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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/28345790/metabolic-responses-to-exogenous-ghrelin-in-obesity-and-early-after-roux-en-y-gastric-bypass-in-humans
#1
Robyn A Tamboli, Joseph Antoun, Reem M Sidani, B Austin Clements, Emily A Eckert, Pam Marks-Shulman, Bruce D Gaylinn, D Brandon Williams, Ronald H Clements, Vance L Albaugh, Naji N Abumrad
AIMS: Ghrelin is a gastric-derived hormone that stimulates growth hormone (GH) secretion and has a multi-faceted role in the regulation of energy homeostasis, including glucose metabolism. Circulating ghrelin concentrations are modulated in response to nutritional status, but responses to ghrelin in altered metabolic states are poorly understood. We investigated the metabolic effects of ghrelin in obesity and early after Roux-en-Y gastric bypass (RYGB). MATERIALS AND METHODS: We assessed central and peripheral metabolic responses to acyl ghrelin infusion (1 pmol kg(-1) min(-1) ) in healthy, lean subjects (n = 9) and non-diabetic, obese subjects (n = 9) before and two weeks after RYGB...
March 27, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28345765/a-synthetic-route-to-%C3%AE-hydroxytyrosine-derived-tetramic-acids-total-synthesis-of-the-fungal-metabolite-f-14329
#2
Sebastian Bruckner, Robert G Haase, Rainer Schobert
3-Acyltetramic acids derived from β-hydroxytyrosine are synthetically challenging. We present the first route to this structural motif, based upon a condensation between a Meldrum's acid conjugate bearing the acyl side chain, and a β-hydroxytyrosinate, N-protected by an ortho-nitrobenzyl group. This group enables the Dieckmann cyclization of the resulting N-(β-ketoacyl)amino ester, after which it can be removed photolytically without com¬promising the delicate 3'-hydroxy group. This strategy was applied to the first total synthesis of the fungal metabolite F-14329 (1)...
March 27, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28345343/electronic-and-steric-optimization-of-fluorogenic-probes-for-biomolecular-imaging
#3
Wen Chyan, Henry R Kilgore, Brian Gold, Ronald T Raines
Fluorogenic probes are invaluable tools for spatiotemporal investigations within live cells. In common fluorogenic probes, the intrinsic fluorescence of a small-molecule fluorophore is masked by esterification until entry into a cell, where endogenous esterases catalyze the hydrolysis of the masking groups, generating fluorescence. The susceptibility of masking groups to spontaneous hydrolysis is a major limitation of these probes. Previous attempts to address this problem have incorporated auto-immolative linkers at the cost of atom economy and synthetic adversity...
March 27, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28344554/cannabis-in-chinese-medicine-are-some-traditional-indications-referenced-in-ancient-literature-related-to-cannabinoids
#4
REVIEW
E Joseph Brand, Zhongzhen Zhao
Cannabis sativa L. (Cannabaceae) has a long history of utilization as a fiber and seed crop in China, and its achenes ("seeds") as well as other plant parts have been recorded in Chinese medical texts for nearly 2000 years. While the primary applications of cannabis in Chinese medicine center around the use of the achenes, ancient indications for the female inflorescence, and other plant parts include conditions such as pain and mental illness that are the subject of current research into cannabinoids such as cannabidiol (CBD) and Δ(9)-tetrahydrocannabinol (THC)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28343385/development-of-a-rapid-lc-ms-ms-method-for-the-quantification-of-cannabidiol-cannabidivarin-%C3%AE-9-tetrahydrocannabivarin-and-cannabigerol-in-mouse-peripheral-tissues
#5
Fabiana Piscitelli, Ester Pagano, Anna Lauritano, Angelo A Izzo, Vincenzo Di Marzo
Cannabis has been known as a medicine for several thousand years across many cultures and its beneficial effects are due to the presence of cannabinoids, unique natural products, whose pharmacology is going to gain increasing interest in scientific community. The discovery of the main psychoactive constituent of Cannabis sativa L., Δ9-tetrahydrocannabinol (Δ9-THC), has led to the identification of at least one hundred additional phytocannabinoids, including cannabidiol (CBD), cannabidivarin (CBDV), Δ9-tetrahydrocannabivarin (Δ9-THCV) and cannabigerol (CBG)...
March 26, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28343112/the-impact-of-australian-legislative-changes-on-synthetic-cannabinoid-exposures-reported-to-the-new-south-wales-poisons-information-centre
#6
Rose Cairns, Jared A Brown, Naren Gunja, Nicholas A Buckley
BACKGROUND: The emergence of new psychoactive substances (NPS), including synthetic cannabinoid receptor agonists (SCRAs) poses novel challenges for drug regulation and public health. Misconceptions of safety and legality, coupled with the fact that NPS are undetectable on routine drugs screens contributes to their popularity. Concerns over the unpredictable toxicity and abuse potential of NPS has led to a variety of legislative responses worldwide. We wish to describe Australian trends in SCRA use, examining the effects of legislative changes on calls to Australia's largest poisons centre...
March 23, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28341460/cortical-adrenoceptor-expression-function-and-adaptation-under-conditions-of-cannabinoid-receptor-deletion
#7
B A S Reyes, A F Carvalho, P Szot, D J Kalamarides, Q Wang, L G Kirby, E J Van Bockstaele
A neurochemical target at which cannabinoids interact to have global effects on behavior is brain noradrenergic circuitry. Acute and repeated administration of a cannabinoid receptor synthetic agonist is capable of increasing multiple indices of noradrenergic activity. This includes cannabinoid-induced 1) increases in norepinephrine (NE) release in the medial prefrontal cortex (mPFC); 2) desensitization of cortical α2-adrenoceptor-mediated effects; 3) activation of c-Fos in brainstem locus coeruleus (LC) noradrenergic neurons; and 4) increases in anxiety-like behaviors...
March 21, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28340730/identification-and-determination-of-synthetic-cannabinoids-in-herbal-products-by-dry-film-attenuated-total-reflectance-infrared-spectroscopy
#8
Victor de la Asunción-Nadal, Sergio Armenta, Salvador Garrigues, Miguel de la Guardia
A new procedure has been developed for the identification and quantitative determination of synthetic cannabinoids in illicit herbal preparations. The methodology is based on the use of attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) measurement of sample extracts with 2-propanol drying 5µL of the extracts onto the ATR crystal. The qualitative identification was carried out on the 2-propanol extract after identification of the herbal matrix, followed by its subtraction and using a cut-off criterion of 75%...
May 15, 2017: Talanta
https://www.readbyqxmd.com/read/28340719/application-of-a-rapid-%C3%AE-spe-clean-up-for-multiclass-quantitative-analysis-of-sixteen-new-psychoactive-substances-in-whole-blood-by-lc-ms-ms
#9
Camilla Montesano, Gabriele Vannutelli, Valeria Piccirilli, Manuel Sergi, Dario Compagnone, Roberta Curini
Europe is an important market for illegal drugs, and nowadays a lot of new different psychoactive substances (NPS) are widespread. This work reports the development of a method to determine simultaneously different classes of NPS, as synthetic cannabinoids (SC) and their metabolites, cathinones and phenetylamines, directly on whole blood (WB) without anti-coagulants and using miniaturized solid phase extraction (μ-SPE). In order to demonstrate the feasibility of the method 16 different NPS belonging to the mentioned classes were selected for the analysis...
May 15, 2017: Talanta
https://www.readbyqxmd.com/read/28340702/selective-solid-phase-extraction-of-jwh-synthetic-cannabinoids-by-using-computationally-designed-peptides
#10
Marcello Mascini, Camilla Montesano, German Perez, Joseph Wang, Dario Compagnone, Manuel Sergi
The objective of the present work is to demonstrate a rational way to prepare selective sorbents able to extract simultaneously several structural analogs. For this purpose the binding specificity of two hexapeptides computationally designed (VYWLVW and YYIGGF) versus four synthetic cannabinoids Naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH 018), naphthalen-1-yl-(1-butylindol-3-yl)methanone (JWH 073), (R)-(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)(naphthalen-1-yl)methanone (AM 1220) and (R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-napthalenylmethanone (WIN 55) was computationally studied and then experimentally tested by solid-phase extraction (SPE) clean-up and ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) analysis...
May 15, 2017: Talanta
https://www.readbyqxmd.com/read/28339898/the-impact-of-the-psychoactive-substances-act-2016-on-the-online-availability-of-mdmb-chmica
#11
M Haden, D M Wood, P I Dargan
Background: In May 2016, the UK Government enacted the Psychoactive Substances Act which made it an offense to produce or supply many drugs including new psychoactive substances (NPS). Aim: We aimed to assess the impact of the Act on the availability of the synthetic cannabinoid receptor agonist methyl 2-[[1-(cyclohexylmethyl)indole-3-carbonyl]amino]-3,3-dimethylbutanoate (MDMB-CHMICA) from internet-based suppliers. Design: Internet snapshot availability study...
February 28, 2017: QJM: Monthly Journal of the Association of Physicians
https://www.readbyqxmd.com/read/28337258/neuroprotective-effect-of-win55-212-2-against-3-nitropropionic-acid-induced-toxicity-in-the-rat-brain-involvement-of-cb1-and-nmda-receptors
#12
Marisol Maya-López, Ana Laura Colín-González, Gabriela Aguilera, María Eduarda de Lima, Ana Colpo-Ceolin, Edgar Rangel-López, Juana Villeda-Hernández, Daniel Rembao-Bojórquez, Isaac Túnez, Armando Luna-López, Roberto Lazzarini-Lechuga, Viridiana Yazmín González-Puertos, Pedro Posadas-Rodríguez, Alejandro Silva-Palacios, Mina Königsberg, Abel Santamaría
The endocannabinoid system (ECS), and agonists acting on cannabinoid receptors (CBr), are known to regulate several physiological events in the brain, including modulatory actions on excitatory events probably through N-methyl-D-aspartate receptor (NMDAr) activity. Actually, CBr agonists can be neuroprotective. The synthetic CBr agonist WIN55,212-2 acts mainly on CB1 receptor. In turn, the mitochondrial toxin 3-nitropropionic acid (3-NP) produces striatal alterations in rats similar to those observed in the brain of Huntington's disease patients...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28337114/precondition-of-right-frontal-region-with-anodal-tdcs-can-restore-the-fear-memory-impairment-induced-by-acpa-in-male-mice
#13
Fariborz Manteghi, Mohammad Nasehi, Mohammad-Reza Zarrindast
Fear memory and learning cause behavioural patterns such as fight or flight responses, which increase survival probability, but unfit processing of fear memory and learning can lead to maladaptive behaviours and maladies such as phobias, Post-Traumatic Stress Disorder (PTSD) and anxiety disorders. The growing prevalence of these maladies shows the need to quest novel methods for their treatment. We used anodal transcranial direct current stimulation (tDCS) on the right frontal region as a precondition neuromodulator and arachidonylcyclopropylamide (ACPA), a selective CB1 cannabinoid receptor agonist, as a fear memory impairing agent to assess their effects on contextual and auditory fear conditioning (reliable model for fear studies)...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28335571/3-substituted-n-benzylpyrazine-2-carboxamide-derivatives-synthesis-antimycobacterial-and-antibacterial-evaluation
#14
Lucia Semelková, Ondřej Janďourek, Klára Konečná, Pavla Paterová, Lucie Navrátilová, František Trejtnar, Vladimír Kubíček, Jiří Kuneš, Martin Doležal, Jan Zitko
A series of substituted N-benzyl-3-chloropyrazine-2-carboxamides were prepared as positional isomers of 5-chloro and 6-chloro derivatives, prepared previously. During the aminolysis of the acyl chloride, the simultaneous substitution of chlorine with benzylamino moiety gave rise to N-benzyl-3-(benzylamino)pyrazine-2-carboxamides as side products, in some cases. Although not initially planned, the reaction conditions were modified to populate this double substituted series. The final compounds were tested against four mycobacterial strains...
March 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28334817/stability-of-synthetic-cannabinoids-in-biological-specimens-analysis-through-liquid-chromatography-tandem-mass-spectrometry
#15
Chelsea Fort, Thomas Jourdan, Jesse Kemp, Byron Curtis
The focus of this study was to determine the stability of four synthetic cannabinoids, XLR-11, UR-144, AB-Pinaca and AB-Fubinaca in biological specimens for the purpose of casework processing prioritization. The study used human whole blood spiked with the compounds of interest to mimic real forensic laboratory samples submitted for synthetic cannabinoid analysis. The spiked whole blood specimens were incubated under one of three temperature conditions: room or ambient (22°C), refrigerated (4°C) and frozen (-20°C) for a period of 12 weeks...
February 18, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28334603/the-cb1-receptor-as-the-cornerstone-of-exostasis
#16
REVIEW
Pier Vincenzo Piazza, Daniela Cota, Giovanni Marsicano
The type-1 cannabinoid receptor (CB1) is the main effector of the endocannabinoid system (ECS), which is involved in most brain and body functions. In this Perspective, we provide evidence indicating that CB1 receptor functions are key determinants of bodily coordinated exostatic processes. First, we will introduce the concepts of endostasis and exostasis as compensation or accumulation for immediate or future energy needs and discuss how exostasis has been necessary for the survival of species during evolution...
March 22, 2017: Neuron
https://www.readbyqxmd.com/read/28334325/endocannabinoid-dependent-long-term-potentiation-of-synaptic-transmission-at-rat-barrel-cortex
#17
Laura Eva Maglio, José Antonio Noriega-Prieto, Maria Jesús Maraver, David Fernández de Sevilla
Brain-derived neurotrophic factor (BDNF) plays a critical role in modulating plasticity in sensory cortices. Indeed, a BDNF-dependent long-term potentiation (LTP) at distal basal excitatory synapses of Layer 5 pyramidal neurons (L5PNs) has been demonstrated in disinhibited rat barrel cortex slices. Although it is well established that this LTP requires the pairing of excitatory postsynaptic potentials (PSPs) with Ca2+ spikes, its induction when synaptic inhibition is working remains unexplored. Here we show that low-frequency stimulation at basal dendrites of L5PNs is able to trigger a PSP followed by an action potential (AP) and a slow depolarization (termed PSP-Ca2+ response) in thalamocortical slices without blocking synaptic inhibition...
March 1, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28334226/loss-of-cannabinoid-cb-1-receptors-induces-cortical-migration-malformations-and-increases-seizure-susceptibility
#18
Javier Díaz-Alonso, Adán de Salas-Quiroga, Juan Paraíso-Luna, Daniel García-Rincón, Patricia P Garcez, Maddy Parsons, Clara Andradas, Cristina Sánchez, François Guillemot, Manuel Guzmán, Ismael Galve-Roperh
Neuronal migration is a fundamental process of brain development, and its disruption underlies devastating neurodevelopmental disorders. The transcriptional programs governing this process are relatively well characterized. However, how environmental cues instruct neuronal migration remains poorly understood. Here, we demonstrate that the cannabinoid CB 1 receptor is strictly required for appropriate pyramidal neuron migration in the developing cortex. Acute silencing of the CB 1 receptor alters neuronal morphology and impairs radial migration...
October 5, 2016: Cerebral Cortex
https://www.readbyqxmd.com/read/28333237/new-paenibacillus-strain-produces-a-family-of-linear-and-cyclic-antimicrobial-lipopeptides-cyclization-is-not-essential-for-their-antimicrobial-activity
#19
En Huang, Xu Yang, Liwen Zhang, Sun Hee Moon, Ahmed E Yousef
A new bacterial isolate, Paenibacillus sp. OSY-N, showed potent antimicrobial activity against Gram-negative and Gram-positive bacteria. Antimicrobials produced by this strain were purified by reverse-phase high performance liquid chromatography (HPLC). Structural analysis, using mass spectrometry (MS), of a single active HPLC fraction revealed two known cyclic lipopeptides, BMY-28160 and permetin A, a new cyclic lipopeptide, and the linear counterparts of these cyclic compounds. The latter were designated as paenipeptin A, B and C, respectively...
February 25, 2017: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/28333097/effects-of-a-sativex-like-combination-of-phytocannabinoids-on-disease-progression-in-r6-2-mice-an-experimental-model-of-huntington-s-disease
#20
Sara Valdeolivas, Onintza Sagredo, Mercedes Delgado, Miguel A Pozo, Javier Fernández-Ruiz
Several cannabinoids afforded neuroprotection in experimental models of Huntington's disease (HD). We investigated whether a 1:1 combination of botanical extracts enriched in either ∆⁸-tetrahydrocannabinol (∆⁸-THC) or cannabidiol (CBD), which are the main constituents of the cannabis-based medicine Sativex(®), is beneficial in R6/2 mice (a transgenic model of HD), as it was previously shown to have positive effects in neurotoxin-based models of HD. We recorded the progression of neurological deficits and the extent of striatal deterioration, using behavioral, in vivo imaging, and biochemical methods in R6/2 mice and their corresponding wild-type mice...
March 23, 2017: International Journal of Molecular Sciences
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