-of-jwh-018-and-11-additional-synthetic-cannabinoids-in-the-presence-of-common-herbal-smoking-substrates
#2
Stephen Raso, Suzanne Bell
Synthetic cannabinoids have become a ubiquitous challenge in forensic toxicology and seized drug analysis. Thermal degradation products have yet to be identified and evaluated for toxicity in comparison to parent and metabolic compounds. An investigation into these pyrolytic products, as the major route of ingestion is inhalation, may produce additional insight to understand the toxicity of synthetic cannabinoids. The pyrolysis of JWH-018 and 11 additional synthetic cannabinoids and six herbal plant substrates were conducted using an in-house constructed smoking simulator...
June 20, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28636769/is-cannabis-treatment-for-anxiety-mood-and-related-disorders-ready-for-prime-time
#3
REVIEW
Jasmine Turna, Beth Patterson, Michael Van Ameringen
Anxiety and related disorders are the most common mental conditions affecting the North American population. Despite their established efficacy, first-line antidepressant treatments are associated with significant side effects, leading many afflicted individuals to seek alternative treatments. Cannabis is commonly viewed as a natural alternative for a variety of medical and mental health conditions. Currently, anxiety ranks among the top five medical symptoms for which North Americans report using medical marijuana...
June 21, 2017: Depression and Anxiety
https://www.readbyqxmd.com/read/28635664/adolescent-exposure-to-the-synthetic-cannabinoid-win-55212-2-modifies-cocaine-withdrawal-symptoms-in-adult-mice
#4
María A Aguilar, Juan Carlos Ledesma, Marta Rodríguez-Arias, Carles Penalva, Carmen Manzanedo, José Miñarro, M Carmen Arenas
Chronic cannabinoid consumption is an increasingly common behavior among teenagers and has been shown to cause long-lasting neurobehavioral alterations. Besides, it has been demonstrated that cocaine addiction in adulthood is highly correlated with cannabis abuse during adolescence. Cocaine consumption and subsequent abstinence from it can cause psychiatric symptoms, such as psychosis, cognitive impairment, anxiety, and depression. The aim of the present research was to study the consequences of adolescent exposure to cannabis on the psychiatric-like effects promoted by cocaine withdrawal in adult mice...
June 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28634109/cannabis-associated-psychosis-neural-substrate-and-clinical-impact
#5
REVIEW
R M Murray, A Englund, A Abi-Dargham, D Lewis, M Di Forti, C Davies, M Sherif, P McGuire, C D'Souza
Prospective epidemiological studies have consistently demonstrated that cannabis use is associated with an increased subsequent risk of both psychotic symptoms and schizophrenia-like psychoses. Early onset of use, daily use of high-potency cannabis, and synthetic cannabinoids carry the greatest risk. The risk-increasing effects are not explained by shared genetic predisposition between schizophrenia and cannabis use. Experimental studies in healthy humans show that cannabis and its active ingredient, delta-9-tetrahydrocannabinol (THC), can produce transient, dose-dependent, psychotic symptoms, as well as an array of psychosis-relevant behavioral, cognitive and psychophysiological effects; the psychotogenic effects can be ameliorated by cannabidiol (CBD)...
June 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28633201/rapid-start-up-of-denitrifying-granular-sludge-by-dosing-with-semi-starvation-fluctuation-c-n-ratio-strategy
#6
Wenyu Niu, Jianbo Guo, Jing Lian, Yuanyuan Song, Caicai Lu, Haibo Li, Yi Han, Pengna Yin
This study cultivated denitrifying granular sludge in three UASB reactors by the semi-starvation fluctuation C/N ratio strategy (reactor 1 (R1): constant C/N ratio; R2: regular fluctuation C/N ratio; and R3: semi-starvation fluctuation C/N ratio (SSF)). Microbial aggregates appeared in R1, R2 and R3 on days 28, 14 and 6, respectively. Compared with the results in R1 and R2, the guanosine tetraphosphate (ppGpp) concentration was highest, the acyl homoserine lactones (AHLs) concentration quickly reached a certain threshold, and more protein (PN) of extracellular polymeric substances (EPS) secretion resulted in the rapid formation of denitrifying granular sludge in R3...
June 1, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28632928/n-acylsulfonamides-synthetic-routes-and-biological-potential-in-medicinal-chemistry
#7
REVIEW
Alessandra Ammazzalorso, Barbara De Filippis, Letizia Giampietro, Rosa Amoroso
Sulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N-acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N-acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors...
June 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28631432/profile-effects-and-toxicity-of-novel-psychoactive-substances-a-systematic-review-of-quantitative-studies
#8
Sulaf Assi, Nargilya Gulyamova, Kinda Ibrahim, Paul Kneller, David Osselton
OBJECTIVE: To investigate the profile, effects, and toxicity of novel psychoactive substances (NPS). METHODS: A systematic literature review was conducted between May 2015 and February 2016 and included 19 databases. Search terms included "novel psychoactive substance(s)," "effect(s)," and "toxicity" and their synonyms. Studies included were those from any country, in any language, and between January 2007 and April 2015. Studies published before 2007 and those regarding the synthesis of NPS were excluded...
June 19, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28631421/impact-of-synthetic-cannabinoids-on-the-duration-of-opioid-related-withdrawal-and-craving-among-patients-of-addiction-clinics-in-kazakhstan-a-prospective-case-control-study
#9
Mariya Prilutskaya, Francesco Saverio Bersani, Ornella Corazza, Sergey Molchanov
OBJECTIVE: The aim of the study was to prospectively assess whether regular use of synthetic cannabinoids (SCs) affects the duration of opioid-related withdrawal and craving symptoms in patients undergoing drug detoxification treatments. METHODS: Patients (n = 193) with opioid use disorder, among which 47 patients are regularly using SCs, underwent integrated drug detoxification therapies. The Clinical Opiate Withdrawal Scale and a specific visual analogue scale were used to assess opioid withdrawal and craving symptoms over time...
June 20, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28631313/salivary-gingival-crevicular-fluid-and-serum-levels-of-ghrelin-and-chemerin-in-patients-with-periodontitis-and-overweight
#10
H F R Jentsch, N Arnold, V Richter, J Deschner, T Kantyka, S Eick
BACKGROUND AND OBJECTIVE: Nutrition and body weight are modifying factors for periodontitis. The purpose of this study was to quantify two molecules (ghrelin and chemerin), released in association with food intake and obesity, in periodontally healthy and diseased individuals with respect to different body mass categories. MATERIAL AND METHODS: The two main groups (patients with chronic periodontitis and periodontally healthy/gingivitis volunteers) were subdivided into groups of subjects with normal weight [body mass index (BMI) <25] and groups of overweight/obese subjects (BMI ≥25)...
June 20, 2017: Journal of Periodontal Research
https://www.readbyqxmd.com/read/28631194/the-use-of-cannabinoids-in-treating-dementia
#11
REVIEW
Megan Weier, Wayne Hall
PURPOSE OF REVIEW: To review and summarise the current evidence on the safety and efficacy of using cannabinoids to treat behavioural and neuropsychiatric symptoms of dementia. RECENT FINDINGS: Two randomised controlled trials testing a synthetic form of tetrahydrocannabinol have shown that while well tolerated, there was no significant therapeutic effect, based on changes to scores on the neuropsychiatric inventory (NPI). Case reports and open label trials have indicated that there may be some therapeutic benefit of adding synthetic cannabinoids as an adjunctive therapy to reduce agitation, aberrant motor behaviour and nighttime behaviour...
August 2017: Current Neurology and Neuroscience Reports
https://www.readbyqxmd.com/read/28629846/hippocampal-gr-and-cb1-mediated-mglur5-differentially-produces-susceptibility-and-resilience-to-acute-and-chronic-mild-stress-in-rats
#12
Hongli Sun, Rujuan Su, Xiaoxiao Zhang, Jun Wen, Dan Yao, Xinru Gao, Zhongliang Zhu, Hui Li
The molecular mechanism of individual response of susceptibility and resilience under psychological stress remains controversial and unclear. The present study aimed to explore the relationship of metabotropic glutamate receptor 5 (mGluR5) with glucocorticoid receptor (GR) or cannabinoid receptor (CB1) and further indicate the molecular mechanism of susceptibility and resilience to acute stress (AS) and chronic mild stress (CMS). Sucrose preference test and open field test were used to evaluate the response of susceptibility and resilience under stress in rats...
June 16, 2017: Neuroscience
https://www.readbyqxmd.com/read/28629227/chemical-and-biological-studies-on-cichorium-intybus-l
#13
Dinara Satmbekova, Radhakrishnan Srivedavyasasri, Yerkebulan Orazbekov, Roza Omarova, Ubaidilla Datkhayev, Samir A Ross
Cichorium intybus L. (Asteraceae family) is a world-wide grown plant known as chicory. In traditional medicine, this plant is used as diuretic, anti-inflammatory, digestive, cardiotonic and liver tonic. Chromatographic purification of the supercritical fluid extract of aerial parts of C. intybus on silica gel column led to isolation of three compounds: new compound, 28β-hydroxytaraxasterol (I), and two known compounds usnic acid (II) and β-sitosterol (III). Purification of the ethanolic extract of aerial parts of this plant on silica gel column chromatography yielded four compounds: 1,3-dioleylglycerate (IV), sitoindoside II (V), 11β-13-dihydrolactucin (VI) and β-sitosterol-3-O-glucoside (VII)...
June 19, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28628892/structural-characterization-of-wall-and-lipidated-polysaccharides-from-clostridium-perfringens-atcc-13124
#14
Evgeny Vinogradov, Annie Aubry, Susan M Logan
Cell surface polysaccharides produced by C. perfringens ATCC 13124 were analyzed using NMR, chemical and immunological methods. Two distinct polymers were identified. The more abundant PS1 had a structure based on a polymer of β-mannosamine with a number of modifications, including varying levels of substitution at O-6 with PEtN, N-acetylation, and different linkages between monosaccharides. The shortest variant of PS1 represented a lipoteichoic acid. It contained only 1-4-linkages between ManNAc residues, minor branching α-Ribf, and glucosyl-glycerol at the reducing end, which was acylated with linear saturated fatty acids C16, C18, and C20 (dominant)...
June 15, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/28628337/buckling-under-pressure-curvature-based-lipid-segregation-and-stability-modulation-in-cardiolipin-containing-bilayers
#15
Kevin J Boyd, Nathan N Alder, Eric R May
Mitochondrial metabolic function is affected by the morphology and protein organization of the mitochondrial inner membrane (MIM). Cardiolipin (CL) is a unique tetra-acyl lipid that is involved in the maintenance of the highly-curved shape of the MIM as well as spatial organization of the proteins necessary for respiration and oxidative phosphorylation. Cardiolipin has been suggested to self-organize into lipid domains due to its inverted conical molecular geometry, though the driving forces for this organization are not fully understood...
June 19, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28626532/development-of-quinazoline-pyrimidine-2-4-1h-3h-diones-as-agonists-of-cannabinoid-receptor-type-2
#16
Hai-Yan Qian, Zhi-Long Wang, You-Lu Pan, Li-Li Chen, Xin Xie, Jian-Zhong Chen
Starting from a prototypical structure 1, we describe our efforts to design and obtain novel quinazoline/pyrimidine-2,4(1H,3H)-diones with high CB2 agonist potency and selectivity as well as improved physicochemical characteristics, mainly hydrophilicity. The most potent and selective CB2 agonists, 8 and 36, in this series were also endowed with lower logP values than that of GW842166X and lead compound 1. These derivatives appear to be promising lead compounds for the development of future CB2 agonists.
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28625856/nitroglycerin-increases-serotonin-transporter-expression-in-rat-spinal-cord-but-anandamide-modulated-this-effect
#17
Gábor Nagy-Grócz, Zsuzsanna Bohár, Annamária Fejes-Szabó, Klaudia Flóra Laborc, Eleonóra Spekker, Lilla Tar, László Vécsei, Árpád Párdutz
Migraine is one of the most prevalent neurological diseases, which affects 16% of the total population. The exact pathomechanism of this disorder is still not well understood, but it seems that serotonin and its transporter have a crucial role in the pathogenesis. One of the animal models of migraine is the systemic administration of nitroglycerin (NTG), a nitric oxide (NO) donor. NO can initiate a central sensitization process in the trigeminal system, which is also present in migraineurs. Recent studies showed that the endocannabinoid system has a modulatory role on the trigeminal activation and sensitization...
June 15, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28625720/the-cannabinoid-system-and-pain
#18
REVIEW
Stephen G Woodhams, Victoria Chapman, David P Finn, Andrea G Hohmann, Volker Neugebauer
Chronic pain states are highly prevalent and yet poorly controlled by currently available analgesics, representing an enormous clinical, societal, and economic burden. Existing pain medications have significant limitations and adverse effects including tolerance, dependence, gastrointestinal dysfunction, cognitive impairment, and a narrow therapeutic window, making the search for novel analgesics ever more important. In this article, we review the role of an important endogenous pain control system, the endocannabinoid (EC) system, in the sensory, emotional, and cognitive aspects of pain...
June 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28625718/synaptic-functions-of-endocannabinoid-signaling-in-health-and-disease
#19
REVIEW
Alfonso Araque, Pablo E Castillo, Olivier J Manzoni, Raffaella Tonini
Endocannabinoids (eCBs) are a family of lipid molecules that act as key regulators of synaptic transmission and plasticity. They are synthetized "on demand" following physiological and/or pathological stimuli. Once released from postsynaptic neurons, eCBs typically act as retrograde messengers to activate presynaptic type 1 cannabinoid receptors (CB1) and induce short- or long-term depression of neurotransmitter release. Besides this canonical mechanism of action, recent findings have revealed a number of less conventional mechanisms by which eCBs regulate neural activity and synaptic function, suggesting that eCB-mediated plasticity is mechanistically more diverse than anticipated...
June 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28624572/role-of-beta-catenin-and-endocannabinoids-in-the-nucleus-accumbens-in-extinction-in-rats-exposed-to-shock-and-reminders
#20
Nachshon Korem, Rachel Lange, Cecilia J Hillard, Irit Akirav
The response to a traumatic experience may be rapid recovery or development of psychopathology such as posttraumatic stress disorder (PTSD). Impaired extinction of fear memories is thought to contribute to the development of the persistent trauma memories and avoidance. The Wnt/β-catenin pathway and the endocannabinoid system appear to play significant roles in anxiety and depressive symptoms. Here we examined the involvement of β-catenin in the nucleus accumbens (NAc) in extinction in rats exposed to the shock and reminders model of PTSD...
June 14, 2017: Neuroscience
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