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https://www.readbyqxmd.com/read/28821542/human-hepatocyte-metabolism-of-novel-synthetic-cannabinoids-mn-18-and-its-5-fluoro-analog-5f-mn-18
#1
Xingxing Diao, Jeremy Carlier, Mingshe Zhu, Marilyn A Huestis
BACKGROUND: In 2014, 2 novel synthetic cannabinoids, MN-18 and its 5-fluoro analog, 5F-MN-18, were first identified in an ongoing survey of novel psychoactive substances in Japan. In vitro pharmacological assays revealed that MN-18 and 5F-MN-18 displayed high binding affinities to human CB1 and CB2 receptors, with Ki being 1.65-3.86 nmol/L. MN-18 and 5F-MN-18 were scheduled in Japan and some other countries in 2014. Despite increasing prevalence, no human metabolism data are currently available, making it challenging for forensic laboratories to confirm intake of MN-18 or 5F-MN-18...
August 18, 2017: Clinical Chemistry
https://www.readbyqxmd.com/read/28821005/anticonvulsant-effect-of-cannabidiol-in-the-pentylenetetrazole-model-pharmacological-mechanisms-electroencephalographic-profile-and-brain-cytokine-levels
#2
Luciano R Vilela, Isabel V Lima, Érica B Kunsch, Hyorrana Priscila P Pinto, Aline S de Miranda, Érica Leandro M Vieira, Antônio Carlos P de Oliveira, Marcio Flávio D Moraes, Antônio L Teixeira, Fabricio A Moreira
Cannabidiol (CBD), the main nonpsychotomimetic compound from Cannabis sativa, inhibits experimental seizures in animal models and alleviates certain types of intractable epilepsies in patients. Its pharmacological profile, however, is still uncertain. Here we tested the hypothesis that CBD anticonvulsant mechanisms are prevented by cannabinoid (CB1 and CB2) and vanilloid (TRPV1) receptor blockers. We also investigated its effects on electroencephalographic (EEG) activity and hippocampal cytokines in the pentylenetetrazole (PTZ) model...
August 15, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28818702/the-effects-of-cannabinoid-receptors-activation-and-glucocorticoid-receptors-deactivation-in-the-amygdala-and-hippocampus-on-the-consolidation-of-a-traumatic-event
#3
Noa Shoshan, Irit Akirav
Ample evidence demonstrates that fear learning contributes significantly to many anxiety pathologies including post-traumatic stress disorder (PTSD). The endocannabinoid (eCB) system may offer therapeutic benefits for PTSD and it is a modulator of the hypothalamic pituitary adrenal (HPA) axis. Here we compared the separated and combined effects of blocking glucocorticoid receptors (GRs) using the GR antagonist RU486 and enhancing CB1r signaling using the CB1/2 receptor agonist WIN55,212-2 in the CA1 and basolateral amygdala (BLA) on the consolidation of traumatic memory...
August 14, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28818631/topical-medical-cannabis-tmc-a-new-treatment-for-wound-pain-three-cases-of-pyoderma-gangrenosum
#4
Vincent Maida, Jason Corban
Pain associated with integumentary wounds is highly prevalent yet it remains an area of significant unmet need within healthcare. Currently, systemically administered opioids are the mainstay of treatment. However, recent publications are casting opioids in a negative light given their high side effect profile, inhibition of wound healing, and association with accidental overdose, incidents that are frequently fatal. Thus, novel analgesic strategies for wound-related pain need to be investigated. The ideal methods of pain relief for wound patients are modalities that are topical, lack systemic side effects, non-invasive, self-administered, and display rapid onset of analgesia...
August 14, 2017: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/28817987/targeting-cannabinoid-receptors-in-gastrointestinal-cancers-for-therapeutic-uses-current-status-and-future-perspectives
#5
Ester Pagano, Francesca Borrelli
No abstract text is available yet for this article.
August 18, 2017: Expert Review of Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28815938/optimization-of-recombinant-%C3%AE-glucuronidase-hydrolysis-and-quantification-of-eight-urinary-cannabinoids-and-metabolites-by-liquid-chromatography-tandem-mass-spectrometry
#6
Cristina Sempio, Karl B Scheidweiler, Allan J Barnes, Marilyn A Huestis
Prolonged urinary cannabinoid excretion in chronic frequent cannabis users confounds identification of recent cannabis intake that may be important in treatment, workplace, clinical, and forensic testing programs. In addition, differentiation of synthetic Δ9-tetrahydrocannabinol (THC) intake from cannabis plant products might be an important interpretive issue. THC, 11-hydroxy-THC (11-OH-THC) and 11-nor-9-carboxy-THC (THCCOOH) urine concentrations were evaluated during previous controlled cannabis administration studies following tandem alkaline/E...
June 14, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28815463/the-many-faces-and-phases-of-ceramide-and-sphingomyelin-i-single-lipids
#7
REVIEW
María Laura Fanani, Bruno Maggio
Ceramides, the simplest kind of two-chained sphingolipids, contain a single hydroxyl group in position 1 of the sphingoid base. Sphingomyelins further contain a phosphocholine group at the OH of position 1 of ceramide. Ceramides and sphingomyelins show a variety of species depending on the fatty acyl chain length, hydroxylation, and unsaturation. Because of the relatively high transition temperature of sphingomyelin compared to lecithin and, particularly, of ceramides with 16:0-18:0 saturated chains, a widespread idea on their functional importance refers to formation of rather solid domains enriched in sphingomyelin and ceramide...
August 16, 2017: Biophysical Reviews
https://www.readbyqxmd.com/read/28815276/determination-of-89-drugs-and-other-micropollutants-in-unfiltered-wastewater-and-freshwater-by-lc-ms-ms-an-alternative-sample-preparation-approach
#8
Alexandros G Asimakopoulos, Pranav Kannan, Sean Higgins, Kurunthachalam Kannan
A liquid chromatography-triple quadrupole-tandem mass spectrometry (LC-qQq-MS/MS) method was developed for simultaneous determination of 89 legal neuropsychiatric pharmaceuticals and illicit drugs (both parent compounds and metabolites) and other micropollutants in unfiltered wastewater and freshwater. The target chemicals fall under the classes of amphetamine-type stimulants, cocaine compounds, opiates and opioids, benzodiazepines, lysergic compounds, antipsychotics, anesthetics, antiepileptics, antidepressants, sympathomimetics, cannabinoids, blood thinners, antihistamines, β-blockers, caffeine derivatives, nicotine derivatives, z-drugs, new designer drugs, and Alzheimer medications...
August 16, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28815215/structural-characterization-of-acidic-m17-leucine-aminopeptidases-from-the-tritryps-and-evaluation-of-their-role-in-nutrient-starvation-in-trypanosoma-brucei
#9
Jennifer Timm, Maria Valente, Daniel García-Caballero, Keith S Wilson, Dolores González-Pacanowska
Leucine aminopeptidase (LAP) is found in all kingdoms of life and catalyzes the metal-dependent hydrolysis of the N-terminal amino acid residue of peptide or amino acyl substrates. LAPs have been shown to participate in the N-terminal processing of certain proteins in mammalian cells and in homologous recombination and transcription regulation in bacteria, while in parasites, they are involved in host cell invasion and provision of essential amino acids for growth. The enzyme is essential for survival in Plasmodium falciparum, where its drug target potential has been suggested...
July 2017: MSphere
https://www.readbyqxmd.com/read/28814545/metabolic-differentiation-of-early-lyme-disease-from-southern-tick-associated-rash-illness-stari
#10
Claudia R Molins, Laura V Ashton, Gary P Wormser, Barbara G Andre, Ann M Hess, Mark J Delorey, Mark A Pilgard, Barbara J Johnson, Kristofor Webb, M Nurul Islam, Adoracion Pegalajar-Jurado, Irida Molla, Mollie W Jewett, John T Belisle
Lyme disease, the most commonly reported vector-borne disease in the United States, results from infection with Borrelia burgdorferi. Early clinical diagnosis of this disease is largely based on the presence of an erythematous skin lesion for individuals in high-risk regions. This, however, can be confused with other illnesses including southern tick-associated rash illness (STARI), an illness that lacks a defined etiological agent or laboratory diagnostic test, and is coprevalent with Lyme disease in portions of the eastern United States...
August 16, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/28813324/cannabinoids-as-therapeutic-for-ptsd
#11
REVIEW
Mallory Je Loflin, Kimberly A Babson, Marcel O Bonn-Miller
Limited efficacy for current pharmacotherapy for PTSD indicates that improved pharmacological treatments are needed. Neurobiological research points to cannabinoids as possible therapeutic agents of interest. Moreover, observational reports indicate that there is growing popular interest in therapeutic use of cannabinoids for the alleviation of trauma symptoms. The aim of this review was to present an up-to-date look at current research on the possible therapeutic value of cannabinoids for PTSD. Experimental, preclinical, and clinical findings are discussed...
April 2017: Current Opinion in Psychology
https://www.readbyqxmd.com/read/28813207/examination-of-synthetic-cannabinoid-and-cathinone-use-among-a-drug-using-offender-sample-2013-2015
#12
Kirsten Elin Smith, Amanda M Bunting, Michele Staton, Robert Walker, Sara Shalash, Erin Winston, Kevin Pangburn
Use of novel psychoactive substances (NPS) such as synthetic cannabinoids (e.g., "Spice," "Serenity") and cathinones (e.g., "bath salts") has proliferated in recent years; however, there is a gap in research examining prevalence among offender samples. This study examined demographics, drug use, mental health characteristics, and criminal histories of NPS users compared to non-NPS users within an offender sample entering drug treatment. Using logistic regression analysis, combined 2013-2015 assessment data were examined (N = 8,791)...
August 16, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28812898/enantioselective-n-heterocyclic-carbene-catalyzed-synthesis-of-functionalized-indenes
#13
Changhe Zhang, David W Lupton
An enantioselective NHC (N-heterocyclic carbene) catalyzed synthesis of indenes from bifunctional α,β-unsaturated acyl fluorides and TMS enol ethers has been discovered. The reaction has broad generality (31 examples) and proceeds with high levels of enantioselectivity (most >92:8 er). Mechanistically the reaction likely occurs via a Michael/β-lactonization/decarboxylation sequence. Derivatization studies and limitations are discussed.
August 16, 2017: Organic Letters
https://www.readbyqxmd.com/read/28811670/sex-dependent-effects-of-cannabis-and-cannabinoids-a-translational-perspective
#14
Ziva D Cooper, Rebecca M Craft
Recent policy changes have led to significant increases in the use of cannabis for both medical and recreational purposes. Although men are more likely to endorse past month cannabis use and are more frequently diagnosed with Cannabis Use Disorder relative to women, a growing proportion of medical cannabis users are reported to be women. The increased popularity of cannabis for medical purposes and the narrowing gap in prevalence of use between men and women raises questions regarding sex-dependent effects related to therapeutic efficacy and negative health effects of cannabis and cannabinoids...
July 17, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28811049/marijuana-and-cannabinoids-in-esrd-and-earlier-stages-of-ckd
#15
Joshua L Rein, Christina M Wyatt
Marijuana is the most commonly used recreational drug in the United States, and legal recreational and medicinal use has gained public acceptance during the last decade. Twenty-nine US states have established medical marijuana programs, 8 of which have also legalized recreational marijuana, and Canada is expected to legalize recreational marijuana in 2018. Advanced chronic kidney disease (CKD) and end-stage renal disease (ESRD) are chronic conditions with significant associated morbidity and mortality. Patients experience substantial symptom burden that is frequently undertreated due to adverse medication side effects...
August 12, 2017: American Journal of Kidney Diseases: the Official Journal of the National Kidney Foundation
https://www.readbyqxmd.com/read/28809492/a-mild-functional-group-tolerant-addition-of-organozinc-nucleophiles-to-n-activated-quinolines-and-isoquinolines
#16
Michael R Luzung, Darryl D Dixon, Adrian Ortiz, Carlos A Guerrero, Sloan Ayers, Jeanne Ho, Michael A Schmidt, Neil A Strotman, Martin D Eastgate
An addition of organozinc nucleophiles to N-acyl activated quinolines and isoquinolines is described. Simple transmetalla-tion with the corresponding Grignard reagents using ZnCl2 forms organozinc compounds which are functional group tolerant and stable to reactive acyl chloride reagents for extended periods. A wide variety of substrates which include reactive elec-tron-withdrawing groups are well tolerated to form 2-substituted dihydroquinolines and dihydroisoquinolines. This method-ology has been applied towards an improved synthetic route of uncialamycin and its analogs...
August 15, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28808587/oral-administration-of-the-endocannabinoid-anandamide-during-lactation-effects-on-hypothalamic-cannabinoid-type-1-receptor-and-food-intake-in-adult-mice
#17
Carolina Aguirre, Valeska Castillo, Miguel Llanos
We have previously shown that administration of the endocannabinoid anandamide (AEA) during lactation leads to overweight, increased body fat accumulation, and insulin resistance in adult mice. This study was designed to elucidate if these effects are due to increased food intake, stimulated by an augmented abundance and binding ability of the hypothalamic cannabinoid type 1 receptor (CB1R). With this aim, male mice pups were treated with a daily oral dose of AEA during lactation. Adult mice were also treated with a single oral dose of AEA, to evaluate acute food intake during 4 h...
2017: Journal of Nutrition and Metabolism
https://www.readbyqxmd.com/read/28808371/efficacy-of-osteopathic-manipulative-treatment-approach-in-the-patient-with-pulmonary-fibrosis-in-critical-care-outpatient-department
#18
Manu Goyal, Kanu Goyal, Kanimozhi Narkeesh, Asir John Samuel, Narkeesh Arumugam, Subhasish Chatterjee, Sorabh Sharma
The purpose of the present case study was to explore the efficacy of osteopathic manipulative treatment (OMT) in patient with pulmonary fibrosis (PF) in the critical care outpatient department. Here, we present a 48-year-old male case with breathlessness, increased frequency of defecation, and pain in and around the nape of neck with diagnosed pulmonary fibrosis. He scored 3 on a patient-reported modified Medical Research Council (mMRC) dyspnea scale. Osteopathic examination reveals multiple somatic findings across the chest and abdominal region and treated by OMT...
July 2017: Indian Journal of Critical Care Medicine
https://www.readbyqxmd.com/read/28805227/landscape-of-the-structure-o-h-bond-dissociation-energy-relationship-of-oximes-and-hydroxylamines
#19
Rina Dao, Xinyu Wang, Kexian Chen, Chenxuan Zhao, Jia Yao, Haoran Li
The relationship between the homolytic O-H bond dissociation enthalpies (BDEs) and the structures of N-oxyl radical precursors (i.e. hydroxylamines and oximes) is important to predict their reactivity. Yet several crucial facts remain hidden to complete the picture such as the substituent electronic effects on the BDEs of oximes. In this work, the O-H BDEs of 120 hydroxylamines and 120 oximes have been calculated. It was found that the majority of the iminoxyl radicals are σ radicals, except for some π radicals...
August 14, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28803965/the-great-divide-separation-between-in-vitro-and-in-vivo-effects-of-psncbam-based-cb1-receptor-allosteric-modulators
#20
Thomas F Gamage, Charlotte E Farquhar, Timothy W Lefever, Brian F Thomas, Thuy Nguyen, Yanan Zhang, Jenny L Wiley
While allosteric modulators of the cannabinoid type-1 receptor (CB1) continue to be developed and characterized, the gap between the in vitro and in vivo data is widening, raising questions regarding translatability of their effects and biological relevance. Among the CB1 allosteric modulators, PSNCBAM-1 has received little attention regarding its effects in vivo. Recently, pregnenolone was reported to act as an allosteric modulator of CB1, blocking THC's effects in vitro and in vivo, highlighting the potential of CB1 allosteric modulators for treatment of cannabis intoxication...
August 10, 2017: Neuropharmacology
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