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Muscarinic receptors

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https://www.readbyqxmd.com/read/29156534/effects-of-standardized-isopropanolic-black-cohosh-and-estrogen-on-salivary-function-in-ovariectomized-rats
#1
Shuya Liu, Kaiyu Niu, Yunmeng Da, Yao Liu, Jing Zhang, Wenjuan Wang, Yi Zhang, Hai Jiang, Ke Wang, Wenpei Bai, Lihua Qin, Jing Jia
Oral dryness is a common feature in menopausal women. Estrogen therapy can relieve this symptom; however, the underlying mechanism was not clear. Standardized isopropanolic black cohosh (Actaea racemosa; Remifemin) can also relieve menopausal symptoms, such as hot flashes and sweating. Our previous study showed that standardized isopropanolic black cohosh could protect the submandibular gland structure. To investigate the effects and possible mechanisms of action of estrogen and standardized isopropanolic black cohosh on submandibular gland function in ovariectomized (OVX) rats, we measured body weight, daily water consumption, and blood flow in the submandibular glands...
November 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29154951/regulation-of-neural-ion-channels-by-muscarinic-receptors
#2
REVIEW
David A Brown
The excitable behaviour of neurons is determined by the activity of their endogenous membrane ion channels. Since muscarinic receptors are not themselves ion channels, the acute effects of muscarinic receptor stimulation on neuronal function are governed by the effects of the receptors on these endogenous neuronal ion channels. This review considers some principles and factors determining the interaction between subtypes and classes of muscarinic receptors with neuronal ion channels, and summarizes the effects of muscarinic receptor stimulation on a number of different channels, the mechanisms of receptor - channel transduction and their direct consequences for neuronal activity...
November 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29154125/endogenous-g%C3%AE-q-coupled-neuromodulator-receptors-activate-protein-kinase-a
#3
Yao Chen, Adam J Granger, Trinh Tran, Jessica L Saulnier, Alfredo Kirkwood, Bernardo L Sabatini
Protein kinase A (PKA) integrates inputs from G-protein-coupled neuromodulator receptors to modulate synaptic and cellular function. Gαs signaling stimulates PKA activity, whereas Gαi inhibits PKA activity. Gαq, on the other hand, signals through phospholipase C, and it remains unclear whether Gαq-coupled receptors signal to PKA in their native context. Here, using two independent optical reporters of PKA activity in acute mouse hippocampus slices, we show that endogenous Gαq-coupled muscarinic acetylcholine receptors activate PKA...
November 3, 2017: Neuron
https://www.readbyqxmd.com/read/29153411/how-do-we-critically-use-long-acting-muscarinic-receptor-antagonists-and-beta-adrenergic-receptor-agonists-monotherapy-or-these-combination-therapies-depending-on-the-situation-in-japanese-patients-with-copd
#4
EDITORIAL
https://www.readbyqxmd.com/read/29151079/mechanisms-of-vasorelaxation-induced-by-total-flavonoids-of-euphorbia-humifusa-in-rat-aorta
#5
T T Wang, Z Q Zhou, S Wang, X W Ji, B Wu, L Y Sun, J F Wen, D G Kang, H S Lee, K W Cho, S N Jin
Euphorbia humifusa Willd. (EH), rich in flavonoids, has long been used for the treatment of bacillary dysentery and enteritis in China, and is known to have antioxidant, hypotensive and hypolipidemic properties. However, the vasorelaxant effect of total flavonoids of EH (TFEH) and action mechanisms are not clearly defined yet. The aim of the present study was to investigate the effects of TFEH on the vascular tension and its underlying mechanisms. Experiments were performed in rat thoracic aorta using the organ bath system...
August 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29146932/activation-of-endogenous-arginine-vasopressin-neurons-inhibit-food-intake-by-using-a-novel-transgenic-rat-line-with-dreadds-system
#6
Mitsuhiro Yoshimura, Kazuaki Nishimura, Haruki Nishimura, Satomi Sonoda, Hiromichi Ueno, Yasuhito Motojima, Reiko Saito, Takashi Maruyama, Yuki Nonaka, Yoichi Ueta
Various studies contributed to discover novel mechanisms of central arginine vasopressin (AVP) system responsible for the behaviour albeit endogenous vasopressin activation. We established a novel transgenic rat line which expresses both human muscarinic acetylcholine receptors (hM3Dq), of which ligand is clozapine-N-oxide (CNO), and mCherry fluorescence specifically in AVP neurons. The mCherry neurons that indicate the expression of the hM3Dq gene were observed in the suprachiasmatic (SCN), supraoptic (SON), and paraventricular nuclei (PVN)...
November 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29146505/muscarinic-receptor-oligomerization
#7
REVIEW
Sara Marsango, Richard J Ward, Elisa Alvarez-Curto, Graeme Milligan
G protein coupled receptors (GPCRs) have been classically described as monomeric entities that function by binding in a 1:1 stoichiometric ratio to both ligand and downstream signalling proteins. However, in recent years, a growing numbers of studies have supported the hypothesis that these receptors can interact to form dimers and higher order oligomers although the molecular basis for these interactions, the overall quaternary arrangements and the functional importance of the GPCR oligomerization remain topics of intense speculation...
November 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29146472/discovery-of-the-first-low-shift-positive-allosteric-modulators-for-the-muscarinic-m1-receptor
#8
Alexander Flohr, Roman Hutter, Barbara Mueller, Claudia Bohnert, Mélanie Pellisson, Hervé Schaffhauser
Positive modulation of the muscarinic M1-receptor has for a long time attracted scientists and drug developers for the potential treatment of Alzheimer's disease or Schizophrenia. The precognitive potential of M1 activation has however not been clinically demonstrated as a result of side effects associated both with agonists and positive allosteric modulators (PAM's) of the M1-receptor. To avoid excessive activation of the M1-receptor we have designed a new screening format and developed the first low-shift positive allosteric modulators for the M1 receptor...
November 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29141986/arfgap1-restricts-mycobacterium-tuberculosis-entry-by-controlling-the-actin-cytoskeleton
#9
Ok-Ryul Song, Christophe J Queval, Raffaella Iantomasi, Vincent Delorme, Sabrina Marion, Romain Veyron-Churlet, Elisabeth Werkmeister, Michka Popoff, Isabelle Ricard, Samuel Jouny, Nathalie Deboosere, Frank Lafont, Alain Baulard, Edouard Yeramian, Laurent Marsollier, Eik Hoffmann, Priscille Brodin
The interaction of Mycobacterium tuberculosis (Mtb) with pulmonary epithelial cells is critical for early stages of bacillus colonization and during the progression of tuberculosis. Entry of Mtb into epithelial cells has been shown to depend on F-actin polymerization, though the molecular mechanisms are still unclear. Here, we demonstrate that mycobacterial uptake into epithelial cells requires rearrangements of the actin cytoskeleton, which are regulated by ADP-ribosylation factor 1 (Arf1) and phospholipase D1 (PLD1), and is dependent on the M3 muscarinic receptor (M3R)...
November 15, 2017: EMBO Reports
https://www.readbyqxmd.com/read/29138081/regulation-and-trafficking-of-muscarinic-acetylcholine-receptors
#10
REVIEW
Dmitry Zenko, James N Hislop
Fidelity of signal transduction relies on cells expressing the appropriate number of functional receptors. Fluctuation in the total number of muscarinic acetylcholine receptors has been implicated in a range of physiological and pathophysiological processes, and the mechanisms responsible for this regulation represent potential molecular targets for therapeutic intervention. This article will review the current literature on the endocytic trafficking of muscarinic receptors and how knowledge of the trafficking of related receptors might influence future studies...
November 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29138080/muscarinic-receptor-subtype-distribution-in-the-central-nervous-system-and-relevance-to-aging-and-alzheimer-s-disease
#11
REVIEW
E P Lebois, C Thorn, J R Edgerton, M Popiolek, S Xi
Muscarinic acetylcholine receptors (mAChRs) are G proteincoupled receptors (GPCRs) that mediate the metabotropic actions of acetylcholine (ACh). There are five subtypes of mAChR, M1 - M5, which are expressed throughout the central nervous system (CNS) on numerous cell types and represent promising treatment targets for a number of different diseases, disorders, and conditions of the CNS. Although the present review will focus on Alzheimer's disease (AD) and amnestic mild cognitive impairment (aMCI), a number of conditions such as Parkinson's disease (PD), schizophrenia, and others represent significant unmet medical needs for which selective muscarinic agents could offer therapeutic benefits...
November 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29128789/diuretic-and-natriuretic-effect-of-luteolin-in-normotensive-and-hypertensive-rats-role-of-muscarinic-acetylcholine-receptors
#12
Thaise Boeing, Luísa Mota da Silva, Marihá Mariott, Sérgio Faloni de Andrade, Priscila de Souza
BACKGROUND: Luteolin is a very common phenolic compound found in a wide variety of natural products. Although several biological properties have already been described regarding the beneficial effect of luteolin in the cardiovascular and renal system, no scientific research explored its potential effect as a diuretic agent in experimental trials. METHODS: Groups of male normotensive (NTR) and spontaneously hypertensive rats (SHR) were orally treated with vehicle, hydrochlorothiazide or luteolin...
May 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128414/mapping-of-the-prenatal-and-postnatal-methamphetamine-effects-on-d1-like-dopamine-m1-and-m2-muscarinic-receptors-in-rat-central-nervous-system
#13
Vladimir Farar, Paulina Valuskova, Maria Sevcikova, Jaromir Myslivecek, Romana Slamberova
Methamphetamine (MA) is worldwide known drug with high potential for addiction that causes dopamine, noradrenaline and serotonin release. MA is also able to increase acetylcholine levels in adult rodents. The aim of this study was to map changes in D1-like dopamine receptors (DR), M1 and M2 muscarinic receptors (MR), and the total number of MR (M1-M5 MR) in the CNS of rats exposed to MA prenatally and in adulthood. Rat mothers were exposed to MA (5mg/kg s.c.) or saline during the entire gestation period and their male offspring were administered in adulthood with single MA (1mg/kg) or saline injection...
November 9, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29128314/early-changes-in-m2-muscarinic-acetylcholine-receptors-machrs-induced-by-sarin-intoxication-may-be-linked-to-long-lasting-neurological-effects
#14
Zipora Pittel, Shlomi Lazar, Rellie Gez, Shira Chapman
The effect of sarin on the binding parameters (KD & Bmax) of M2 muscarinic acetylcholine receptor (mAChR) was studied 24h and 1 week post exposure. Male & female Sprague-Daweley rats were poisoned with 1XLD50 sarin (80μg/kg, im) followed by treatment of trimedoxime bromide and atropine (7.5:5mg/kg, im) 1min later. Brains were removed and analyzed for M2 mAChR binding, using [(3)H]AFDX384, an M2 selective antagonist. A significant increase in KD of M2 mAChR was found in the cortex 24h post poisoning, displaying elevation from 4...
November 8, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/29127015/oxotremorine-m-potentiates-nmda-receptors-by-muscarinic-receptor-dependent-and-independent-mechanisms
#15
Ruud Zwart, Hannah Reed, Emanuele Sher
Muscarinic acetylcholine M1 receptors play an important role in synaptic plasticity in the hippocampus and cortex. Potentiation of NMDA receptors as a consequence of muscarinic acetylcholine M1 receptor activation is a crucial event mediating the cholinergic modulation of synaptic plasticity, which is a cellular mechanism for learning and memory. In Alzheimer's disease, the cholinergic input to the hippocampus and cortex is severely degenerated, and agonists or positive allosteric modulators of M1 receptors are therefore thought to be of potential use to treat the deficits in cognitive functions in Alzheimer's disease...
November 7, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29123207/atropine-augments-cardiac-contractility-by-inhibiting-camp-specific-phosphodiesterase-type-4
#16
Ruwan K Perera, Thomas H Fischer, Michael Wagner, Matthias Dewenter, Christiane Vettel, Nadja I Bork, Lars S Maier, Marco Conti, Juergen Wess, Ali El-Armouche, Gerd Hasenfuß, Viacheslav O Nikolaev
Atropine is a clinically relevant anticholinergic drug, which blocks inhibitory effects of the parasympathetic neurotransmitter acetylcholine on heart rate leading to tachycardia. However, many cardiac effects of atropine cannot be adequately explained solely by its antagonism at muscarinic receptors. In isolated mouse ventricular cardiomyocytes expressing a Förster resonance energy transfer (FRET)-based cAMP biosensor, we confirmed that atropine inhibited acetylcholine-induced decreases in cAMP. Unexpectedly, even in the absence of acetylcholine, after G-protein inactivation with pertussis toxin or in myocytes from M2- or M1/3-muscarinic receptor knockout mice, atropine increased cAMP levels that were pre-elevated with the β-adrenergic agonist isoproterenol...
November 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29122691/sexually-diergic-hypothalamic-pituitary-adrenal-axis-responses-to-selective-and-non-selective-muscarinic-antagonists-prior-to-cholinergic-stimulation-by-physostigmine-in-rats
#17
Marissa A Smail, Jessica L Soles, Tracy E Karwoski, Robert T Rubin, Michael E Rhodes
Central cholinergic systems regulate the hypothalamic-pituitary-adrenal (HPA) axis differentially in males and females (sexual diergism). We previously investigated the role of muscarinic receptors in this regulation by administering physostigmine (PHYSO), an acetylcholinesterase inhibitor, to male and female rats pretreated with scopolamine (SCOP), a nonselective muscarinic antagonist. SCOP pretreatment enhanced adrenocorticotropic hormone (ACTH) and corticosterone (CORT) responses in both sexes; males had greater ACTH responses while females had greater CORT responses...
November 7, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29122673/involvement-of-dual-mechanisms-of-anti-muscarinic-and-ca-antagonistic-activities-to-validate-the-folkloric-uses-of-cyperus-niveus-retz-in-multiple-gastrointestinal-ailments
#18
Ambreen Aleem, Khalid Hussain Janbaz
ETHNOPHARMACOLOGICAL RELEVANCE: Cyperus species are famous for their traditional uses and very commonly used for their anti-spasmodic and anti-diarrheal activities. Cyperus niveus Retz. is used in local traditional system of medicine in Pakistan to treat various gastrointestinal ailments. AIM OF THE STUDY: The aim of the study was to validate the traditional uses and to provide the possible mechanisms for the medicinal use of Cyperus niveus Retz. in gastrointestinal ailments...
November 6, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29121457/drugs-implicated-in-systemic-autoimmunity-modulate-neutrophil-extracellular-trap-formation
#19
Jorge A Irizarry-Caro, Carmelo Carmona-Rivera, Daniella M Schwartz, Sami S Khaznadar, Mariana J Kaplan, Peter C Grayson
OBJECTIVE: Aberrant neutrophil extracellular trap (NET) formation has been implicated as a mechanism to induce auto-reactivity in at-risk individuals. The study objective was to assess whether medications implicated in cases of drug-induced autoimmunity (hydralazine and procainamide) and medications less commonly associated with drug-induced autoimmunity (minocycline and clozapine) induce NET formation and/or prevent NET degradation. METHODS: Human neutrophils were incubated with the drugs of interest and resultant NET formation was quantified by fluorescent microscopy...
November 9, 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29120510/in-vitro-characterization-of-gamma-oscillations-in-the-hippocampal-formation-of-the-domestic-chick
#20
Pradeep Dheerendra, Nicholas M Lynch, Joseph Crutwell, Mark O Cunningham, Tom V Smulders
Avian and mammalian brains have evolved independently from each other for about 300 million years. During that time, the hippocampal formation (HF) has diverged in morphology and cyto-architecture, but seems to have conserved much of its function. It is therefore an open question how seemingly different neural organizations can generate the same function. A prominent feature of the mammalian hippocampus is that it generates different neural oscillations, including the gamma rhythm, which plays an important role in memory processing...
November 9, 2017: European Journal of Neuroscience
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