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https://www.readbyqxmd.com/read/28549792/endocannabinoids-modulate-apoptosis-in-endometriosis-and-adenomyosis
#1
Elif Bilgic, Elif Guzel Meydanli, Sevil Kose, Makbule Cisel Aydin, Eda Karaismailoglu, Irem Akar, Alp Usubutun, Petek Korkusuz
Adenomyosis that is a form of endometriosis is the growth of ectopic endometrial tissue within the muscular wall of the uterus (myometrium), which may cause dysmenorrhea and infertility. Endocannabinoid mediated apoptotic mechanisms of endometriosis and adenomyosis are not known. We hypothesized that the down regulation of endocannabinoid receptors and/or alteration in their regulatory enzymes may have a direct role in the pathogenesis of endometriosis and adenomyosis through apoptosis. Endocannabinoid receptors CB1 and CB2, their synthesizing and catabolizing enzymes (FAAH, NAPE-PLD, DAGL, MAGL) and the apoptotic indexes were immunohistochemically assessed in endometriotic and adenomyotic tissues...
May 23, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28549258/immunohistochemical-localization-of-cannabinoid-receptor-1-cb1-in-the-submandibular-gland-of-mice-under-normal-conditions-and-when-stimulated-by-isoproterenol-or-carbachol
#2
Wipawee Thoungseabyoun, Apussara Tachow, Sawetree Pakkarato, Atsara Rawangwong, Suthankamon Krongyut, Waraporn Sakaew, Hisatake Kondo, Wiphawi Hipkaeo
OBJECTIVE: We wished to investigate the subcellular localization of CB1, a receptor for the endocannabinoids in mouse submandibular glands (SMGs) under normal conditions and when stimulated by adrenergic or cholinergic agonists. MATERIALS AND METHODS: SMGs of both male and female adult mice were utilized for immunoblotting and immuno-light and -electron microscopic analyses. Isoproterenol and carbachol were used as adrenergic and cholinergic stimulants, respectively...
May 17, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/28545167/synthesis-of-s-2-s-3-4-chlorophenyl-n-4-chlorophenyl-sulfonyl-4-phenyl-4-5-dihydro-1h-pyrazole-1-carboximidamido-3-methyl-d3-butanamide-d5-octa-deuterated-jd5037
#3
Malliga R Iyer, Resat Cinar, Nathan J Coffey, Robert J Chorvat, George Kunos
JD5037 (1) is a potent and selective, peripherally acting inverse agonist of the cannabinoid (CB1 R) receptor. Peripheral CB1 receptor antagonists/inverse agonists have great potential in the treatment of metabolic disorders like type 2 diabetes, obesity and NASH. We report the synthesis of octa-deuterated [(2) H8 ]-JD5037 (S, S) (8) along with its (S, R) diastereomer (13) from commercially available L-valine-d8 starting material. The [(2) H8 ]-JD5037 compound will be used to quantitate unlabeled JD5037 during clinical ADME studies and will be used as an LC-MS/MS bioanalytical standard...
May 25, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28544560/fatal-intoxication-by-5f-adb-and-diphenidine-detection-quantification-and-investigation-of-their-main-metabolic-pathways-in-human-by-lc-ms-ms-and-lc-q-tofms
#4
Maiko Kusano, Kei Zaitsua, Kentaro Taki, Kazuaki Hisatsune, Jun'ichi Nakajima, Takako Moriyasu, Tomomi Asano, Yumi Hayashi, Hitoshi Tsuchihashi, Akira Ishii
Despite the implementation of the new blanket scheduling system in 2013, new psychoactive substance (NPS) abuse remains a serious social concern in Japan. We present a fatal intoxication case involving 5F-ADB (methyl 2-[1-(5-fluoropentyl)-1H-indazole-3-carboxamido]-3,3-dimethylbutanoate) and diphenidine. Postmortem blood screening by liquid chromatography/quadrupole time-of-flight mass spectrometry (LC/Q-TOFMS) in the information dependent acquisition (IDA) mode only detected diphenidine. Further urinary screening using an in-house database containing new NPS and metabolites detected not only diphenidine but also possible 5F-ADB metabolites; subsequent targeted screening by LC/tandem mass spectrometry (LC/MS/MS) allowed for the detection of very low level of unchanged 5F-ADB in postmortem heart blood...
May 21, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28540200/targeting-cannabinoid-signaling-for-peritoneal-dialysis-induced-oxidative-stress-and-fibrosis
#5
REVIEW
Chih-Yu Yang, Yat-Pang Chau, Ann Chen, Oscar Kuang-Sheng Lee, Der-Cherng Tarng, An-Hang Yang
Long-term exposure to bioincompatible peritoneal dialysis (PD) solutions frequently results in peritoneal fibrosis and ultrafiltration failure, which limits the life-long use of and leads to the cessation of PD therapy. Therefore, it is important to elucidate the pathogenesis of peritoneal fibrosis in order to design therapeutic strategies to prevent its occurrence. Peritoneal fibrosis is associated with a chronic inflammatory status as well as an elevated oxidative stress (OS) status. Beyond uremia per se, OS also results from chronic exposure to high glucose load, glucose degradation products, advanced glycation end products, and hypertonic stress...
May 6, 2017: World Journal of Nephrology
https://www.readbyqxmd.com/read/28539997/interaction-between-the-cannabinoid-and-vanilloid-systems-on-anxiety-in-male-rats
#6
Nafiseh Faraji, Alireza Komaki, Iraj Salehi
INTRODUCTION: Previous studies have shown that the cannabinoid system is involved in anxiety. In addition, transient receptor potential vanilloid type-1 (TRPV1) channels are new targets for the development of anxiolytics. The present study investigated the possible interaction between the cannabinoid and vanilloid systems on anxiety-like behavior in rats. METHODS: Four different groups of male Wistar rats received intraperitoneal (IP) injections of (1) vehicle (DMSO+saline), (2) cannabinoid receptor agonist WIN55212-2 (WIN) (1 mg/kg), (3) TRPV1 receptor antagonist capsazepine (CPZ) (5 mg/kg), or (4) combined WIN (1 mg/kg) and CPZ (5 mg/kg) treatment 30 minutes before testing in the elevated plus maze...
March 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28536867/suppressing-effect-of-cor659-on-alcohol-sucrose-and-chocolate-self-administration-in-rats-involvement-of-the-gabab-and-cannabinoid-cb1-receptors
#7
Paola Maccioni, Giancarlo Colombo, Irene Lorrai, Alessandro Zaru, Mauro A M Carai, Gian Luigi Gessa, Antonella Brizzi, Claudia Mugnaini, Federico Corelli
RATIONALE AND OBJECTIVES: COR659 [methyl2-(4-chlorophenylcarboxamido)-4-ethyl-5-methylthiophene-3-carboxylate] is a new, positive allosteric modulator (PAM) of the GABAB receptor. This study evaluated whether COR659 shared with previously tested GABAB PAMs the capacity to reduce alcohol self-administration in rats. RESULTS: Treatment with non-sedative doses of COR659 (2.5, 5, and 10 mg/kg; i.p.) suppressed lever-responding for alcohol (15% v/v) in Sardinian alcohol-preferring (sP) rats under the fixed ratio (FR) 4 (FR4) and progressive ratio (PR) schedules of reinforcement; COR659 was more potent and effective than the reference GABAB PAM, GS39783...
May 24, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28536285/gut-microbiota-mediates-the-protective-effects-of-dietary-capsaicin-against-chronic-low-grade-inflammation-and-associated-obesity-induced-by-high-fat-diet
#8
Chao Kang, Bin Wang, Kanakaraju Kaliannan, Xiaolan Wang, Hedong Lang, Suocheng Hui, Li Huang, Yong Zhang, Ming Zhou, Mengting Chen, Mantian Mi
Metabolic endotoxemia originating from dysbiotic gut microbiota has been identified as a primary mediator for triggering the chronic low-grade inflammation (CLGI) responsible for the development of obesity. Capsaicin (CAP) is the major pungent bioactivator in chili peppers and has potent anti-obesity functions, yet the mechanisms linking this effect to gut microbiota remain obscure. Here we show that mice fed a high-fat diet (HFD) supplemented with CAP exhibit lower levels of metabolic endotoxemia and CLGI associated with lower body weight gain...
May 23, 2017: MBio
https://www.readbyqxmd.com/read/28533288/apparent-affinity-estimates-and-reversal-of-the-effects-of-synthetic-cannabinoids-am-2201-cp-47-497-jwh-122-and-jwh-250-by-rimonabant-in-rhesus-monkeys
#9
Lenka Hruba, Lance R McMahon
Synthetic cannabinoids have been prohibited due to abuse liability and toxicity. Four such synthetic cannabinoids, AM-2201, CP-47,497, JWH-122, and JWH-250, were tested for their capacity to produce CB1 receptor-mediated discriminative stimulus effects in two groups of rhesus monkeys. One group (n=4) discriminated ∆9-THC (0.1 mg/kg i.v.) and a second group (n=4) discriminated the cannabinoid antagonist rimonabant (1 mg/kg i.v.) while receiving 1 mg/kg/12 h of ∆9-THC. AM-2201, JWH-122, CP-47,497, JWH-250, and ∆9-THC increased ∆9-THC-lever responding...
May 22, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28529018/effects-of-anandamide-administration-on-components-of-reward-processing-during-free-choice
#10
Luke C Zona, Benjamin R Fry, Jacob A LaLonde, Howard C Cromwell
Previous research has implicated the positive modulation of anandamide, an endocannabinoid neurotransmitter, on feeding behavior. Anandamide is particularly noteworthy as it acts as an endogenous ligand of the CB1 receptor, the same receptor that is activated by tetrahydrocannabinol, the primary psychoactive component in Cannabis sativa. Cannabis legalization in North America has presented with a need to study endocannabinoid agonists and their effects on behavior. Much has yet to be determined in terms of the role of the endocannabinoid system in decision-making scenarios...
May 18, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28527758/modulation-of-cb1-cannabinoid-receptor-by-allosteric-ligands-pharmacology-and-therapeutic-opportunities
#11
REVIEW
Leepakshi Khurana, Ken Mackie, Daniele Piomelli, Debra A Kendall
Cannabinoid pharmacology has been intensely studied because of cannabis' pervasive medicinal and non-medicinal uses as well as for the therapeutic potential of cannabinoid-based drugs for the treatment of pain, anxiety, substance abuse, obesity, cancer and neurodegenerative disorders. The identification of allosteric modulators of the cannabinoid receptor 1 (CB1) has given a new direction to the development of cannabinoid-based therapeutics due to the many advantages offered by targeting allosteric site(s)...
May 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28526263/n-stearoyl-l-tyrosine-inhibits-the-cell-senescence-and-apoptosis-induced-by-h2o2-in-hek293-tau-cells-via-the-cb2-receptor
#12
Yue Hu, Kai-Yi Zhou, Ze-Jian Wang, Yang Lu, Ming Yin
Although considerable energy and money have been spent trying to inhibit Aβ production and its related metabolic enzyme activities, there are still no drug treatments available to cure even slow for Alzheimer's disease. Therefore, tau protein has been focused recently as the new target for the treatment of Alzheimer's disease. The transfected human embryonic kidney 293 (HEK 293) cells with or without Tau 411 plasmid were used to evaluate the effect of tau protein on cell viability. H2O2 was added to simulate microenvironment of oxidative stress (OS) during aging...
May 16, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28523112/development-of-highly-affine-and-selective-fluorinated-cannabinoid-type-2-receptor-ligands
#13
Rareş-Petru Moldovan, Kristin Hausmann, Winnie Deuther-Conrad, Peter Brust
Cannabinoid type 2 receptors (CB2 receptors) are involved in various pathological processes, and the visualization of their in vivo availability with positron emission tomography (PET) is of high interest. The study focuses on the introduction of fluorine into the structure of the highly affine and selective CB2 receptor ligand N-(adamantan-1-yl)-5-ethyl-2-methyl-1-phenyl-1H-imidazole-4-carboxamide (5). A novel series of compounds was developed by modifying (i) the adamantane-3-position, (ii) the imidazole-N-phenyl ring, and (iii) the imidazole-2-position, and the impact on the CB2 binding affinity and selectivity toward cannabinoid type 1 receptors (CB1) was evaluated...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28520937/atypical-endocannabinoid-signaling-initiates-a-new-form-of-memory-related-plasticity-at-a-cortical-input-to-hippocampus
#14
Weisheng Wang, Yousheng Jia, Danielle T Pham, Linda C Palmer, Kwang-Mook Jung, Conor D Cox, Gavin Rumbaugh, Daniele Piomelli, Christine M Gall, Gary Lynch
Endocannabinoids (ECBs) depress transmitter release at sites throughout the brain. Here, we describe another form of ECB signaling that triggers a novel form of long-term potentiation (LTP) localized to the lateral perforant path (LPP) which conveys semantic information from cortex to hippocampus. Two cannabinoid CB1 receptor (CB1R) signaling cascades were identified in hippocampus. The first is pregnenolone sensitive, targets vesicular protein Munc18-1 and depresses transmitter release; this cascade is engaged by CB1Rs in Schaffer-Commissural afferents to CA1 but not in the LPP, and it does not contribute to LTP...
May 17, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28516479/g%C3%AE-s-signalling-of-the-cb1-receptor-and-the-influence-of-receptor-number
#15
David B Finlay, Erin E Cawston, Natasha L Grimsey, Morag R Hunter, Anisha Korde, V Kiran Vemuri, Alexandros Makriyannis, Michelle Glass
BACKGROUND AND PURPOSE: CB1 cannabinoid receptor signalling is canonically mediated through inhibitory Gαi proteins, but signalling through other G proteins occurs under some circumstances; Gαs being the most characterised secondary pathway. Determinants of this signalling switch identified to date include Gαi blockade, CB1 /D2 dopamine receptor co-stimulation, CB1 agonist class, and cell background. The aim of this study was to examine the effects of receptor number and ligand dependence on CB1 signalling...
May 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28511899/signaling-pathways-to-and-from-the-hypophysial-pars-tuberalis-an-important-center-for-the-control-of-seasonal-rhythms
#16
REVIEW
Horst-Werner Korf
Seasonal (circannual) rhythms play an important role for the control of body functions (reproduction, metabolism, immune responses) in nearly all living organisms. Also humans are affected by the seasons with regard to immune responses and mental functions, the seasonal affective disorder being one of the most prominent examples. The hypophysial pars tuberalis (PT), an important interface between the hypophysial pars distalis and neuroendocrine centers in the brain, plays an essential role in the regulation of seasonal functions and may even be the seat of the circannual clock...
May 13, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28497982/neuroprotection-in-oxidative-stress-related-neurodegenerative-diseases-role-of-endocannabinoid-system-modulation
#17
Janos Paloczi, Zoltan V Varga, George Hasko, Pal Pacher
SIGNIFICANCE: Redox imbalance may lead to overproduction of reactive oxygen and nitrogen species (ROS/RNS) and subsequent oxidative tissue damage which is a critical event in the course of neurodegenerative diseases. It is still not fully elucidated, however, whether oxidative stress is the primary trigger or a consequence in process of neurodegeneration. Recent Advances: Increasing evidence suggests that oxidative stress is involved in the propagation of neuronal injury and consequent inflammatory response, which in concert promote development of pathological alterations characteristic of most common neurodegenerative diseases...
May 12, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28496122/structural-insights-into-a-20-8-kda-tegumental-allergen-like-tal-protein-from-clonorchis-sinensis
#18
Chang Hwa Jo, Jonghyeon Son, Sulhee Kim, Takashi Oda, Jaehoon Kim, Myoung-Ro Lee, Mamoru Sato, Hyun Tae Kim, Satoru Unzai, Sam-Yong Park, Kwang Yeon Hwang
Survival of Clonorchis sinensis, a cause of human clonorchiasis, requires tegument proteins, which are localized to the tegumental outer surface membrane. These proteins play an important role in a host response and parasite survival. Thus, these proteins are interesting molecular targets for vaccine and drug development. Here, we have determined two crystal structures of the calmodulin like domain (amino acid [aa] positions 1-81) and dynein light chain (DLC)-like domain (aa 83-177) of a 20.8-kDa tegumental-allergen-like protein from Clonorchis sinensis (CsTAL3)...
May 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28496039/pyrolysis-of-ur-144-a-synthetic-cannabinoid-augments-an-affinity-to-human-cb1-receptor-and-cannabimimetic-effects-in-mice
#19
Asuka Kaizaki-Mitsumoto, Kyoko Hataoka, Masahiko Funada, Yuki Odanaka, Hiroki Kumamoto, Satoshi Numazawa
Drug abusers most often smoke 'herbal incense' as a cigarette or inhale it using a smoking tool. Smoking may cause pyrolysis of the drug and produce decomposed products of which biological effect has never been investigated. The synthetic cannabinoid UR-144 is known to undergo thermal degradation, giving a ring-opened isomer, so-called UR-144 degradant. The present study demonstrates by using UR-144 as a model drug that the smoke of burned UR-144 contains the UR-144 degradant. The UR-144 degradant showed approximately four fold higher agonist activity to human CB1 receptor and augmented hypothermic and akinetic actions in mice compared to UR-144...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28495855/marijuana-smoke-induces-severe-pulmonary-hyperresponsiveness-inflammation-and-emphysema-in-a-predictive-mouse-model-not-via-cb1-receptor-activation
#20
Zsuzsanna Helyes, Ágnes Kemény, Kata Csekő, Eva Szoke, Krisztian Elekes, Miklós Mester, Katalin Sándor, Anikó Perkecz, László Kereskai, Laszlo Mark, Ágnes Bona, András Benkő, Erika Pintér, János Szolcsányi, Catherine Ledent, Beáta Sperlágh, Tamás F Molnár
Sporadic clinical reports suggested that marijuana smoking induces spontaneous pneumothorax, but no animal models were available to validate these observations and to study the underlying mechanisms. Therefore, we performed a systematic study in CD1 mice as a predictive animal model and assessed the pathophysiological alterations in response to 4-month-long whole body marijuana smoke with integrative methodologies in comparison with tobacco smoke. Bronchial responsiveness was measured with unrestrained whole body plethysmography, cell profile in the bronchoalveolar lavage fluid with flow-cytometry, myeloperoxidase activity with spectrophotometry, inflammatory cytokines with ELISA, and histopathological alterations by light microscopy...
May 11, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
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