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N-acyl or cannabinoid or NAPE

Jenny Ceccarini, Rawaha Ahmad, Laura Van de Vliet, Cindy Casteels, Mathieu Vandenbulcke, Wim Vandenberghe, Koen Van Laere
Many Huntington disease (HD) mutation carriers already have cognitive and psychiatric symptoms in the premanifest (premotor) phase of the disease, but the molecular underpinnings of these symptoms are not well understood. Previous work has shown reduced availability of the cerebral type 1 cannabinoid receptor (CB1 R) in manifest HD. Here, we investigated whether CB1 R binding is related to cognitive and psychiatric symptoms in premanifest HD mutation carriers (preHD). Methods: CB1R binding was measured with 18 F-MK-9470 PET in 15 preHD subjects (8M/7F; age 39...
June 22, 2018: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Vaida Kitrytė, Dovyda Bagdonaitė, Petras Rimantas Venskutonis
C. sativa threshing residues were biorefined by consecutive supercritical carbon dioxide (SFE-CO2 ) pressurised liquid (PLE) and enzyme-assisted extractions (EAE). SFE-CO2 at optimised parameters yielded 8.3g/100g of lipophilic fraction containing 0.2 and 2.2g of cannabidiol and cannabidiolic acid per 100g of threshing residues, respectively. The recovery of cannabinoids from plant material was >93%. PLE gave 4.3 and 18.9g/100g of flavonoid-containing polar extracts, while EAE added 20.2% (w/w) of water-soluble constituents and increased the release of mono- and disaccharides by up to 94%...
November 30, 2018: Food Chemistry
Ryan Graddy, Megan E Buresh, Darius A Rastegar
Several novel psychoactive substances have emerged in recent years. Users are typically young men who use other substances. In the category of stimulants, cathinones ("bath salts") have predominated and can lead to agitation, psychosis, hyperthermia, and death. Synthetic cannabinoids ("spice") are more potent than marijuana and can lead to agitation, psychosis, seizures, and death. There are no rapid tests to identify these substances and general treatment includes benzodiazepines for agitation and supportive therapy...
July 2018: Medical Clinics of North America
Annie Lévesque, Bernard Le Foll
Cannabis (marijuana) is a drug product derived from the plant Cannabis sativa. Cannabinoid is a general term for all chemical constituents of the cannabis plant. Legalization of marijuana in numerous US states, the availability of cannabis of higher potency, and the emergence of synthetic cannabinoids may have contributed to increased demand for related medical services. The most effective available treatments for cannabis use disorder are psychosocial approaches. There is no pharmacotherapy approved treatment...
July 2018: Medical Clinics of North America
Mara Turri, Francesco Teatini, Francesco Donato, Giampietro Zanette, Valeria Tugnoli, Luciano Deotto, Bruno Bonetti, Giovanna Squintani
Background. Delta-9-tetrahydrocannabinol (THC)/cannabidiol (CBD) (nabiximols or Sativex® ) is an oromucosal spray formulation containing THC and CBD at an approximately 1:1 fixed ratio. Its administration for the treatment of pain in patients with multiple sclerosis (MS) has been established. MS patients generally complain of different kinds of pain, including spasticity-related and neuropathic pain. In this study, we compared and evaluated pain modulation and thermal/pain threshold of MS patients before and after THC/CBD administration...
June 21, 2018: Medicines (Basel, Switzerland)
C Sagnelli, C Uberti-Foppa, H Hasson, G Bellini, C Minichini, S Salpietro, E Messina, D Barbanotti, M Merli, F Punzo, N Coppola, A Lazzarin, E Sagnelli, F Rossi
OBJECTIVES: The aim of the study was to investigate whether the rs35761398 variants of the cannabinoid receptor 2 (CB2) gene may influence the acquisition of HIV infection and the clinical presentation of HIV/hepatitis C virus (HCV) coinfection. METHODS: We compared 166 HIV/HCV-coinfected patients with 186 HCV-monoinfected patients, all with biopsy-proven chronic hepatitis (using the Ishak scoring system), naïve for anti-HCV treatment and tested for the CB2 rs35761398 polymorphism (using the TaqMan assay)...
June 22, 2018: HIV Medicine
Koby Cohen, Aviv M Weinstein
There is a growing use of novel psychoactive substances containing synthetic cannabinoids. Synthetic cannabinoid products have effects similar to those of natural cannabis, yet, these drugs are more potent and dangerous, and have been associated with dangerous adverse effects. Here, we review current literature on the epidemiology, acute, and chronic effects of synthetic and natural cannabinoid-based drugs. Synthetic drugs contain a mixture of psychoactive compounds that mostly bind cannabinoid receptors with high potency...
2018: Frontiers in Public Health
Andrea Porzionato, Elena Stocco, Diego Guidolin, Luigi Agnati, Veronica Macchi, Raffaele De Caro
In the carotid body (CB), a wide series of neurotransmitters and neuromodulators have been identified. They are mainly produced and released by type I cells and act on many different ionotropic and metabotropic receptors located in afferent nerve fibers, type I and II cells. Most metabotropic receptors are G protein-coupled receptors (GPCRs). In other transfected or native cells, GPCRs have been demonstrated to establish physical receptor-receptor interactions (RRIs) with formation of homo/hetero-complexes (dimers or receptor mosaics) in a dynamic monomer/oligomer equilibrium...
2018: Frontiers in Physiology
Pengcheng Peng, Hui Huang, Hongqiang Ren, Haijun Ma, Yuan Lin, Jinju Geng, Ke Xu, Yan Zhang, Lili Ding
Startup of biofilm process triggered by initial adhesion of bacteria is difficult in high ammonia nitrogen wastewater treatment. In this study, the influence of two commonly used N-acyl homoserine lactones (AHLs), N-Hexanoyl-l-homoserine lactone (C6-HSL) and N-Octanoyl-l-homoserine lactone (C8-HSL), on the adhesion of soluble macromolecules and bacteria in four types of high ammonia nitrogen wastewater to surfaces of model biocarriers (i.e. polystyrene, polyamide and polyethylene terephthalate) was investigated by using a quartz crystal microbalance with dissipation (QCM-D) monitoring technology...
May 15, 2018: Science of the Total Environment
Dusan Kolar
Treatment-resistant mood disorders and anxiety disorders require intensive treatment, but treatment options should balance benefits and adverse effects or other potential detrimental effects on patients, including the risk of developing prescription medication addiction. Some of the newer treatment modalities for mood and anxiety disorders may have similar properties to benzodiazepines. The goal of this review was to identify the potential for developing dependence on the novel treatment approaches to treatment-resistant depression and refractory anxiety disorders...
2018: Neuropsychiatric Disease and Treatment
Vijai Datta Upadhyaya, Ankur Bhatnagar, Basant Kumar, Zafar Neyaz, J S Kishore, Eti Sthapak
Background: Intralesional bleomycin scelro-therapy has become a favored line of treatment for macrocystic lymphatic malformations. However the need for multiple sessions is a drawback associated with this treatment modality. Our aim is to document whether multiple session of intra- lesional sclero-therapy is necessary for complete resolution of cystic lymphatic malformation. Method: Intralesional bleomycin under Ultrasound guidance was used for macrocystic lymphangioma at concentration of 3mg/ml but not exceeding the total dose (1mg/kg) body weight for single session or cumulative dose of 5mg/kg...
January 2018: Indian Journal of Plastic Surgery: Official Publication of the Association of Plastic Surgeons of India
Giles Newton-Howes
The use of cannabis as a medicine has a long tradition in western medicine. It has been seen as a viable option for the treatment of various neurological and psychiatric conditions, and recently there is again interest in the place of cannabinoids in the pharmacopoeia. What has become increasingly clear, however, is these benefits need to be weighed carefully against the potential difficulty associated with herbal cannabis and cannabinoid compounds for an individual's mental health. This challenges the use of cannabis as a medication and the regulation of its prescription...
June 20, 2018: British Journal of Clinical Pharmacology
Dan P Covey, Hannah M Dantrassy, Samantha E Yohn, Alberto Castro, P Jeffrey Conn, Yolanda Mateo, Joseph F Cheer
Prominent motor deficits (e.g., chorea) that typify Huntington's disease (HD) arise following a prolonged prodromal stage characterized by psychiatric disturbances. Apathy, a disorder of motivation characterized by diminished goal-directed behavior, is one of the earliest and most common psychiatric symptoms in HD, but the underlying neurobiology is unclear and treatment options are limited. Alterations in the endocannabinoid (eCB) and dopamine systems represent prominent pathophysiological markers in HD that-similar to motivational deficits-present early and decline across disease progression...
June 1, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
Lalanthi Ratnayake, Keyur K Adhvaryu, Elizabeth Kafes, Kamyar Motavaze, Patricia Lakin-Thomas
The TOR (Target of Rapamycin) pathway is a highly-conserved signaling pathway in eukaryotes that regulates cellular growth and stress responses. The cellular response to amino acids or carbon sources such as glucose requires anchoring of the TOR kinase complex to the lysosomal/vacuolar membrane by the Ragulator (mammals) or EGO (yeast) protein complex. Here we report a connection between the TOR pathway and circadian (daily) rhythmicity. The molecular mechanism of circadian rhythmicity in all eukaryotes has long been thought to be transcription/translation feedback loops (TTFLs)...
June 20, 2018: PLoS Genetics
M Agar
The treatment of symptoms in people with palliative diagnoses begins with meticulous clinical assessment with treatment choice (s) selected based on an understanding of the symptom aetiology and the evidence which underpins its treatment. Increasingly the merits of palliative care have been established earlier in the disease trajectory where treatment outcomes may include increased survival and maintenance of function. There is strong public support for the availability of medicinal cannabis, particularly for people with palliative diagnoses...
June 20, 2018: British Journal of Clinical Pharmacology
Jessica Rice, Michelle Cameron
PURPOSE OF REVIEW: Cannabis and cannabinoids have been used medically and recreationally for thousands of years and recently there has been a growing body of research in this area. With increased access now that medical marijuana is available in many jurisdictions, patients and providers want to know more about the evidence for benefits and risks of cannabinoid use. This paper provides an overview of the available cannabinoid-based formulations, a summary of the highest quality evidence for the use of cannabinoids for treating spasticity and pain associated with multiple sclerosis (MS), and a discussion of possible dosing regimens based on information from these studies...
June 19, 2018: Current Neurology and Neuroscience Reports
Ruiqing Ni, Linjing Mu, Simon Ametamey
Cannabinoid receptor CB2 (CB2 R) is upregulated on activated microglia and astrocytes in the brain under inflammatory conditions and plays important roles in many neurological diseases, such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. The advent of positron emission tomography (PET) using CB2 R radiotracers has enabled the visualization of CB2 R distribution in vivo in animal models of central nervous system inflammation, however translation to humans has been less successful...
June 19, 2018: Acta Pharmacologica Sinica
Chun Wang, Fang Wang, Xiaoxue Chen, Yefang Zou, Hong Zhu, Qingjie Zhao, Jingshan Shen, Yan Li, Yongjun Li, Bin He
Sirtuin inhibitors as physiological research tools and therapeutic potentials have caught many attentions in last decades. The mimics of acyl lysine have been approved to be a very efficient strategy for development of mechanism-based sirtuin inhibitors. In current study, a novel scaffold of l-S-(3-carboxamidopropyl) cysteine (l-CAPC) has been exploited for design and synthesis of sirtuin inhibitors. As a result, the mimics of Nε -acyl-lysine derived from cysteine including small molecules (5a-m) and peptides (9a-m) have been synthesized...
June 16, 2018: Bioorganic & Medicinal Chemistry Letters
Vincenzo Miragliotta, Pier Luca Ricci, Francesco Albanese, Andrea Pirone, Danika Tognotti, Francesca Abramo
BACKGROUND: Cannabinoid receptors and peroxisome proliferator-activated receptor-alpha (PPAR-α) are gaining recognition as potential therapeutic targets for the treatment of skin disorders. HYPOTHESIS/OBJECTIVES: The aim of this study was to investigate the distribution of cannabinoid type 1 and 2 receptors (CBR1 and CBR2) and PPAR-α in feline skin and verify whether changes occur in the course of hypersensitivity dermatitis. ANIMALS: Twelve privately owned cats...
June 19, 2018: Veterinary Dermatology
Lisa Strauch, Jens Pfannstiel, Armin Huber, Olaf Voolstra
Protein phosphorylation is an abundant molecular switch that regulates a multitude of cellular processes. In contrast to other subfamilies of phosphoprotein phosphatases, the PPEF subfamily is only poorly investigated. Drosophila retinal degeneration C (RDGC) constitutes the founding member of the PPEF subfamily. RDGC dephosphorylates the visual pigment rhodopsin and the ion channel TRP. rdgC null mutant flies exhibit rhodopsin and TRP hyperphosphorylation, altered photoreceptor physiology, and retinal degeneration...
June 19, 2018: FEBS Letters
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