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https://www.readbyqxmd.com/read/27913166/dose-dependent-effect-of-donepezil-administration-on-long-term-enhancement-of-visually-evoked-potentials-and-cholinergic-receptor-overexpression-in-rat-visual-cortex
#1
Mira Chamoun, Marianne Groleau, Menakshi Bhat, Elvire Vaucher
Stimulation of the cholinergic system tightly coupled with periods of visual stimulation boosts the processing of specific visual stimuli via muscarinic and nicotinic receptors in terms of intensity, priority and long-term effect. However, it is not known whether more diffuse pharmacological stimulation with donepezil, a cholinesterase inhibitor, is an efficient tool for enhancing visual processing and perception. The goal of the present study was to potentiate cholinergic transmission with donepezil treatment (0...
November 29, 2016: Journal of Physiology, Paris
https://www.readbyqxmd.com/read/27909459/a-case-of-ileus-in-a-patient-with-schizophrenia-under-paliperidone-palmitate-treatment
#2
Serdar Süleyman Can, Esra Kabadayı
Constipation is a side effect of antipsychotic drugs that have high affinity for muscarinic cholinergic receptors. In addition, ileus is an important side effect of antipsychotic treatment, with potentially morbid and mortal consequences if early detection fails. In this report, a colonic ileus case is described in a patient with schizophrenia under the treatment of paliperidone palmitate. Consequently, complete physical examination and close screening of side effects are recommended when antipsychotics are prescribed...
November 2016: Psychiatry Investigation
https://www.readbyqxmd.com/read/27908290/bile-acid-a-potential-inducer-of-colon-cancer-stem-cells
#3
Lulu Farhana, Pratima Nangia-Makker, Evan Arbit, Kathren Shango, Sarah Sarkar, Hamidah Mahmud, Timothy Hadden, Yingjie Yu, Adhip P N Majumdar
BACKGROUND: Although the unconjugated secondary bile acids, specifically deoxycholic acid (DCA) and lithocholic acid (LCA), are considered to be risk factors for colorectal cancer, the precise mechanism(s) by which they regulate carcinogenesis is poorly understood. We hypothesize that the cytotoxic bile acids may promote stemness in colonic epithelial cells leading to generation of cancer stem cells (CSCs) that play a role in the development and progression of colon cancer. METHODS: Normal human colonic epithelial cells (HCoEpiC) were used to study bile acid DCA/LCA-mediated induction of CSCs...
December 1, 2016: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/27903755/homobivalent-conjugation-increases-the-allosteric-effect-of-9-aminoacridine-at-the-%C3%AE-1-adrenergic-receptors
#4
Adrian P Campbell, Laurence P G Wakelin, William A Denny, Angela M Finch
The α1 adrenergic receptors are targets for a number of cardiovascular and CNS conditions, however current drugs for these receptors lack specificity to be of optimal clinical value. Allosteric modulators offer an alternative mechanism of action to traditional α1 adrenergic ligands, yet there is little information describing this drug class at the α1 adrenergic receptors. We have identified a series of 9-aminoacridine compounds that demonstrate allosteric modulation of the α1A and α1B adrenergic receptors...
November 30, 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27900215/drug-treatment-of-bothersome-lower-urinary-tract-symptoms-after-ureteric-jj-stent-insertion-a-contemporary-comparative-prospective-randomised-placebo-controlled-study-single-centre-experience
#5
Ihab A Hekal
OBJECTIVE: To provide a guide for medication to alleviate bothersome lower urinary tract symptoms (LUTS) in patients after JJ ureteric stenting. PATIENTS AND METHODS: Between June 2011 and June 2015, a prospective randomised placebo-controlled study was conducted on 200 consecutive cases of ureteric stones that required JJ stents. All patients had signed informed consent and JJ-stent placement confirmed by X-ray. The patients were randomised into five groups: A, solifenacin 5 mg; B, trospium chloride 20 mg; C, antispasmodic; and E, α-blocker; and a placebo group (D)...
December 2016: Arab Journal of Urology
https://www.readbyqxmd.com/read/27899232/expression-of-muscarinic-acetylcholine-receptors-in-hepatocytes-from-rat-fibrotic-liver
#6
Lin Luo, Tingting Xu, Pengbo Wang, Liuliu Mao, Chenghao Xi, Jinhua Huang, Wei Zhang
The pathological changes of parasympathetic nerve are considered as an independent prognostic factor of the survival rate of patients with chronic liver disease. The non-selective muscarinic acetylcholine receptors (mAchR) agonists and antagonists can affect the proliferation of hepatocytes and hepatic stellate cells, but the subtypes of mAchR expressions in HCs are still uncertain. Here, we investigate the expression of mAchR in hepatic fibrosis on rats. 3ml/kg 40% carbon tetrachloride (CCL4) was given to induce hepatic fibrosis on rats and the hepatocytes were isolated...
November 26, 2016: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
https://www.readbyqxmd.com/read/27895421/carbon-monoxide-contributes-to-the-constipating-effects-of-granisetron-in-rat-colon
#7
Carmela Nacci, Margherita Fanelli, Maria Assunta Potenza, Valentina Leo, Monica Montagnani, Maria Antonietta De Salvia
AIM: To investigate the mechanisms underlying the potential contribution of the heme oxygenase/carbon monoxide (HO/CO) pathway in the constipating effects of granisetron. METHODS: For in vivo studies, gastrointestinal motility was evaluated in male rats acutely treated with granisetron [25, 50, 75 μg/kg/subcutaneous (sc)], zinc protoporphyrin IX [ZnPPIX, 50 μg/kg/intraperitoneal (ip)] and hemin (50 μmol/L/kg/ip), alone or in combination. For in vitro studies, the contractile neurogenic response to electrical field stimulation (EFS, 3, 5, 10 Hz, 14 V, 1 ms, pulse trains lasting 10 s), as well as the contractile myogenic response to acetylcholine (ACh, 0...
November 14, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27889577/brain-uptake-and-metabolism-of-the-endocannabinoid-anandamide-labeled-in-either-the-arachidonoyl-or-ethanolamine-moiety
#8
Kun Hu, Shilpa Sonti, Sherrye T Glaser, Richard I Duclos, Samuel J Gatley
INTRODUCTION: Anandamide (N-arachidonoylethanolamine) is a retrograde neuromodulator that activates cannabinoid receptors. The concentration of anandamide in the brain is controlled by fatty acid amide hydrolase (FAAH), which has been the focus of recent drug discovery efforts. Previous studies in C57BL/6 mice using [(3)H-arachidonoyl]anandamide demonstrated deposition of tritium in thalamus and cortical areas that was blocked by treatment with an FAAH inhibitor and that was not seen in FAAH-knockout mice...
November 9, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27888375/hbk-14-and-hbk-15-with-antidepressant-like-and-or-memory-enhancing-properties-increase-serotonin-levels-in-the-hippocampus-after-chronic-treatment-in-mice
#9
Karolina Pytka, Katarzyna Gawlik, Dorota Pawlica-Gosiewska, Jadwiga Witalis, Anna Waszkielewicz
5-HT1A and 5-HT7 receptor ligands might have antidepressant-like properties and improve cognitive function. We previously reported significant antidepressant- and anxiolytic-like effects of two dual 5-HT1A and 5-HT7 receptor antagonists in various behavioral tests in rodents. As a continuation of our previous experiments, in this study we aimed to investigate whether chronic administration of 1-[(2,6-dimethylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15) caused antidepressant-like effects and elevated serotonin levels in the murine hippocampus...
November 25, 2016: Metabolic Brain Disease
https://www.readbyqxmd.com/read/27888045/effects-of-tiotropium-on-lung-function-in-current-smokers-and-never-smokers-with-bronchial-asthma
#10
Makoto Yoshida, Yasuko Kaneko, Akiko Ishimatsu, Masashi Komori, Tomoaki Iwanaga, Hiromasa Inoue
The effects of tiotropium, an inhaled long-acting muscarinic antagonist, on lung function were investigated in current smokers and nonsmokers with asthma treated with inhaled corticosteroids (ICSs) and other asthma controllers: inhaled long-acting β2 agonists, leukotriene receptor antagonists, and/or theophylline. We conducted a double-blind, placebo-controlled study of an inhaled single dose of tiotropium in 9 asthmatics currently smoking and 9 asthmatics who have never smoked in a crossover manner. Lung function was measured before and 1, 3, and 24 h after inhalation of 18 μg of tiotropium or a placebo...
November 22, 2016: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27883993/stimulation-of-the-nonneuronal-cholinergic-system-by-highly-diluted-acetylcholine-in-keratinocytes
#11
Francesca Uberti, Claudio Bardelli, Vera Morsanuto, Sabrina Ghirlanda, Andrea Cochis, Claudio Molinari
The physiological effects of acetylcholine on keratinocytes depend on the presence of nicotinic and muscarinic receptors. The role of nonneuronal acetylcholine in keratinocytes could have important clinical implications for patients with various skin disorders such as nonhealing wounds. In order to evaluate the efficacy of highly diluted acetylcholine solutions obtained by sequential kinetic activation, we aimed to investigate the effects of these solutions on normal human keratinocytes. Two different concentrations (10 fg/mL and 1 pg/mL) and formulations (kinetically activated and nonkinetically activated) of acetylcholine were used to verify keratinocyte viability, proliferation, and migration and the intracellular pathways involved using MTT, crystal violet, wound healing, and Western blot compared to 147 ng/mL acetylcholine...
November 25, 2016: Cells, Tissues, Organs
https://www.readbyqxmd.com/read/27882567/autoantibodies-directed-against-the-endothelin-a-receptor-in-patients-with-benign-prostatic-hyperplasia
#12
Gerd Wallukat, Burkhard Jandrig, Rudolf Kunze, Johann J Wendler, Johannes Müller, Martin Schostak, Ingolf Schimke
BACKGROUND: Over-stimulation of G-protein coupled receptors (GPCRs) such as α1-adrenergic, muscarinic, endothelin, and AT1 receptors is considered to drive benign prostatic hyperplasia (BHP) which is often associated with lower urinary tract syndrome (LUTS). However, in addition to physiologic GPCR ligands, there is a new class of autoantibodies called functional autoantibodies that target the same GPCRs (GPCR-AABs) for over-stimulation, thus, presenting pathogenic potency. We hypothesize that patients with BPH/LUTS could carry GPCR-AABs representing potential targets for treatment...
November 24, 2016: Prostate
https://www.readbyqxmd.com/read/27873015/muscarinic-receptor-binding-changes-in-postmortem-parkinson-s-disease
#13
Caitlin McOmish, Geoff Pavey, Catriona McLean, Malcolm Horne, Brian Dean, Elizabeth Scarr
Parkinson's disease (PD) is a devastating disorder, affecting approximately 2% of people aged 60 and above. It is marked by progressive neurodegeneration that has long been known to impact dopaminergic cells and circuits, but more recently the acetylcholine system has also been implicated in the complex aetiology and symptomatology of the disease. While broad changes in cholinergic markers have been described, insight into the contribution of specific acetylcholine receptors is less clear. To address this important unknown, in this study we performed [(3)H] pirenzepine, [(3)H] 4DAMP, and [(3)H] AF-DX 384 in situ radioligand binding on postmortem tissues from Brodmann's area 6, 9, 46, and the caudate putamen, from PD and matched controls to detect muscarinic M1, M3, and M1/2/4 receptors, respectively...
November 21, 2016: Journal of Neural Transmission
https://www.readbyqxmd.com/read/27872646/mercury-vapour-long-lasting-exposure-lymphocyte-muscarinic-receptors-as-neurochemical-markers-of-accidental-intoxication
#14
E Roda, A Giampreti, S Vecchio, P Apostoli, T Coccini
Introduction. Chronic poisoning may result in home setting after mercury (Hg) vapours inhalation from damaged devices. We report a chronic, nonoccupational Hg poisoning due to 10-year indoor exposure to mercury spillage. Case Report. A 72-year-old man with polyneuropathy of suspected toxic origin. At hospitalization, toxicological clinical evaluations confirmed the altered neurological picture documented across the last decade. Periodic blood and urine Hg levels (BHg, UHg) monitoring were performed from admission (t0), until 1 year later (t2), paralleled by blood neurochemical markers assessment, that is, lymphocytes muscarinic receptors (l-MRs)...
2016: Case Reports in Medicine
https://www.readbyqxmd.com/read/27866962/distribution-of-muscarinic-acetylcholine-receptor-subtypes-in-the-murine-small-intestine
#15
Eleanor D Muise, Neeru Gandotra, John J Tackett, Michaela C Bamdad, Robert A Cowles
AIMS: Serotonin stimulates enterocyte turnover in the small intestine and studies suggest this is mediated by neuronal signaling via a cholinergic pathway. Distribution of the five known muscarinic receptor subtypes (mAChRs) in the small intestine has not been fully studied, and their role in intestinal growth is unknown. We hypothesized that mAChRs have distinct anatomic distributions within the bowel, and that mAChRs present within intestinal crypts mediate the effects of acetylcholine on the small intestinal mucosa...
November 17, 2016: Life Sciences
https://www.readbyqxmd.com/read/27866902/the-atypical-antipsychotic-olanzapine-disturbs-depotentiation-by-modulating-machrs-and-impairs-reversal-learning
#16
Woo Seok Song, Jin Hee Cha, Sang Ho Yoon, Young Seon Cho, Kyeong-Yeol Park, Myoung-Hwan Kim
Antipsychotic medication is an essential component for treating schizophrenia, which is a serious mental disorder that affects approximately 1% of the global population. Olanzapine (Olz), one of the most frequently prescribed atypical antipsychotics, is generally considered a first-line drug for treating schizophrenia. In contrast to psychotic symptoms, the effects of Olz on cognitive symptoms of schizophrenia are still unclear. In addition, the mechanisms by which Olz affects the neural circuits associated with cognitive function are unknown...
November 17, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27866739/an-integrated-approach-for-identifying-priority-contaminant-in-the-great-lakes-basin-investigations-in-the-lower-green-bay-fox-river-and-milwaukee-estuary-areas-of-concern
#17
Shibin Li, Daniel L Villeneuve, Jason P Berninger, Brett R Blackwell, Jenna E Cavallin, Megan N Hughes, Kathleen M Jensen, Zachary Jorgenson, Michael D Kahl, Anthony L Schroeder, Kyle E Stevens, Linnea M Thomas, Matthew A Weberg, Gerald T Ankley
Environmental assessment of complex mixtures typically requires integration of chemical and biological measurements. This study demonstrates the use of a combination of instrumental chemical analyses, effects-based monitoring, and bio-effects prediction approaches to help identify potential hazards and priority contaminants in two Great Lakes Areas of Concern (AOCs), the Lower Green Bay/Fox River located near Green Bay, WI, USA and the Milwaukee Estuary, located near Milwaukee, WI, USA. Fathead minnows were caged at four sites within each AOC (eight sites total)...
November 17, 2016: Science of the Total Environment
https://www.readbyqxmd.com/read/27866394/repeated-otilonium-bromide-administration-prevents-neurotransmitter-changes-in-colon-of-rats-underwent-to-wrap-restraint-stress
#18
Chiara Traini, Stefano Evangelista, Vincent Girod, Maria Simonetta Faussone-Pellegrini, Maria Giuliana Vannucchi
Otilonium bromide (OB) is a spasmolytic drug successfully used for the treatment of irritable bowel syndrome (IBS). Its efficacy has been attributed to the block of L- and T-type Ca(2+) channels and muscarinic and tachykinin receptors in the smooth muscle. Furthermore, in healthy rats, repeated OB administration modified neurotransmitter expression and function suggesting other mechanisms of action. On this basis, we investigated whether repeated OB treatment prevented the functional and neurochemical changes observed in the colon of rats underwent to wrap restrain stress (WRS) a psychosocial stressor considered suitable to reproduce the main IBS signs and symptoms...
November 20, 2016: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/27865910/multi-target-directed-therapeutic-potential-of-7-methoxytacrine-adamantylamine-heterodimers-in-the-alzheimer-s-disease-treatment
#19
Zuzana Gazova, Ondrej Soukup, Vendula Sepsova, Katarina Siposova, Lucie Drtinova, Petr Jost, Katarina Spilovska, Jan Korabecny, Eugenie Nepovimova, Diana Fedunova, Martin Horak, Martina Kaniakova, Ze-Jun Wang, Ayman K Hamouda, Kamil Kuca
Alzheimer's disease (AD) is a progressive neurodegenerative disorder and currently there is no efficient treatment. The classic drug-design strategy based on the "one-molecule-one-target" paradigm was found to be ineffective in the case of multifactorial diseases like AD. A novel multi-target-directed ligand strategy based on the assumption that a single compound consisting of two or more distinct pharmacophores is able to hit multiple targets has been proposed as promising. Herein, we investigated 7-methoxytacrine - memantine heterodimers developed with respect to the multi-target-directed ligand theory...
November 16, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27865771/cholinergic-activation-affects-the-acute-and-chronic-antinociceptive-effects-of-morphine
#20
Kinga Gawel, Ewa Gibula-Bruzda, Marcin Dziedzic, Malgorzata Jenda-Wojtanowska, Marta Marszalek-Grabska, Jerzy Silberring, Jolanta H Kotlinska
Current studies indicate that the cholinergic and opioid systems interact to modulate pain. In the present work, we investigated the influence of the cholinesterase inhibitors, donepezil (0.5; 1 or 3mg/kg, i.p.) and rivastigmine (0.03; 0.5 or 1mg/kg, i.p.), on the acute antinociceptive effects of morphine (5mg/kg, i.p.) in the hot plate test in mice. Herein, both inhibitors were found to enhance and prolong the analgesic effects of morphine without affecting latencies themselves. In an extension of this work, we determined which cholinergic receptors subtype mediates the enhancement of analgesic effects of morphine, following inhibition of cholinesterases...
November 16, 2016: Physiology & Behavior
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