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Muscarinic receptors

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https://www.readbyqxmd.com/read/28632409/l-satropane-prevents-retinal-neuron-damage-by-attenuating-cell-apoptosis-and-a%C3%AE-production-via-activation-of-m1-muscarinic-acetylcholine-receptor
#1
Ping Yu, Wei Zhou, Lu Liu, Ya-Bin Tang, Yun Song, Juan-Juan Lu, Li-Na Hou, Hong-Zhuan Chen, Yong-Yao Cui
Muscarinic acetylcholine receptor (mAChR) agonists have been used to treat glaucoma due to their intraocular pressure-lowering effects. Recently, it has been reported that retinal mAChRs activation can also stimulate neuroprotective pathways. PURPOSE: In our study, we evaluated the potential neuroprotective effect of L-satropane, a novel mAChR agonist, on retinal neuronal injury induced by cobalt chloride (CoCl2) and ischemia/reperfusion (I/R). METHODS: CoCl2-induced hypoxia injury in cultured cell models and I/R-induced retinal neuronal damage in rats in vivo were used to evaluate the abilities of L-satropane...
June 20, 2017: Current Eye Research
https://www.readbyqxmd.com/read/28629847/evidence-for-m2-muscarinic-receptor-modulation-of-axon-terminals-and-dendrites-in-the-rodent-basolateral-amygdala-an-ultrastructural-and-electrophysiological-analysis
#2
Ana Fajardo-Serrano, Lei Liu, David D Mott, Alexander J McDonald
The basolateral amygdala receives a very dense cholinergic innervation from the basal forebrain that is important for memory consolidation. Although behavioral studies have shown that both M1 and M2 muscarinic receptors are critical for these mnemonic functions, there have been very few neuroanatomical and electrophysiological investigations of the localization and function of different types of muscarinic receptors in the amygdala. In the present study we investigated the subcellular localization of M2 muscarinic receptors (M2Rs) in the anterior basolateral nucleus (BLa) of the mouse, including the localization of M2Rs in parvalbumin (PV) immunoreactive interneurons, using double-labeling immunoelectron microscopy...
June 16, 2017: Neuroscience
https://www.readbyqxmd.com/read/28628945/precise-spike-timing-dynamics-of-hippocampal-place-cell-activity-sensitive-to-cholinergic-disruption
#3
Ehren L Newman, Sarah Jo C Venditto, Jason R Climer, Elijah A Petter, Shea N Gillet, Sam Levy
New memory formation depends upon both the hippocampus and modulatory effects of acetylcholine. The mechanism by which acetylcholine levels in the hippocampus enable new encoding remains poorly understood. Here, we tested the hypothesis that cholinergic modulation supports memory formation by leading to structured spike timing in the hippocampus. Specifically, we tested if phase precession in dorsal CA1 was reduced under the influence of a systemic cholinergic antagonist. Unit and field potential was recorded from the dorsal CA1 of rats as they completed laps on a circular track for food rewards before and during the influence of the systemically administered acetylcholine muscarinic receptor antagonist scopolamine...
June 19, 2017: Hippocampus
https://www.readbyqxmd.com/read/28625139/targeting-cholinergic-system-to-modulate-liver-injury
#4
Ravirajsinh N Jadeja, Vikrant P Rachakonda, Sandeep Khurana
Over the past few decades, evidence accumulated to indicate that parasympathetic innervation regulates liver injury and regeneration. Liver derives its parasympathetic input via vagus nerve. In animal models, vagus nerve stimulation and transection are frequently used to determine the impact of parasympathetic input on liver injury responses. Such strategies provide limited understanding of post-neuronal mechanisms involved in regulation of liver injury. The hepatic branch of vagus nerve releases acetylcholine (ACh), which activates muscarinic and nicotinic receptors in hepatocytes as well as non-parenchymal cells to modulate cellular functions...
June 18, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28623171/broad-analgesic-activity-of-a-novel-selective-m1-agonist
#5
Michael W Wood, Giovanni Martino, Martin Coupal, Mattias Lindberg, Patricia Schroeder, S Santhakumar, Manon Valiquette, Johan Sandin, Daniel Widzowski, Jennifer Laird
Although the muscarinic receptor family has long been a source of potentially compelling targets for small molecule drug discovery, it was difficult to achieve agonist selectivity within the family. A new class of M1 muscarinic agonists has emerged, and these compounds have been characterized as agonists that activate the receptor at an allosteric site. Members of this class of M1 agonists have been shown to be selective across the muscarinic receptors. However, upon introduction of a novel pharmacologic mechanism, it is prudent to ensure that no new off-target activities have arisen, particularly within the context of in vivo experiments...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28619712/targeting-acetylcholine-receptor-m3-prevents-the-progression-of-airway-hyperreactivity-in-a-mouse-model-of-childhood-asthma
#6
Kruti R Patel, Yan Bai, Kenneth G Trieu, Juliana Barrios, Xingbin Ai
Asthma often progresses into adulthood from early-life episodes of adverse environmental exposures. However, how the injury to developing lungs contributes to the pathophysiology of persistent asthma remains poorly understood. In this study, we identified an age-related mechanism along the cholinergic nerve-airway smooth muscle (ASM) axis that underlies prolonged airway hyperreactivity (AHR) in mice. We showed that ASM continued to mature until ∼3 wk after birth. Coinciding with postnatal ASM maturation, there was a critical time window for the development of ASM hypercontractility after cholinergic stimulation...
June 15, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28610667/why-choose-tiotropium-for-my-patient-a-comprehensive-review-of-actions-and-outcomes-versus-other-bronchodilators
#7
REVIEW
David M Halpin, Alan G Kaplan, Richard K Russell
PURPOSE: Chronic obstructive pulmonary disease (COPD) and asthma are leading causes of morbidity and mortality. This narrative review provides an appraisal of the pharmacological and clinical characteristics of tiotropium in COPD and asthma, and examines how these compare with other long-acting bronchodilators. The evidence base is placed into context by relating it to factors affecting clinicians' choice of therapy. MAIN FINDINGS: Desirable attributes of a long-acting muscarinic antagonist (LAMA) maintenance therapy include effective pharmacological bronchodilation, improved lung function, exacerbation efficacy, and positive effects on symptom control, exercise capacity and quality of life across a broad patient population...
July 2017: Respiratory Medicine
https://www.readbyqxmd.com/read/28609709/novel-muscarinic-acetylcholine-receptor-hybrid-ligands-embedding-quinuclidine-and-1-4-dioxane-fragments
#8
Fabio Del Bello, Alessandro Bonifazi, Gianfabio Giorgioni, Riccardo Petrelli, Wilma Quaglia, Angela Altomare, Aurelia Falcicchio, Rosanna Matucci, Giulio Vistoli, Alessandro Piergentili
To obtain novel muscarinic acetylcholine receptor (mAChR) antagonists, the enantiomers of the hybrid compounds 3-5, in which the quinuclidin-3-yloxy fragment of solifenacin and the 6,6-diphenyl-1,4-dioxane-2-yl moiety of 2 linked by an ester or ether spacer were embedded in the same chemical entity, were prepared and evaluated for their affinity at the five mAChR subtypes (M1-M5). Stereochemistry and the nature of the linker between the quinuclidine moiety and the 1,4-dioxane nucleus play an important role on the affinities of the compounds...
June 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28609577/cerebrolysin-prevents-deficits-in-social-behavior-repetitive-conduct-and-synaptic-inhibition-in-a-rat-model-of-autism
#9
Roberto Cuevas-Olguin, Swagata Roychowdhury, Anwesha Banerjee, Francisco Garcia-Oscos, Eric Esquivel-Rendon, María Elena Bringas, Michael P Kilgard, Gonzalo Flores, Marco Atzori
Autism spectrum disorder (ASD) is a syndrome of diverse neuropsychiatric diseases of growing incidence characterized by repetitive conduct and impaired social behavior and communication for which effective pharmacological treatment is still unavailable. While the mechanisms and etiology of ASD are still unknown, a consensus is emerging about the synaptic nature of the syndrome, suggesting a possible avenue for pharmacological treatment with synaptogenic compounds. The peptidic mixture cerebrolysin (CBL) has been successfully used during the last three decades in the treatment of stroke and neurodegenerative disease...
June 13, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28608746/new-insights-in-the-metabolism-of-oxybutynin-evidence-of-n-oxidation-of-propargylamine-moiety-and-rearrangement-to-enaminoketone
#10
Silvio Aprile, Rossana Canavesi, Rosanna Matucci, Cristina Bellucci, Erika Del Grosso, Giorgio Grosa
1. Oxybutynin hydrochloride is an antimuscarinic agent prescribed to patients with an overactive bladder and symptoms of urinary urge incontinence. Oxybutynin undergoes pre-systemic metabolism, and the N-desethyloxybutynin (Oxy-DE), is reported to have similar anticholinergic effects. 2. We revisited the oxidative metabolic fate of oxybutynin by liquid chromatography tandem mass spectrometry analysis of incubations with rat and human liver fractions, and by measuring plasma and urine samples collected after oral administration of oxybutynin in rats...
June 13, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28608540/sevoflurane-vs-propofol-in-post-operative-catheter-related-bladder-discomfort-a-prospective-randomized-study
#11
H-C Kim, H-P Park, J Lee, M-H Jeong, K-H Lee
BACKGROUND: Post-operative catheter-related bladder discomfort (CRBD) causes increased emergence agitation. Muscarinic receptor activation is a major mechanism in CRBD development. Experimental studies showed that sevoflurane has anti-muscarinic effects whereas propofol does not. Our hypothesis was that sevoflurane anaesthesia would reduce the incidence of CRBD following bladder surgery. METHODS: In total, 82 patients undergoing transurethral bladder tumour excision (TURBT) were assigned randomly to two groups according to the maintenance anaesthetic agent received: sevoflurane (n = 41) or propofol (n = 41)...
June 13, 2017: Acta Anaesthesiologica Scandinavica
https://www.readbyqxmd.com/read/28600746/dopamine-induces-inhibitory-effects-on-the-circular-muscle-contractility-of-mouse-distal-colon-via-d1-and-d2-like-receptors
#12
Michelangelo Auteri, Maria Grazia Zizzo, Antonella Amato, Rosa Serio
Dopamine (DA) acts as gut motility modulator, via D1- and D2-like receptors, but its effective role is far from being clear. Since alterations of the dopaminergic system could lead to gastrointestinal dysfunctions, a characterization of the enteric dopaminergic system is mandatory. In this study, we investigated the role of DA and D1- and D2-like receptors in the contractility of the circular muscle of mouse distal colon by organ-bath technique. DA caused relaxation in carbachol-precontracted circular muscle strips, sensitive to domperidone, D2-like receptor antagonist, and mimicked by bromocriptine, D2-like receptor agonist...
June 9, 2017: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28600120/effects-of-cevimeline-on-excitability-of-parasympathetic-preganglionic-neurons-in-the-superior-salivatory-nucleus-of-rats
#13
Yoshihiro Mitoh, Hirotaka Ueda, Hiroyuki Ichikawa, Masako Fujita, Motoi Kobashi, Ryuji Matsuo
The superior salivatory nucleus (SSN) contains parasympathetic preganglionic neurons innervating the submandibular and sublingual salivary glands. Cevimeline, a muscarinic acetylcholine receptor (mAChR) agonist, is a sialogogue that possibly stimulates SSN neurons in addition to the salivary glands themselves because it can cross the blood-brain barrier (BBB). In the present study, we examined immunoreactivities for mAChR subtypes in SSN neurons retrogradely labeled with a fluorescent tracer in neonatal rats...
May 30, 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/28598634/design-and-synthesis-of-%C3%AE-and-%C3%AE-lactam-m1-positive-allosteric-modulators-pams-convulsion-and-cholinergic-toxicity-of-an-m1-selective-pam-with-weak-agonist-activity
#14
Jennifer E Davoren, Michelle Garnsey, Betty Pettersen, Michael A Brodney, Jeremy R Edgerton, Jean Philippe Fortin, Sarah Grimwood, Antony R Harris, Stephen Jenkinson, Terry P Kenakin, John T Lazzaro, Che-Wah Lee, Susan M Lotarski, Lisa Nottebaum, Steven V O'Neil, Michael Popiolek, Simeon Ramsey, Stefanus J Steyn, Catherine A Thorn, Lei Zhang, Damien Webb
Recent data demonstrated that activation of the muscarinic M1 receptor by a subtype-selective positive allosteric modulator (PAM) contributes to the gastrointestinal (GI) and cardiovascular (CV) cholinergic adverse events (AEs) previously attributed to M2 and M3 activation. These studies were completed using PAMs that also exhibited allosteric agonist activity, leaving open the possibility that direct agonism, rather than allosteric modulation, could be responsible for the adverse effects. This manuscript describes the design and synthesis of lactam-derived M1 PAMs that address this question...
June 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28598489/nicotinic-acetylcholine-receptor-mediated-protection-of-the-rat-heart-exposed-to-ischemia-reperfusion
#15
Spyros A Mavropoulos, Nayaab S Khan, Asaph C J Levy, Bradley T Faliks, Cristina P Sison, Valentin A Pavlov, Youhua Zhang, Kaie Ojamaa
Reperfusion injury following acute myocardial infarction is associated with significant morbidity. Activation of neuronal or non-neuronal cholinergic pathways in the heart has been shown to reduce ischemic injury and this effect has been attributed primarily to muscarinic acetylcholine receptors. In contrast, the role of nicotinic receptors, specifically alpha-7 subtype (α7nAChR) in the myocardium remains unknown which offers an opportunity to potentially repurpose several agonists/modulators that are currently under development for neurologic indications...
June 8, 2017: Molecular Medicine
https://www.readbyqxmd.com/read/28589042/pyridostigmine-induced-prolonged-asystole-in-a-patient-with-myasthenia-gravis-successfully-treated-with-hyoscyamine
#16
Mohammad Saud Khan, Abhinav Tiwari, Zubair Khan, Himani Sharma, Mohammad Taleb, Jeffrey Hammersley
Reversible acetylcholinesterase inhibitors are used as first-line treatment for myasthenia gravis. They improve symptoms by increasing concentration of acetylcholine at the neuromuscular junction and stimulating nicotinic receptors. Serious bradyarrhythmias can occur from muscarinic stimulation in heart, which in rare cases may progress to asystole. These patients can initially be managed with hyoscyamine, a muscarinic antagonist. Persistence of bradyarrhythmias even after hyoscyamine treatment may warrant pacemaker placement...
2017: Case Reports in Cardiology
https://www.readbyqxmd.com/read/28587876/strength-of-cholinergic-tone-dictates-the-polarity-of-dopamine-d2-receptor-modulation-of-striatal-cholinergic-interneuron-excitability-in-dyt1-dystonia
#17
Mariangela Scarduzio, Chelsea N Zimmerman, Karen L Jaunarajs, Qin Wang, David G Standaert, Lori L McMahon
Balance between cholinergic and dopaminergic signaling is central to striatal control of movement and cognition. In dystonia, a common disorder of movement, anticholinergic therapy is often beneficial. This observation suggests there is a pathological increase in cholinergic tone, yet direct confirmation is lacking. In DYT1, an early-onset genetic form of dystonia caused by a mutation in the protein torsinA (TorA), the suspected heightened cholinergic tone is commonly attributed to faulty dopamine D2 receptor (D2R) signaling where D2R agonists cause excitation of striatal cholinergic interneurons (ChIs), rather than the normal inhibition of firing observed in wild-type animals, an effect known as "paradoxical excitation"...
June 3, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28585805/ligand-specific-restriction-of-extracellular-conformational-dynamics-constrains-signaling-of-the-m2-muscarinic-receptor
#18
Marcel Bermudez, Andreas Bock, Fabian Krebs, Ulrike Holzgrabe, Klaus Mohr, Martin J Lohse, Gerhard Wolber
G protein-coupled receptors transmit extracellular signals across cell membranes via different G protein classes and β-arrestins. Some pathways may be therapeutically beneficial, whereas others may be detrimental under certain pathophysiological conditions. For many GPCRs, biased agonists are available, which preferentially signal through one pathway or a subset of pathways, and harnessing biased agonism could be a potential novel therapeutic strategy. However, the incomplete mechanistic understanding of biased agonism hampers rational design of biased ligands...
June 12, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28584269/time-dependent-changes-and-potential-mechanisms-of-glucose-lipid-metabolic-disorders-associated-with-chronic-clozapine-or-olanzapine-treatment-in-rats
#19
Xuemei Liu, Zhixiang Wu, Jiamei Lian, Chang-Hua Hu, Xu-Feng Huang, Chao Deng
Chronic treatment with second-generation antipsychotic drugs (SGAs) has been associated with an increased risk of metabolic syndrome. To evaluate the longitudinal changes in glucose-lipid homeostasis after SGA use, we studied the time-dependent effects of olanzapine (OLZ) (3 mg/kg, b.i.d.) or clozapine (CLZ) (20 mg/kg, b.i.d.) treatment on metabolic profiles for 9 weeks in rats. Although only OLZ significantly increased body weight in rats, both OLZ and CLZ elevated blood lipid levels. Chronic OLZ treatment induced significant weight gain leading to a higher fasting insulin level and impaired glucose tolerance, whereas CLZ lowered fasting insulin levels and impaired glucose tolerance independent of weight gain...
June 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28580487/role-of-cyclic-nucleotides-in-the-effect-of-hydrogen-sulfide-on-contractions-of-rat-jejunum
#20
D M Gabitova, I F Shaidullov, G I Sabirullina, M U Shafigullin, F G Sitdikov, G F Sitdikova
We studied the role of cyclic nucleotides in the influence of hydrogen sulfide (H2S) donor, sodium hydrosulfide (NaHS, 200 μM), on motor activity of rat jejunum. NaHS reduced spontaneous and carbachol-induced contractions of rat jejunum segment, which suggests that H2S can act through mechanisms involving muscarinic receptor activation. Against the background of a membrane-penetrating non-hydrolyzable cAMP analogue or under conditions of adenylate cyclase blockade, the inhibitory effect of NaHS on the carbachol-induced contractions was maintained...
June 3, 2017: Bulletin of Experimental Biology and Medicine
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