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https://www.readbyqxmd.com/read/27909995/solithromycin-a-novel-fluoroketolide-for-the-treatment-of-community-acquired-bacterial-pneumonia
#1
REVIEW
George G Zhanel, Erika Hartel, Heather Adam, Sheryl Zelenitsky, Michael A Zhanel, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew J Walkty, Alfred S Gin, Daryl J Hoban, Joseph P Lynch, James A Karlowsky
Solithromycin is a novel fluoroketolide developed in both oral and intravenous formulations to address increasing macrolide resistance in pathogens causing community-acquired bacterial pneumonia (CABP). When compared with its macrolide and ketolide predecessors, solithromycin has several structural modifications which increase its ribosomal binding and reduce its propensity to known macrolide resistance mechanisms. Solithromycin, like telithromycin, affects 50S ribosomal subunit formation and function, as well as causing frame-shift errors during translation...
December 1, 2016: Drugs
https://www.readbyqxmd.com/read/27908269/levamisole-a-positive-allosteric-modulator-for-the-%C3%AE-3%C3%AE-4-nicotinic-acetylcholine-receptors-prevents-weight-gain-in-cd-1-mice-on-a-high-fat-diet
#2
Jeanne A Lewis, Jerrel L Yakel, Anshul A Pandya
Neuronal nicotinic acetylcholine receptors (nAChRs) regulate the function of multiple neurotransmitter pathways throughout the central nervous system. This includes nAChRs found on the proopiomelanocortin neurons in the hypothalamus. Activation of these nAChRs by nicotine causes a decrease in consumption of food in rodents. In this study, we tested the effect of subtype selective allosteric modulators for nAChRs on the body weight of CD-1 mice. Levamisole, an allosteric modulator for the α3β4 subtype of nAChRs, prevented weight gain in mice that were fed a high fat diet...
December 1, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27907050/when-is-the-brain-dead-living-like-electrophysiological-responses-and-photon-emissions-from-applications-of-neurotransmitters-in-fixed-post-mortem-human-brains
#3
Michael A Persinger, Nicolas Rouleau, Nirosha J Murugan, Lucas W E Tessaro, Justin N Costa
The structure of the post-mortem human brain can be preserved by immersing the organ within a fixative solution. Once the brain is perfused, cellular and histological features are maintained over extended periods of time. However, functions of the human brain are not assumed to be preserved beyond death and subsequent chemical fixation. Here we present a series of experiments which, together, refute this assumption. Instead, we suggest that chemical preservation of brain structure results in some retained functional capacity...
2016: PloS One
https://www.readbyqxmd.com/read/27907022/nicotine-induces-podocyte-apoptosis-through-increasing-oxidative-stress
#4
Xiqian Lan, Rivka Lederman, Judith M Eng, Seyedeh Shadafarin Marashi Shoshtari, Moin A Saleem, Ashwani Malhotra, Pravin C Singhal
BACKGROUND: Cigarette smoking plays an important role in the progression of chronic kidney disease (CKD). Nicotine, one of the major components of cigarette smoking, has been demonstrated to increase proliferation of renal mesangial cells. In this study, we examined the effect of nicotine on podocyte injury. METHODS: To determine the expression of nicotinic acetylcholine receptors (nAChR subunits) in podocytes, cDNAs and cell lysate of cultured human podocytes were used for the expression of nAChR mRNAs and proteins, respectively; and mouse renal cortical sections were subjected to immunofluorescant staining...
2016: PloS One
https://www.readbyqxmd.com/read/27905561/anti-hu-antibodies-activate-enteric-and-sensory-neurons
#5
Qin Li, Klaus Michel, Anita Annahazi, Ihsan E Demir, Güralp O Ceyhan, Florian Zeller, Lars Komorowski, Winfried Stöcker, Michael J Beyak, David Grundy, Gianrico Farrugia, Roberto De Giorgio, Michael Schemann
IgG of type 1 anti-neuronal nuclear antibody (ANNA-1, anti-Hu) specificity is a serological marker of paraneoplastic neurological autoimmunity (including enteric/autonomic) usually related to small-cell lung carcinoma. We show here that IgG isolated from such sera and also affinity-purified anti-HuD label enteric neurons and cause an immediate spike discharge in enteric and visceral sensory neurons. Both labelling and activation of enteric neurons was prevented by preincubation with the HuD antigen. Activation of enteric neurons was inhibited by the nicotinic receptor antagonists hexamethonium and dihydro-β-erythroidine and reduced by the P2X antagonist pyridoxal phosphate-6-azo (benzene-2,4-disulfonic acid (PPADS) but not by the 5-HT3 antagonist tropisetron or the N-type Ca-channel blocker ω-Conotoxin GVIA...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27901080/block-of-nicotinic-acetylcholine-receptors-by-philanthotoxins-is-strongly-dependent-on-their-subunit-composition
#6
Hamid S Kachel, Rohit N Patel, Henrik Franzyk, Ian R Mellor
Philanthotoxin-433 (PhTX-433) is an active component of the venom from the Egyptian digger wasp, Philanthus triangulum. PhTX-433 inhibits several excitatory ligand-gated ion channels, and to improve selectivity two synthetic analogues, PhTX-343 and PhTX-12, were developed. Previous work showed a 22-fold selectivity of PhTX-12 over PhTX-343 for embryonic muscle-type nicotinic acetylcholine receptors (nAChRs) in TE671 cells. We investigated their inhibition of different neuronal nAChR subunit combinations as well as of embryonic muscle receptors expressed in Xenopus oocytes...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27899792/nature-nurtures-the-design-of-new-semi-synthetic-macrolide-antibiotics
#7
REVIEW
Prabhavathi Fernandes, Evan Martens, David Pereira
Erythromycin and its analogs are used to treat respiratory tract and other infections. The broad use of these antibiotics during the last 5 decades has led to resistance that can range from 20% to over 70% in certain parts of the world. Efforts to find macrolides that were active against macrolide-resistant strains led to the development of erythromycin analogs with alkyl-aryl side chains that mimicked the sugar side chain of 16-membered macrolides, such as tylosin. Further modifications were made to improve the potency of these molecules by removal of the cladinose sugar to obtain a smaller molecule, a modification that was learned from an older macrolide, pikromycin...
November 30, 2016: Journal of Antibiotics
https://www.readbyqxmd.com/read/27896932/mesoionic-insecticides-a-novel-class-of-insecticides-that-modulate-nicotinic-acetylcholine-receptors
#8
Caleb W Holyoke, Daniel Cordova, Wenming Zhang, James D Barry, Robert M Leighty, Robert F Dietrich, James J Rauh, Thomas F Pahutski, George P Lahm, My-Hanh Thi Tong, Eric A Benner, John L Andreassi, Rejane M Smith, Daniel R Vincent, Laurie A Christianson, Luis A Teixeira, Vineet Singh, Kenneth A Hughes
BACKGROUND: As the world population grows toward 9 billion by 2050 it is projected that food production will need to increase by 60%. A critical part of this growth includes the safe and effective use of insecticides to reduce the estimated 20-49% loss of global crop yields due to pests. Development of new insecticides will help sustain this protection and overcome insecticide resistance. RESULTS: A novel class of mesoionic compounds has been discovered with exceptional insecticidal activity on a range of Hemiptera and Lepidoptera...
November 29, 2016: Pest Management Science
https://www.readbyqxmd.com/read/27895161/the-e-loop-of-the-transmitter-binding-site-is-a-key-determinant-of-the-modulatory-effects-of-physostigmine-on-neuronal-nicotinic-%C3%AE-4%C3%AE-2-receptors
#9
Xiaochun Jin, Megan M McCollum, Allison L Germann, Gustav Akk, Joseph H Steinbach
Physostigmine is a well-known inhibitor of acetylcholinesterase, which can also activate, potentiate and inhibit acetylcholine receptors, including neuronal nicotinic receptors comprising α4 and β2 subunits. We have found that the two stoichiometric forms of this receptor differ in the effects of physostigmine. The form containing 3 copies of α4 and 2 of β2 was potentiated at low concentrations of ACh and physostigmine, while the form containing 2 copies of α4 and 3 of β2 was inhibited. Chimeric constructs of subunits indicated that the presence of inhibition or potentiation depended on the source of the extracellular ligand-binding domain of the subunit...
November 28, 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27890744/gene-expression-of-pro-opiomelanocortin-and-melanocortin-receptors-is-regulated-in-the-hypothalamus-and-mesocorticolimbic-system-following-nicotine-administration
#10
Damla E Tapinc, Rabia Ilgin, Egemen Kaya, Oguz Gozen, Muzeyyen Ugur, Ersin O Koylu, Lutfiye Kanit, Aysegul Keser, Burcu Balkan
Pro-opiomelanocortin (POMC)-derived peptides and their receptors have been shown to play important roles in natural and drug-induced reward and reinforcement. Reward process may involve the regulation of POMC gene expression and the gene expression of POMC-derived peptide receptors. The present study investigated the alterations observed in the transcript levels of POMC, melanocortin 3 (MC3R), melanocortin 4 (MC4R) and mu-opioid receptors (MOR) in the hypothalamus and mesocorticolimbic system during nicotine exposure...
November 24, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27886263/nicotinic-and-opioid-receptor-regulation-of-striatal-dopamine-d2-receptor-mediated-transmission
#11
Aphroditi A Mamaligas, Yuan Cai, Christopher P Ford
In addition to dopamine neuron firing, cholinergic interneurons (ChIs) regulate dopamine release in the striatum via presynaptic nicotinic receptors (nAChRs) on dopamine axon terminals. Synchronous activity of ChIs is necessary to evoke dopamine release through this pathway. The frequency-dependence of disynaptic nicotinic modulation has led to the hypothesis that nAChRs act as a high-pass filter in the dopaminergic microcircuit. Here, we used optogenetics to selectively stimulate either ChIs or dopamine terminals directly in the striatum...
November 25, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27883993/stimulation-of-the-nonneuronal-cholinergic-system-by-highly-diluted-acetylcholine-in-keratinocytes
#12
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/27878656/mille-modis-morimur-we-die-in-a-thousand-ways
#13
Gaspar Banfalvi
Dying cells subjected to apoptotic programs are engulfed by neighboring cells or by professional phagocytes, without inflammation or immunological reactions in the tissue where apoptosis takes place. Apoptotic cells release danger-associated project signals to their neighbours, through different molecular patterns, stimulate antigen production and immune responses. Microenvironmental effects with several functional consequences indicate that cell death is a complex process and may take place in several ways...
November 23, 2016: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/27874086/combined-administration-of-anisodamine-and-neostigmine-rescued-acute-lethal-crush-syndrome-through-%C3%AE-7nachr-dependent-jak2-stat3-signaling
#14
Zhe-Qi Xu, Bo-Zong Shao, Ping Ke, Jian-Guo Liu, Guo-Ku Liu, Xiong-Wen Chen, Ding-Feng Su, Chong Liu
Previously we showed that Ani (anisodamine)/Neo (neostigmine) combination produced anti-shock effect via activating α7 nicotinic acetylcholine receptor (α7nAChR). In this study, we aim to investigate the therapeutic effect and underlying mechanisms of Ani/Neo combination in acute lethal crush syndrome (CS). In rat and rabbit CS models, Ani/Neo combination increased the 24 h survival rates, improved hemodynamics and decreased the levels of creatine kinase, MB isoenzyme of creatine kinase, blood urea nitrogen, creatinine, K(+) in serum...
November 22, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27871840/probing-the-structure-of-the-uncoupled-nicotinic-acetylcholine-receptor
#15
Jiayin Sun, J Frederique Comeau, John E Baenziger
In the absence of activating anionic lipids and cholesterol, the nicotinic acetylcholine receptor (nAChR) from Torpedo adopts an uncoupled conformation that does not usually gate open in response to agonist. The uncoupled conformation binds both agonists and non-competitive channel blockers with a lower affinity than the desensitized state, consistent with both the extracellular agonist-binding and transmembrane channel-gating domains individually adopting resting-state like conformations. To test this hypothesis, we characterized the binding of the agonist, acetylcholine, and two fluorescent channel blockers, ethidium and crystal violet, to resting, desensitized and uncoupled nAChRs in reconstituted membranes...
November 19, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27871728/the-chrna5-a3-b4-gene-cluster-and-smoking-from-discovery-to-therapeutics
#16
REVIEW
Glenda Lassi, Amy E Taylor, Nicholas J Timpson, Paul J Kenny, Robert J Mather, Tim Eisen, Marcus R Munafò
Genome-wide association studies (GWASs) have identified associations between the CHRNA5-CHRNA3-CHRNB4 gene cluster and smoking heaviness and nicotine dependence. Studies in rodents have described the anatomical localisation and function of the nicotinic acetylcholine receptors (nAChRs) formed by the subunits encoded by this gene cluster. Further investigations that complemented these studies highlighted the variability of individuals' smoking behaviours and their ability to adjust nicotine intake. GWASs of smoking-related health outcomes have also identified this signal in the CHRNA5-CHRNA3-CHRNB4 gene cluster...
November 18, 2016: Trends in Neurosciences
https://www.readbyqxmd.com/read/27870937/spinosad-induces-programmed-cell-death-involves-mitochondrial-dysfunction-and-cytochrome-c-release-in-spodoptera-frugiperda-sf9-cells
#17
Mingjun Yang, Bo Wang, Jufang Gao, Yang Zhang, Wenping Xu, Liming Tao
Spinosad, a reduced-risk insecticide, acts on the nicotinic acetylcholine receptors and the gamma-aminobutyric acid receptor in the nervous system of target insects. However, its mechanism of action in non-neural insect cells is unclear. This study aimed to evaluate mitochondrial functional changes associated with spinosad in Spodoptera frugiperda (Sf9) insect cells. Our results indicate that in Sf9 cells, spinosad induces programmed cell death and mitochondrial dysfunction through enhanced reactive oxygen species production, mitochondrial permeability transition pore (mPTP) opening, and mitochondrial membrane potential collapse, eventually leading to cytochrome C release and apoptosis...
November 18, 2016: Chemosphere
https://www.readbyqxmd.com/read/27870426/sex-dependent-effects-of-nicotine-on-the-developing-brain
#18
REVIEW
Sarah J Cross, Kay E Linker, Frances M Leslie
The use of tobacco products represents a major public health concern, especially among women. Epidemiological data have consistently demonstrated that women have less success quitting tobacco use and a higher risk for developing tobacco-related diseases. The deleterious effects of nicotine are not restricted to adulthood, as nicotinic acetylcholine receptors regulate critical aspects of neural development. However, the exact mechanisms underlying the particular sensitivity of women to develop tobacco dependence have not been well elucidated...
January 2, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/27866776/activation-of-%C3%AE-7-nicotinic-acetylcholine-receptors-facilitates-long-term-potentiation-at-the-hippocampal-prefrontal-cortex-synapses-in-vivo
#19
Milan Stoiljkovic, Craig Kelley, Dávid Nagy, Raymond Hurst, Mihály Hajós
Activation of α7 nAChRs has been shown to improve performance in a variety of nonclinical assays of cognitive function. The role of α7 nAChRs in cognitive processes is likely related to their role in modulating synaptic transmission and plasticity that have been reported in cell culture, brain slices, and intact animals. Here we report the effects of the α7 nAChR agonist FRM-17874 on synaptic plasticity within the hippocampal-medial prefrontal cortex pathway. Long-term potentiation (LTP) was generated by tetanic stimulation of CA1/subiculum region in urethane anesthetized male rats...
November 17, 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27865910/multi-target-directed-therapeutic-potential-of-7-methoxytacrine-adamantylamine-heterodimers-in-the-alzheimer-s-disease-treatment
#20
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
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