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https://www.readbyqxmd.com/read/28733581/structural-determinants-at-the-m2-muscarinic-receptor-modulate-the-rgs4-girk-response-to-pilocarpine-by-impairment-of-the-receptor-voltage-sensitivity
#1
I-Shan Chen, Kazuharu Furutani, Yoshihisa Kurachi
Membrane potential controls the response of the M2 muscarinic receptor to its ligands. Membrane hyperpolarization increases response to the full agonist acetylcholine (ACh) while decreasing response to the partial agonist pilocarpine. We previously have demonstrated that the regulator of G-protein signaling (RGS) 4 protein discriminates between the voltage-dependent responses of ACh and pilocarpine; however, the underlying mechanism remains unclear. Here we show that RGS4 is involved in the voltage-dependent behavior of the M2 muscarinic receptor-mediated signaling in response to pilocarpine...
July 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729220/cognitive-enhancement-and-antipsychotic-like-activity-following-repeated-dosing-with-the-selective-m4-pam-vu0467154
#2
Robert W Gould, Michael D Grannan, Barak W Gunter, Jacob Ball, Michael Bubser, Thomas M Bridges, Jurgen Wess, Michael W Wood, Nicholas J Brandon, Mark E Duggan, Colleen M Niswender, Craig W Lindsley, P Jeffrey Conn, Carrie K Jones
Although selective activation of the M1 muscarinic acetylcholine receptor (mAChR) subtype has been shown to improve cognitive function in animal models of neuropsychiatric disorders, recent evidence suggests that enhancing M4 mAChR function can also improve memory performance. Positive allosteric modulators (PAMs) targeting the M4 mAChR subtype have shown therapeutic potential for the treatment of multiple symptoms observed in schizophrenia, including positive and cognitive symptoms when assessed in acute preclinical dosing paradigms...
July 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28729041/pharmacological-preclinical-characterization-of-las190792-a-novel-inhaled-bifunctional-muscarinic-receptor-antagonist-%C3%AE-2-adrenoceptor-agonist-maba-molecule
#3
Mònica Aparici, Carla Carcasona, Israel Ramos, José Luís Montero, José Luís Ortiz, Julio Cortijo, Carlos Puig, Dolors Vilella, Chris Doe, Amadeu Gavaldà, Montserrat Miralpeix
LAS190792 is a novel muscarinic antagonist and β2-adrenoceptor agonist in development for chronic respiratory diseases. This study investigated the pharmacological profile of LAS190792 in comparison to batefenterol, tiotropium, indacaterol and olodaterol. LAS190792 is potent at the human M3 receptor (pIC50: 8.8 in binding assays). It is selective for the β2-adrenoceptor over the β1-and β3-adrenoceptor, and shows a functional potency in a similar range to batefenterol and LABA compounds (pEC50 in spontaneous tone isolated trachea: 9...
July 17, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28728517/using-molecular-dynamics-for-the-refinement-of-atomistic-models-of-gpcrs-by-homology-modeling
#4
Cecylia S Lupala, Bahareh Rasaeifar, Patricia Gomez-Gutierrez, Juan J Perez
Despite GPCRs share a common seven helix bundle, analysis of the diverse crystallographic structures available reveal specific features that might be relevant for ligand design. Despite the number of crystallographic structures of GPCRs is steadily increasing, there are still challenges that hamper the availability of new structures. In the absence of a crystallographic structure, homology modelling remains one of the important techniques for constructing 3D models of proteins. In the present study we investigated the use of molecular dynamics simulations for the refinement of GPCRs models constructed by homology modeling...
July 20, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28726567/possible-mechanisms-involved-in-the-anti-nociceptive-effects-of-hydro-ethanolic-leaf-extract-of-ziziphus-abyssinica
#5
Eric Boakye-Gyasi, Isaac Tabiri Henneh, Wonder Kofi Mensah Abotsi, Elvis Ofori Ameyaw, Eric Woode
CONTEXT: Various parts of Ziziphus abyssinica Hochst ex. A. Rich (Rhamnaceae) have been used in Ghanaian and African traditional medicine as an analgesic. However, there are little scientific data to support the anti-nociceptive effects of the hydro-ethanolic leaf extract of Ziziphus abyssinica (EthE) as well as the possible mechanisms involved in its anti-nociceptive effects. PURPOSE: To predict possible nociceptive pathways involved in the anti-nociceptive effects of EthE...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28724783/intra-and-intersegmental-influences-among-central-pattern-generating-networks-in-the-walking-system-of-the-stick-insect
#6
Charalampos Mantziaris, Till Bockemühl, Philip Holmes, Anke Borgmann, Silvia Daun, Ansgar Bueschges
In order to efficiently move around, animals need to coordinate their limbs. Proper, context-dependent coupling among the neural networks underlying leg movement is necessary for generating intersegmental coordination. In the slow-walking stick insect local sensory information is very important for shaping coordination. However, central coupling mechanisms among segmental central pattern generators (CPGs) may also contribute to this. Here, we analyzed the interactions between contralateral networks that drive the depressor trochanteris muscle of the legs in both isolated and interconnected deafferented thoracic ganglia of the stick insect upon application of pilocarpine, a muscarinic acetylcholine receptor agonist...
July 19, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28722769/promoter-iv-bdnf-deficiency-disturbs-cholinergic-gene-expression-of-chrna5-chrm2-and-chrm5-effects-of-drug-and-environmental-treatments
#7
Kazuko Sakata, Abigail E Overacre
Brain-derived neurotrophic factor (BDNF) promotes maturation of cholinergic neurons. However, how activity-dependent BDNF expression affects specific cholinergic gene expression remains unclear. This study addressed this question by determining mRNA levels of 22 acetylcholine receptor subunits, the choline transporter (CHT), and the choline acetyltransferase (ChAT) in mice deficient in activity-dependent BDNF via promoter IV (KIV) and control wild-type mice. Quantitative RT-PCR revealed significant reductions in nicotinic acetylcholine receptor alpha 5 (CHRNA5) in the frontal cortex and hippocampus and M5 muscarinic acetylcholine receptor (CHRM5) in the hippocampus, but significant increases in M2 muscarinic acetylcholine receptor (CHRM2) in the frontal cortex of KIV mice compared to wild-type mice...
July 19, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28722259/l-ornithine-and-l-lysine-stimulate-gastrointestinal-motility-via-transient-receptor-potential-vanilloid-1
#8
Junya Nakato, Yee Yin Ho, Ryo Omae, Takafumi Mizushige, Kunitoshi Uchida, Makoto Tominaga, Minji Kim, Tsuyoshi Goto, Nobuyuki Takahashi, Teruo Kawada, Saori Akiduki, Ryuhei Kanamoto, Kousaku Ohinata
SCOPE: The gastrointestinal (GI) tract senses and responds to intraluminal nutrients and these interactions often affect GI functions. We found that, among basic amino acids, L-ornithine (Orn) and L-lysine (Lys) stimulated but L-arginine (Arg) suppressed GI motility after oral administration (24 mmol/kg) in mice (Orn and Lys, 14.3 and 26.4% promotion; Arg, 7.7% suppression). We investigated the mechanism of the action of Orn and Lys on GI motility. METHODS AND RESULTS: Orn-induced promotion of small intestinal transit was significantly inhibited (P<0...
July 18, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28721035/intracellular-interactions-of-umeclidinium-and-vilanterol-in-human-airway-smooth-muscle
#9
Nooreen Shaikh, Malcolm Johnson, David A Hall, Kian Fan Chung, John H Riley, Sally Worsley, Pankaj K Bhavsar
BACKGROUND: Intracellular mechanisms of action of umeclidinium (UMEC), a long-acting muscarinic receptor antagonist, and vilanterol (VI), a long-acting β2-adrenoceptor (β2R) agonist, were investigated in target cells: human airway smooth-muscle cells (ASMCs). MATERIALS AND METHODS: ASMCs from tracheas of healthy lung-transplant donors were treated with VI, UMEC, UMEC and VI combined, or control compounds (salmeterol, propranolol, ICI 118.551, or methacholine [MCh])...
2017: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/28720796/eeg-machine-learning-for-accurate-detection-of-cholinergic-intervention-and-alzheimer-s-disease
#10
Sonja Simpraga, Ricardo Alvarez-Jimenez, Huibert D Mansvelder, Joop M A van Gerven, Geert Jan Groeneveld, Simon-Shlomo Poil, Klaus Linkenkaer-Hansen
Monitoring effects of disease or therapeutic intervention on brain function is increasingly important for clinical trials, albeit hampered by inter-individual variability and subtle effects. Here, we apply complementary biomarker algorithms to electroencephalography (EEG) recordings to capture the brain's multi-faceted signature of disease or pharmacological intervention and use machine learning to improve classification performance. Using data from healthy subjects receiving scopolamine we developed an index of the muscarinic acetylcholine receptor antagonist (mAChR) consisting of 14 EEG biomarkers...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28720132/efficacy-and-safety-of-direct-switch-to-indacaterol-glycopyrronium-in-patients-with-moderate-copd-the-crystal-open-label-randomised-trial
#11
Claus F Vogelmeier, Mina Gaga, Maryam Aalamian-Mattheis, Timm Greulich, Jose M Marin, Walter Castellani, Vincent Ninane, Stephen Lane, Xavier Nunez, Francesco Patalano, Andreas Clemens, Konstantinos Kostikas
BACKGROUND: Dual bronchodilation combining a long-acting β2-agonist (LABA) and a long-acting muscarinic antagonist (LAMA) is the preferred choice of treatment recommended by the Global Initiative for Chronic Obstructive Lung Disease (GOLD) 2017 guidelines for the management of patients with moderate-to-severe chronic obstructive pulmonary disease (COPD). The once-daily (q.d.) fixed-dose combination (FDC) of LABA, indacaterol 110 μg and LAMA, glycopyrronium 50 μg (IND/GLY 110/50 μg q...
July 18, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28719697/diagnosis-and-management-of-asthma-in-adults-a-review
#12
Jennifer L McCracken, Sreenivas P Veeranki, Bill T Ameredes, William J Calhoun
Importance: Asthma affects about 7.5% of the adult population. Evidence-based diagnosis, monitoring, and treatment can improve functioning and quality of life in adult patients with asthma. Observations: Asthma is a heterogeneous clinical syndrome primarily affecting the lower respiratory tract, characterized by episodic or persistent symptoms of wheezing, dyspnea, and cough. The diagnosis of asthma requires these symptoms and demonstration of reversible airway obstruction using spirometry...
July 18, 2017: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/28716723/pharmacological-characterization-of-the-interaction-between-umeclidinium-and-vilanterol-in-human-bronchi
#13
Luigino Calzetta, Paola Rogliani, Francesco Facciolo, Erino Rendina, Mario Cazzola, Maria Gabriella Matera
The long-acting β2-agonist (LABA) / long-acting muscarinic antagonist (LAMA) fixed dose combination (FDC) therapy represents the cornerstone for the treatment of chronic obstructive pulmonary disease (COPD). Nevertheless, conflicting clinical findings still exist on the real benefit of the LABA/LAMA FDCs. Therefore, we investigated whether combining the LABA vilanterol with the LAMA umeclidinium may induce synergistic bronchorelaxant effect in isolated airways. The effect of umeclidinium and vilanterol, administered alone, in combination at the ratio of concentrations reproducing the doses delivered by Anoro(®) Ellipta(®) (55:22), or at isoeffective low concentrations, was investigated on the cholinergic contractile tone induced by the parasympathetic activation of human isolated airways...
July 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28714717/acetylcholine-contributes-to-the-integration-of-self-movement-cues-in-head-direction-cells
#14
Ryan M Yoder, Jeremy H M Chan, Jeffrey S Taube
Acetylcholine contributes to accurate performance on some navigational tasks, but details of its contribution to the underlying brain signals are not fully understood. The medial septal area provides widespread cholinergic input to various brain regions, but selective damage to medial septal cholinergic neurons generally has little effect on landmark-based navigation, or the underlying neural representations of location and directional heading in visual environments. In contrast, the loss of medial septal cholinergic neurons disrupts navigation based on path integration, but no studies have tested whether these path integration deficits are associated with disrupted head direction (HD) cell activity...
August 2017: Behavioral Neuroscience
https://www.readbyqxmd.com/read/28714121/acetylcholine-dependent-upregulation-of-task-1-channels-in-thalamic-interneurons-by-a-smooth-muscle-like-signalling-pathway
#15
Michael Leist, Susanne Rinné, Maia Datunashvili, Ania Aissaoui, Hans-Christian Pape, Niels Decher, Sven G Meuth, Thomas Budde
The dorsal part of the lateral geniculate nucleus (dLGN) is the main thalamic site for state-dependent transmission of visual information. Non-retinal inputs from the ascending arousal system and inhibition provided by γ-aminobutyric acid (GABA)ergic local circuit interneurons (INs) control neuronal activity within the dLGN. In particular, acetylcholine (ACh) depolarizes thalamocortical relay (TC) neurons by inhibiting two-pore domain potassium (K2P ) channels. Conversely, ACh also hyperpolarizes INs via an as-yet-unknown mechanism...
July 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28711697/role-of-muscarinic-receptors-in-the-contraction-of-jejunal-smooth-muscle-in-the-horse-an-in-vitro-study
#16
Alessandro Menozzi, Cristina Pozzoli, Enzo Poli, Giada Bontempi, Paolo Serventi, Valentina Meucci, Luigi Intorre, Simone Bertini
Nonselective antimuscarinic drugs are clinically useful in several pathologic conditions of horses, but, blocking all muscarinic receptor (MR) subtypes, may cause several side effects. The availability of selective antimuscarinic drugs could improve therapeutic efficacy and safety. We aimed to enlighten the role of different MR subtypes by evaluating the effects of nonselective, and selective M1, M2 and M3 MR antagonists on the contractions of horse jejunum. Segments of circular muscle of equine jejunum, were put into organ baths, connected to isotonic transducers, and the effects on ACh concentration-response curves, and on electrical field stimulation (EFS)-evoked contractions of intestinal preparations, induced by nonselective or selective MR antagonists, compared to pre-drug level, were studied...
July 11, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28711308/the-impact-of-scopolamine-pretreatment-on-3-iodothyronamine-t1am-effects-on-memory-and-pain-in-mice
#17
Annunziatina Laurino, Ersilia Lucenteforte, Gaetano De Siena, Laura Raimondi
We previously demonstrated that 3-iodothyronamine (T1AM), a by-product of thyroid hormone metabolism, pharmacologically administered to mice acutely stimulated learning and memory acquisition and provided hyperalgesia with a mechanism which remains to be defined. We now aimed to investigate whether the T1AM effect on memory and pain was maintained in mice pre-treated with scopolamine, a non-selective muscarinic antagonist expected to induce amnesia and, possibly, hyperalgesia. Mice were pre-treated with scopolamine and, after 20min, injected intracerebroventricularly (i...
July 19, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28700094/regulation-of-synaptic-acetylcholine-concentrations-by-acetylcholine-transport-in-rat-striatal-cholinergic-transmission
#18
Ikunobu Muramatsu, Junsuke Uwada, Takayoshi Masuoka, Hatsumi Yoshiki, Kiyonao Sada, Kung-Shing Lee, Matomo Nishio, Takaharu Ishibashi, Takanobu Taniguchi
In addition to hydrolysis by acetylcholine esterase (AChE), acetylcholine (ACh) is also directly taken up into brain tissues. In the present study, we examined whether the uptake of ACh is involved in the regulation of synaptic ACh concentrations. Superfusion experiments with rat striatal segments pre-incubated with [(3) H]choline were performed using an ultra-mini superfusion vessel, which was developed to minimize superfusate retention within the vessel. Hemicholinium-3 (HC-3) at concentrations less than 1 μM, selectively inhibited the uptake of [(3) H]choline by the high affinity-choline transporter 1 (CHT1) and had no effect on basal and electrically evoked [(3) H]efflux in superfusion experiments...
July 12, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28698560/all-muscarinic-acetylcholine-receptors-m1-m5-are-expressed-in-murine-brain-microvascular-endothelium
#19
Beatrice Mihaela Radu, Antonio Marco Maria Osculati, Eda Suku, Adela Banciu, Grygoriy Tsenov, Flavia Merigo, Marzia Di Chio, Daniel Dumitru Banciu, Cristina Tognoli, Petr Kacer, Alejandro Giorgetti, Mihai Radu, Giuseppe Bertini, Paolo Francesco Fabene
Clinical and experimental studies indicate that muscarinic acetylcholine receptors are potential pharmacological targets for the treatment of neurological diseases. Although these receptors have been described in human, bovine and rat cerebral microvascular tissue, a subtype functional characterization in mouse brain endothelium is lacking. Here, we show that all muscarinic acetylcholine receptors (M1-M5) are expressed in mouse brain microvascular endothelial cells. The mRNA expression of M2, M3, and M5 correlates with their respective protein abundance, but a mismatch exists for M1 and M4 mRNA versus protein levels...
July 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28695546/knockdown-of-myo-inositol-transporter-smit1-normalizes-cholinergic-and-glutamatergic-function-in-an-immortalized-cell-line-established-from-the-cerebral-cortex-of-a-trisomy-16-fetal-mouse-an-animal-model-of-human-trisomy-21-down-syndrome
#20
Ana María Cárdenas, Paola Fernández-Olivares, Ignacio Díaz-Franulic, Arlek M González-Jamett, Takeshi Shimahara, Juan Segura-Aguilar, Raúl Caviedes, Pablo Caviedes
The Na(+)/myo-inositol cotransporter (SMIT1) is overexpressed in human Down syndrome (DS) and in trisomy 16 fetal mice (Ts16), an animal model of the human condition. SMIT1 overexpression determines increased levels of intracellular myo-inositol, a precursor of phophoinositide synthesis. SMIT1 is overexpressed in CTb cells, an immortalized cell line established from the cerebral cortex of a Ts16 mouse fetus. CTb cells exhibit impaired cytosolic Ca(2+) signals in response to glutamatergic and cholinergic stimuli (increased amplitude and delayed time-dependent kinetics in the decay post-stimulation), compared to our CNh cell line, derived from the cerebral cortex of a euploid animal...
July 10, 2017: Neurotoxicity Research
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