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Muscarinic receptors

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https://www.readbyqxmd.com/read/28807620/muscarinic-acetylcholine-receptor-but-not-nicotinic-acetylcholine-receptor-plays-a-role-in-morphine-induced-behavioral-sensitization-in-rats
#1
Jinling Sun, Lin Tian, Ruisi Cui, Heng Ruan, Xinwang Li
Background and Aim The cholinergic system can affect drug reward. The present study aimed to examine the roles of muscarinic acetylcholine receptor (mAChR) and nicotinic acetylcholine receptor (nAChR) in morphine-induced behavioral sensitization. METHODS: To analyze the roles of mAChR and nAChR in behavioral sensitization induced by morphine (5mg/kg), seven experiments were designed. Experiments 1 and 2 examined the effects of 3, 1, and 0.3 mg/kg scopolamine and 0.2, 0.1, and 0.05mg/kg scopolamine, respectively, on the locomotor activity when administered alone...
August 11, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28807148/acetylcholine-induces-intracellular-ca-2-oscillations-and-nitric-oxide-release-in-mouse-brain-endothelial-cells
#2
Estella Zuccolo, Dmitry Lim, Dlzar Ali Kheder, Angelica Perna, Paolo Catarsi, Laura Botta, Vittorio Rosti, Laura Riboni, Giulio Sancini, Franco Tanzi, Egidio D'Angelo, Germano Guerra, Francesco Moccia
Basal forebrain neurons increase cortical blood flow by releasing acetylcholine (Ach), which stimulates endothelial cells (ECs) to produce the vasodilating gasotransmitter, nitric oxide (NO). Surprisingly, the mechanism whereby Ach induces NO synthesis in brain microvascular ECs is unknown. An increase in intracellular Ca(2+) concentration recruits a multitude of endothelial Ca(2+)-dependent pathways, such as Ca(2+)/calmodulin endothelial NO synthase (eNOS). The present investigation sought to investigate the role of intracellular Ca(2+) signaling in Ach-induced NO production in bEND5 cells, an established model of mouse brain microvascular ECs, by conventional imaging of cells loaded with the Ca(2+)-sensitive dye, Fura-2/AM, and the NO-sensitive fluorophore, DAF-DM diacetate...
September 2017: Cell Calcium
https://www.readbyqxmd.com/read/28796813/a-novel-organotypic-3d-sweat-gland-model-with-physiological-functionality
#3
Patricia Klaka, Sabine Grüdl, Bernhard Banowski, Melanie Giesen, Andrea Sättler, Peter Proksch, Thomas Welss, Thomas Förster
Dysregulated human eccrine sweat glands can negatively impact the quality-of-life of people suffering from disorders like hyperhidrosis. Inability of sweating can even result in serious health effects in humans affected by anhidrosis. The underlying mechanisms must be elucidated and a reliable in vitro test system for drug screening must be developed. Here we describe a novel organotypic three-dimensional (3D) sweat gland model made of primary human eccrine sweat gland cells. Initial experiments revealed that eccrine sweat gland cells in a two-dimensional (2D) culture lose typical physiological markers...
2017: PloS One
https://www.readbyqxmd.com/read/28793049/possible-mechanisms-involved-in-the-vasorelaxant-effect-produced-by-clobenzorex-in-aortic-segments-of-rats
#4
J Lozano-Cuenca, A González-Hernández, O A López-Canales, J R Villagrana-Zesati, J D Rodríguez-Choreão, R Morín-Zaragoza, E F Castillo-Henkel, J S López-Canales
Clobenzorex is a metabolic precursor of amphetamine indicated for the treatment of obesity. Amphetamines have been involved with cardiovascular side effects such as hypertension and pulmonary arterial hypertension. The aim of the present study was to investigate whether the direct application of 10-9-10-5 M clobenzorex on isolated phenylephrine-precontracted rat aortic rings produces vascular effects, and if so, what mechanisms may be involved. Clobenzorex produced an immediate concentration-dependent vasorelaxant effect at the higher concentrations (10-7...
August 7, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28782490/unmet-needs-in-schizophrenia
#5
Maurizio Pompili, Herbert Y Meltzer
The objectives of this article are to describe current trends in the treatment of schizophrenia and the most interesting new approaches to optimizing outcome and fostering the development of new schizophrenia treatments. RESULTS: Increasing utilization of diverse types of atypical antipsychotic drugs (AAPDs), e.g. clozapine-type serotonin (5-HT)2A and weak dopamine (DA) D2 antagonist, amisulpride, a D2/D3/5-HT7 antagonist, and cariprazine, a D3 partial agonist with additional neurotransmitter targets, is occurring as their advantages in efficacy, especially for cognitive impairment and mood symptoms, and side effects is becoming appreciated...
August 3, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28781727/cross-state-dependent-learning-interaction-between-scopolamine-and-morphine-in-mice-the-role-of-dorsal-hippocampus
#6
Morteza Maleki, Majid Hassanpour-Ezatti, Majid Navaeian
INTRODUCTION: The current study aimed at investigating the existence of the cross state-dependent learning between morphine and scopolamine (SCO) in mice by passive avoidance method, pointing to the role of CA1 area. METHODS: The effects of pre-training SCO (0.75, 1.5, and 3 μg, Intra-CA1), or morphine (1, 3, and 6 mg/kg, intraperitoneal (i.p.) was evaluated on the retrieval of passive avoidance learning using step-down task in mice (n=10). Then, the effect of pretest administration of morphine (1...
May 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28777299/ultrafast-and-slow-cholinergic-transmission-different-involvement-of-acetylcholinesterase-molecular-forms
#7
REVIEW
Yves Dunant, Victor Gisiger
Acetylcholine (ACh), an ubiquitous mediator substance broadly expressed in nature, acts as neurotransmitter in cholinergic synapses, generating specific communications with different time-courses. (1) Ultrafast transmission. Vertebrate neuromuscular junctions (NMJs) and nerve-electroplaque junctions (NEJs) are the fastest cholinergic synapses; able to transmit brief impulses (1-4 ms) at high frequencies. The collagen-tailed A12 acetylcholinesterase is concentrated in the synaptic cleft of NMJs and NEJs, were it curtails the postsynaptic response by ultrafast ACh hydrolysis...
August 4, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28776261/roles-of-na-ca-2-and-k-channels-in-the-generation-of-repetitive-firing-and-rhythmic-bursting-in-adrenal-chromaffin-cells
#8
REVIEW
Christopher J Lingle, Pedro L Martinez-Espinosa, Laura Guarina, Emilio Carbone
Adrenal chromaffin cells (CCs) are the main source of circulating catecholamines (CAs) that regulate the body response to stress. Release of CAs is controlled neurogenically by the activity of preganglionic sympathetic neurons through trains of action potentials (APs). APs in CCs are generated by robust depolarization following the activation of nicotinic and muscarinic receptors that are highly expressed in CCs. Bovine, rat, mouse, and human CCs also express a composite array of Na(+), K(+), and Ca(2+) channels that regulate the resting potential, shape the APs, and set the frequency of AP trains...
August 3, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28775269/hipp-neurons-in-the-dentate-gyrus-mediate-the-cholinergic-modulation-of-background-context-memory-salience
#9
Syed Ahsan Raza, Anne Albrecht, Gürsel Çalışkan, Bettina Müller, Yunus Emre Demiray, Susann Ludewig, Susanne Meis, Nicolai Faber, Roland Hartig, Burkhart Schraven, Volkmar Lessmann, Herbert Schwegler, Oliver Stork
Cholinergic neuromodulation in the hippocampus controls the salience of background context memory acquired in the presence of elemental stimuli predicting an aversive reinforcement. With pharmacogenetic inhibition we here demonstrate that hilar perforant path-associated (HIPP) cells of the dentate gyrus mediate the devaluation of background context memory during Pavlovian fear conditioning. The salience adjustment is sensitive to reduction of hilar neuropeptide Y (NPY) expression via dominant negative CREB expression in HIPP cells and to acute blockage of NPY-Y1 receptors in the dentate gyrus during conditioning...
August 4, 2017: Nature Communications
https://www.readbyqxmd.com/read/28772121/cell-type-specific-translation-profiling-reveals-a-novel-strategy-for-treating-fragile-x-syndrome
#10
Sophie R Thomson, Sang S Seo, Stephanie A Barnes, Susana R Louros, Melania Muscas, Owen Dando, Caoimhe Kirby, David J A Wyllie, Giles E Hardingham, Peter C Kind, Emily K Osterweil
Excessive mRNA translation downstream of group I metabotropic glutamate receptors (mGlu1/5) is a core pathophysiology of fragile X syndrome (FX); however, the differentially translating mRNAs that contribute to altered neural function are not known. We used translating ribosome affinity purification (TRAP) and RNA-seq to identify mistranslating mRNAs in CA1 pyramidal neurons of the FX mouse model (Fmr1(-/y)) hippocampus, which exhibit exaggerated mGlu1/5-induced long-term synaptic depression (LTD). In these neurons, we find that the Chrm4 transcript encoding muscarinic acetylcholine receptor 4 (M4) is excessively translated, and synthesis of M4 downstream of mGlu5 activation is mimicked and occluded...
August 2, 2017: Neuron
https://www.readbyqxmd.com/read/28767678/pharmacoperone-rescue-of-vasopressin-2-receptor-mutants-reveals-unexpected-constitutive-activity-and-coupling-bias
#11
Jo Ann Janovick, Timothy P Spicer, Thomas D Bannister, Louis Scampavia, P Michael Conn
Pharmacoperones are small molecules that diffuse into cells and rescue misfolded, mistrafficked protein mutants, restoring their function. These substances act with high target specificity, serving as templates to fold (or refold) receptors, enzymes, ion channels or other proteins and enable them to pass the scrutiny of the cellular quality control system ("rescue"). In the present study we demonstrate that a rescued mutant (L83Q) of the vasopressin type 2 receptor (V2R), shows a strong bias for Gs coupling unlike the WT V2 receptor, which couples to both Gs and Gq/11...
2017: PloS One
https://www.readbyqxmd.com/read/28766156/a-primer-on-nerve-agents-what-the-emergency-responder-anesthesiologist-and-intensivist-needs-to-know
#12
Keith Candiotti
PURPOSE: The purpose of this review article is to familiarize first responders, anesthesiologists, and intensivists with the medical management of patients exposed to nerve agents. SOURCE: This review is based on the current medical literature available to the general medical community. PRINCIPAL FINDINGS: Nerve agents are some of the deadliest substances known to humanity. Though they kill primarily via muscle paralysis, which leads to respiratory arrest, these agents affect virtually every organ system in the body...
August 1, 2017: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
https://www.readbyqxmd.com/read/28762161/muscarinic-receptors-in-adrenal-chromaffin-cells-physiological-role-and-regulation-of-ion-channels
#13
REVIEW
Masumi Inoue, Hidetada Matsuoka, Keita Harada, Lung-Sen Kao
Adrenal medullary chromaffin cells in mammals are innervated by sympathetic preganglionic nerve fibers, as are sympathetic ganglion neurons. Acetylcholine in the ganglion neurons is well established as mediating fast and slow excitatory postsynaptic potentials through nicotinic and muscarinic acetylcholine receptors (AChRs), respectively. The role of muscarinic AChRs during neuronal transmission in chromaffin cells varies among different mammals. Furthermore, the ion channel mechanisms associated with the muscarinic AChR-mediated increase in excitability of chromaffin cells are complicated and different from the excitation of ganglion neurons, which has been ascribed to the inhibition of M-type K(+) channels...
July 31, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28758583/new-trends-in-the-treatment-of-schizophrenia
#14
Herbert Y Meltzer
The objectives of this article are to describe current trends in the treatment of schizophrenia and the most interesting new approaches to optimizing outcome and fostering the development of new schizophrenia treatments. RESULTS: Increasing utilization of diverse types of atypical antipsychotic drugs (AAPDs), e.g. clozapine-type serotonin (5-HT)2A and weak dopamine (DA) D2 antagonist, amisulpride, a D2/D3/5-HT7 antagonist, and cariprazine, a D3 partial agonist with additional neurotransmitter targets, is occurring as their advantages in efficacy, especially for cognitive impairment and mood symptoms, and side effects is becoming appreciated...
July 28, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28754132/interactions-between-glycopyrronium-and-indacaterol-on-cholinergic-neurotransmission-and-contractile-response-in-bovine-trachealis
#15
Michele Baroffio, Giovanni Barisione, Vito Brusasco
BACKGROUND: Muscarinic-receptor antagonists and β-adrenoceptor agonists are used, alone or in combination, as first-line treatment for chronic obstructive pulmonary disease. Both drugs decrease airway smooth muscle tone by post-junctional mechanisms but they may have opposing effects on pre-junctional acetylcholine (ACh)-release. METHODS: We studied the effects of the muscarinic-receptor antagonist glycopyrronium (GLY), the β-adrenoceptor agonist indacaterol (IND) and their combination on electrically-induced ACh-release and contractile response in isolated bovine trachealis...
July 28, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28752576/influence-of-prostanoids-in-the-diuretic-and-natriuretic-effects-of-extracts-and-kaempferitrin-from-bauhinia-forficata-link-leaves-in-rats
#16
Priscila de Souza, Luisa Mota da Silva, Thaise Boeing, Lincon Bordignon Somensi, Camile Cecconi Cechinel-Zanchett, Adriana Campos, Clarissa de Medeiros Amorim Krueger, Jairo Kenupp Bastos, Valdir Cechinel-Filho, Sérgio Faloni de Andrade
Although Bauhinia forficata Link is popularly used in Brazil to induce diuresis, no scientific investigation has focused on demonstrating its efficacy in preclinical trials. For that, normotensive male Wistar and spontaneously hypertensive rats were used to test the effect of extracts and kaempferitrin obtained from Bauhinia forficata leaves in the experimental model of diuresis. Cumulative urine volume, Na(+) and K(+) excretion, calcium, creatinine, prostaglandin E2 , pH, density, and conductivity were measured at the end of the experiment (after 8 or 24 h)...
July 28, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28751069/activity-dependent-brain-derived-neurotrophic-factor-release-is-required-for-the-rapid-antidepressant-actions-of-scopolamine
#17
Sriparna Ghosal, Eunyoung Bang, Wenzhu Yue, Brendan D Hare, Ashley E Lepack, Matthew J Girgenti, Ronald S Duman
BACKGROUND: Brain-derived neurotrophic factor (BDNF) plays a key role in the pathophysiology and treatment of depression. Recent clinical studies demonstrate that scopolamine, a nonselective muscarinic acetylcholine receptor antagonist, produces rapid antidepressant effects in patients with depression. Rodent studies demonstrate that scopolamine increases glutamate transmission and synaptogenesis in the medial prefrontal cortex (mPFC). Here we tested the hypothesis that activity-dependent BDNF release within the mPFC is necessary for the antidepressant actions of scopolamine...
June 23, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28750255/effect-of-anti-muscarinic-autoantibodies-on-leukocyte-function-in-sj%C3%A3-gren-s-syndrome
#18
Eun Namkoong, Sang-Woo Lee, Nahyun Kim, Youngnim Choi, Kyungpyo Park
Patients with primary Sjögren's syndrome, a systemic autoimmune disease, have been shown to have serum autoantibodies that react with the muscarinic acetylcholine type 3 receptor (M3R).Primary Sjögren's syndrome is a systemic autoimmune disease. Patients with primary Sjögren's syndrome have been shown to have serum autoantibodies that react with the muscarinic acetylcholine type 3 receptor (M3R). Leukopenia has been reported to be significantly more common in primary Sjögren's syndrome patients who have anti-M3R-autoantibodies in their sera...
July 24, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28744897/furosemide-suppresses-ileal-and-colonic-contractility-via-interactions-with-gaba-a-receptor-in-mice
#19
Kannaree Kaewsaro, Suphap Nuanplub, Sara Bumrungsri, Pissared Khuituan
The loop diuretic furosemide has an action to inhibit Na(+) -K(+) -2Cl(-) co-transporter at the thick ascending limb of Henle's loop resulting in diuresis. Furosemide also has the non-diuretic effects by binding to GABA-A receptor which may involve the gastrointestinal tract. The aim of this study was to investigate the effects of furosemide on smooth muscle contractions in mice ileum and proximal colon. Each intestinal segment suspended in an organ bath was connected to a force transducer. Signal output of mechanical activity was amplified and recorded for analysis using PowerLab(®) System...
July 26, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28744880/chemical-composition-and-diuretic-natriuretic-and-kaliuretic-effects-of-extracts-of-mimosa-bimucronata-dc-kuntze-leaves-and-its-majority-constituent-methyl-gallate-in-rats
#20
Fabile Schlickmann, Priscila de Souza, Thaise Boeing, Luisa N B Mariano, Viviane M B Steimbach, Clarissa de M A Krueger, Luísa M da Silva, Sérgio F de Andrade, Valdir Cechinel-Filho
OBJECTIVES: Some species of the genus Mimosa showed promising results in previous investigations, which include diuretic effect; however, no chemical analyses or animal model has been conducted so far to evaluate the biological properties of M. bimucronata. METHODS: Male Wistar rats received the oral treatment with vehicle; hydrochlorothiazide; methanolic extract from M. bimucronata (MEMB), dichloromethane (DCM) and ethyl acetate (EA) fractions or methyl gallate (MG)...
July 26, 2017: Journal of Pharmacy and Pharmacology
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