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Muscarinic receptors

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https://www.readbyqxmd.com/read/29353067/antinociception-of-the-spirocyclopiperazinium-salt-compound-lxm-15-via-activating-%C3%AE-7-nachr-and-m4-machr-and-inhibiting-camkii%C3%AE-camp-creb-cgrp-signalling-pathway-in-mice
#1
Hua Yang, Qi Sun, Yingying Liang, Yimin Jiang, Runtao Li, Jia Ye
The aim of this study was to investigate the analgesic effect of the spirocyclopiperazinium salt compound LXM-15 by intragastric administration in thermal and chemical pain models and further to elucidate the possible molecular mechanisms. The results showed that LXM-15 exerted significant antinociception in hot-plate test, formalin test and acetic acid writhing test. Western blot analysis showed that LXM-15 significantly reduced the upregulation of phosphorylation of calcium/calmodulin -dependent protein kinaseⅡα (CaMKIIα) and cAMP response element-binding protein (CREB), and further decreased the elevation of calcitonin gene related peptide (CGRP) in the dorsal root ganglion (DRG) and spinal cord in mice...
January 15, 2018: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/29352184/expression-and-relevance-of-the-g-protein-gated-k-channel-in-the-mouse-ventricle
#2
Allison Anderson, Kanchan Kulkarni, Ezequiel Marron Fernandez de Velasco, Nicholas Carlblom, Zhilian Xia, Atsushi Nakano, Kirill A Martemyanov, Elena G Tolkacheva, Kevin Wickman
The atrial G protein-gated inwardly rectifying K+ (GIRK) channel is a critical mediator of parasympathetic influence on cardiac physiology. Here, we probed the details and relevance of the GIRK channel in mouse ventricle. mRNAs for the atrial GIRK channel subunits (GIRK1, GIRK4), M2 muscarinic receptor (M2R), and RGS6, a negative regulator of atrial GIRK-dependent signaling, were detected in mouse ventricle at relatively low levels. The cholinergic agonist carbachol (CCh) activated small GIRK currents in adult wild-type ventricular myocytes that exhibited relatively slow kinetics and low CCh sensitivity; these currents were absent in ventricular myocytes from Girk1-/- or Girk4-/- mice...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29348527/the-human-muscarinic-acetylcholine-receptor-antagonist-dicyclomine-targets-signal-transduction-genes-and-inhibits-the-virulence-factors-in-the-human-pathogen-candida-albicans
#3
Awad Ali, Ashwini Jadhav, Priyanka Jangid, Rajendra Patil, Amruta Shelar, Sankunny Mohan Karuppayil
Dicyclomine is a human muscarinic acetylcholine receptor antagonist used for the treatment of abdominal cramps. We are reporting here that dicyclomine can inhibit the in vitro growth and virulence factors of the human pathogen Candida albicans very effectively. Dicyclomine inhibited adhesion, early biofilm, mature biofilm, and planktonic growth. Yeast to hyphal form transition of C. albicans in various inducer media such as serum, proline, glucose, and N-acetylglucosamine was inhibited. Dicyclomine also could kill C...
January 18, 2018: Journal of Antibiotics
https://www.readbyqxmd.com/read/29335357/nonlinear-relationship-between-spike-dependent-calcium-influx-and-trpc-channel-activation-enables-robust-persistent-spiking-in-neurons-of-the-anterior-cingulate-cortex
#4
Stéphanie Ratté, Sergei Karnup, Steven A Prescott
Persistent spiking - the continuation of spiking after a stimulus ends - is thought to support working memory. Muscarinic receptor activation enables persistent spiking among synaptically isolated pyramidal neurons in anterior cingulate cortex (ACC) but a detailed characterization of that spiking is lacking and the underlying mechanisms remain unclear. Here we show that the rate of persistent spiking in ACC neurons is insensitive to the intensity and number of triggers but can be modulated by injected current, and that persistent spiking can resume after several seconds of hyperpolarization-imposed quiescence...
January 15, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29333036/autonomic-receptors-and-nitric-oxide-involvements-in-mediating-vasorelaxation-effect-induced-by-syzygium-polyanthum-leaves-extract
#5
Azlini Ismail, Wan Amir Nizam Wan Ahmad
Context: Syzygium polyanthum (Wight) Walp leaves are traditionally used by Malays for treating hypertension. Our previous study showed that aqueous extract of S. polyanthum (AESP) and methanolic extract of S. polyanthum (MESP) extracts of S. polyanthum leaves significantly reduced blood pressure of normotensive Wistar-Kyoto (WKY) and spontaneously hypertensive rats (SHR). Aims: This study aimed to investigate their vasorelaxation potential and the possible involvement of autonomic receptors and nitric oxide in mediating their effect...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29331508/compartmentalized-crosstalk-of-cftr-and-tmem16a-ano1-through-epac1-and-adcy1
#6
Joana Lérias, Madalena Pinto, Roberta Benedetto, Rainer Schreiber, Margarida Amaral, Massimo Aureli, Karl Kunzelmann
Airway epithelial cells express both Ca2+ activated TMEM16A/ANO1 and cAMP activated CFTR anion channels. Previous work suggested a significant crosstalk of intracellular Ca2+ and cAMP signaling pathways, leading to activation of both chloride channels. We demonstrate that in airway epithelial cells, stimulation of purinergic or muscarinic G-protein coupled receptors (GPCRs) activates TMEM16A and CFTR. Additional expression of Gq/11 and phospholipase C coupled GPCRs strongly enhanced the crosstalk between Ca2+- and cAMP-dependent signaling...
January 10, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29329111/severe-peri-ictal-respiratory-dysfunction-is-common-in-dravet-syndrome
#7
YuJaung Kim, Eduardo Bravo, Caitlin K Thirnbeck, Lori A Smith-Mellecker, Se Hee Kim, Brian K Gehlbach, Linda C Laux, Douglas R Nordli Jr, George B Richerson
Dravet syndrome (DS) is a severe childhood-onset epilepsy commonly due to mutations of the sodium channel gene SCN1A. DS patients have a high risk of sudden unexplained death in epilepsy (SUDEP), believed to be due to cardiac mechanisms. Here we show that DS patients have peri-ictal respiratory dysfunction. One patient who had severe and prolonged postictal hypoventilation later died of SUDEP. Mice with an Scn1aR1407X/+ loss of function mutation died after spontaneous and heat-induced seizures due to central apnea followed by progressive bradycardia...
January 11, 2018: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29323700/heat-shock-protein-hsp-regulation-by-muscarinic-acetylcholine-receptor-machr-activation-in-the-rat-hippocampus
#8
Frinchi Monica, Scaduto Pietro, Cappello Francesco, Belluardo Natale, Mudò Giuseppa
The cholinergic system plays a crucial role in modulating in the central nervous system physiological responses such as neurogenesis, neuronal differentiation, synaptic plasticity and neuroprotection. In a recent study, we showed that Oxotremorine-M, a non-selective muscarinic acetylcholine receptor agonist, is able to transactivate the fibroblast growth factor receptor and to produce a significant increase in the hippocampal primary neurite outgrowth. In the present study we aimed to explore in the rat hippocampus the possible effect of acute or chronic treatment with Oxotremorine-M on some heat shock proteins (Hsp60, Hsp70, Hsp90) and on activation of related transcription factor heat shock factor 1 (HSF1)...
January 11, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29321959/daily-voluntary-exercise-enhances-pilocarpine-induced-saliva-secretion-and-aquaporin-1-expression-in-rat-submandibular-glands
#9
Kentaro Matsuzaki, Naotoshi Sugimoto, Masanori Katakura, Eri Sumiyoshi, Toshiko Hara, Michio Hashimoto, Osamu Shido
Saliva-a water-based fluid containing electrolytes, immunoglobulins, and enzymes-has many functions, including the protection and hydration of mucosal structures within the oral cavity and the initiation of digestion. Aquaporins (AQPs) are proteins that act as water channels through membranes. We have previously reported upregulation of the expression levels of AQP 1 and 5 in the submandibular glands (SMGs) in heat-acclimated rats. In this study, we investigated pilocarpine-induced saliva secretion and AQP expression in rats after voluntary exercise...
January 2018: FEBS Open Bio
https://www.readbyqxmd.com/read/29319226/discovery-of-novel-muscarinic-receptor-modulators-by-integrating-natural-product-framework-with-bioactive-molecule
#10
Rajesh Varkhedkar, Shalini Dogra, Divya Tiwari, Yusuf Hussain, Prem Narayan Yadav, Ganesh Pandey
Muscarinic acetylcholine receptors (mAChRs) are important therapeutic targets for several diseases of central nervous system and periphery. However, lack of subtype selective ligands of these receptors is a major challenge. A novel approach of integrating natural product framework with bioactive molecule (iNPBM) by utilizing the Gephyrotoxin and isoindoline framework, is demonstrated for discovery of new and selective mAChR modulators. We established a scalable and versatile synthetic scheme to enable synthesis of various analogues that provided the first SAR study of this class of compounds...
January 10, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29317054/promising-horizon-to-alleviate-alzeheimer-s-disease-pathological-hallmarks-via-inhibiting-mtor-signaling-pathway-a-new-application-for-a-commonplace-analgesic
#11
Leila Pourtalebi Jahromi, Zahra Sasanipour, Amir Azadi
Alzheimer's disease (AD) is a very prevalent and burdensome disease of elderlies but albeit extensive studies, mechanisms underlying its pathology and consequently its definite treatment is ambiguous. Intra and extra-cellular aggregation of abnormal proteins and impaired autophagy machinery, two closely related events taking place in AD brains proposed to be directly controlled by mTOR signaling pathway. On the other hand, tramadol that is a very well tolerated opioid analgesic has been revealed to inhibit mTOR upstream controllers through interaction with specific types of muscarinic, serotonergic, nicotinic and NMDA receptors, although it seems to induce the opposite effect via µ-opioid receptor...
January 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29311510/discovery-and-development-of-muscarinic-acetylcholine-m4-activators-as-promising-therapeutic-agents-for-cns-diseases
#12
Kentaro Takai, Takeshi Enomoto
Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4 mAChRs-preferring agonist. Both orthosteric agonists and positive allosteric modulators of M4 mAChR have been reported as promising ligands that not only have antipsychotic effects, but can also improve cognitive impairment and motor dysfunction...
2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29311142/regulation-of-lateral-hypothalamic-orexin-activity-by-local-gabaergic-neurons
#13
Loris L Ferrari, Daniel Park, Lin Zhu, Matthew R Palmer, Rebecca Y Broadhurst, Elda Arrigoni
Orexin (also known as hypocretin) neurons are considered a key component of the ascending arousal system. They are active during wakefulness, at which time they drive and maintain arousal, and are silent during sleep. Their activity is controlled by long-range inputs from many sources, as well as by more short-range inputs, including from presumptive GABAergic neurons in the lateral hypothalamus/perifornical region (LH/PF). To characterize local GABAergic input to orexin neurons we employed channelrhodopsin-2 (ChR2)-assisted-circuit-mapping in brain slices...
January 8, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29307007/neurophysiology-and-neurochemistry-of-corticobasal-syndrome
#14
REVIEW
Aditya A Murgai, Mandar S Jog
Corticobasal syndrome is a rare neurodegenerative disorder, which presents with a progressive, asymmetrical, akinetic rigid syndrome and early cortical signs. However, clinical, pathological, and electrophysiological heterogeneity makes the understanding of this syndrome challenging. Corticobasal syndrome can have various pathological substrates including corticobasal degeneration, Alzheimer's disease, Fronto-temporal degeneration with TDP inclusions, Creutzfeldt-Jakob disease, and progressive supranuclear palsy (PSP)...
January 6, 2018: Journal of Neurology
https://www.readbyqxmd.com/read/29305920/nicotinic-acetylcholine-receptor-nachr-mediated-dopamine-release-in-larval-drosophila-melanogaster
#15
Poojan Pyakurel, Mimi Shin, B Jill Venton
Acetylcholine is an excitatory neurotransmitter in the central nervous system of insects and the nicotinic acetylcholine receptor (nAChR) is a target for neonicotinoid insecticides. Functional insect nAChRs are difficult to express in host cells, and hence difficult to study. In mammals, acetylcholine and nicotine evoke dopamine release, but the extent to which this mechanism is conserved in insects is unknown. In intact larval ventral nerve cords (VNCs), we studied dopamine evoked by acetylcholine, nicotine, or neonicotinoids...
January 3, 2018: Neurochemistry International
https://www.readbyqxmd.com/read/29305262/point-mutation-of-a-conserved-aspartate-d69-in-the-muscarinic-m2-receptor-does-not-modify-voltage-sensitive-agonist-potency
#16
Richard Ågren, Kristoffer Sahlholm, Johanna Nilsson, Peter Århem
The muscarinic M2 receptor (M2R) has been shown to display voltage-sensitive agonist binding, based on G protein-activated inward rectifier potassium channel (GIRK) opening and radioligand binding at different membrane voltages. A conserved aspartate in transmembrane segment (TM) II of M2R, D69, has been proposed as the voltage sensor. While a recent paper instead presented evidence of tyrosines in TMs III, VI, and VII acting as voltage sensors, these authors were not able to record GIRK channel activation by a D69N mutant M2R...
January 2, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29302720/anti-inflammatory-effect-and-mechanism-of-the-spirocyclopiperazinium-salt-compound-lxm-15-in-rats-and-mice
#17
Xiaoli Gao, Qi Sun, Weiwei Zhang, Yimin Jiang, Runtao Li, Jia Ye
OBJECTIVE: This study aimed to investigate the anti-inflammatory effects of a novel spirocyclopiperazinium salt compound LXM-15, and explore the underlying mechanisms. METHODS: Xylene-induced mouse ear oedema and carrageenan-induced rat paw oedema tests were used to evaluate the anti-inflammatory effects of LXM-15. The protein levels of TNF-α, IL-6, phosphorylation of Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3) were detected by ELISA or Western blot analysis...
January 4, 2018: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/29302615/homeostatic-changes-in-gaba-and-acetylcholine-muscarinic-receptors-on-gabaergic-neurons-in-the-mesencephalic-reticular-formation-following-sleep-deprivation
#18
Hanieh Toossi, Esther Del Cid-Pellitero, Barbara E Jones
We have examined whether GABAergic neurons in the mesencephalic reticular formation (RFMes), which are believed to inhibit the neurons in the pons that generate paradoxical sleep (PS or REMS), are submitted to homeostatic regulation under conditions of sleep deprivation (SD) by enforced waking during the day in mice. Using immunofluorescence, we investigated first, by staining for c-Fos, whether GABAergic RFMes neurons are active during SD and then, by staining for receptors, whether their activity is associated with homeostatic changes in GABAA or acetylcholine muscarinic type 2 (AChM2) receptors (Rs), which evoke inhibition...
November 2017: ENeuro
https://www.readbyqxmd.com/read/29291374/af710b-an-m1-sigma-1-receptor-agonist-with-long-lasting-disease-modifying-properties-in-a-transgenic-rat-model-of-alzheimer-s-disease
#19
Hélène Hall, M Florencia Iulita, Palma Gubert, Lisi Flores Aguilar, Adriana Ducatenzeiler, Abraham Fisher, A Claudio Cuello
INTRODUCTION: AF710B (aka ANAVEX 3-71) is a novel selective allosteric M1 muscarinic and sigma-1 receptor agonist. In 3×Tg-AD mice, AF710B attenuates cognitive deficits and decreases Alzheimer-like hallmarks. We now report on the long-lasting disease-modifying properties of AF710B in McGill-R-Thy1-APP transgenic (Tg) rats. METHODS: Chronic treatment with AF710B (10 μg/kg) was initiated in postplaque 13-month-old Tg rats. Drug or vehicle was administered orally daily for 4...
December 29, 2017: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
https://www.readbyqxmd.com/read/29290549/cholinergic-sensorimotor-integration-regulates-olfactory-steering
#20
He Liu, Wenxing Yang, Taihong Wu, Fengyun Duan, Edward Soucy, Xin Jin, Yun Zhang
Sensorimotor integration regulates goal-directed movements. We study the signaling mechanisms underlying sensorimotor integration in C. elegans during olfactory steering, when the sinusoidal movements of the worm generate an in-phase oscillation in the concentration of the sampled odorant. We show that cholinergic neurotransmission encodes the oscillatory sensory response and the motor state of head undulations by acting through an acetylcholine-gated channel and a muscarinic acetylcholine receptor, respectively...
December 21, 2017: Neuron
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