Genomes and Genes
Summary: One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.
Publications181 found, 100 shown here
- Lack of coupling of muscarinic receptors to phosphoinositide metabolism and adenylyl cyclase in human lymphocytes and polymorphonuclear leukocytes: studies in healthy subjects and allergic asthmatic patientsH Meurs
Department of Allergology, University Hospital, Groningen, The Netherlands
Int Arch Allergy Immunol 100:19-27. 1993..The results indicate that leukocytes are not a suitable model to investigate the muscarinic receptor function in relation to bronchial asthma...
- Nigrostriatal dopamine release modulated by mesopontine muscarinic receptorsAnthony D Miller
Department of Psychology, Macquarie University, Sydney, NSW 2109, Australia
Neuroreport 15:1805-8. 2004..These results suggest that M2/4 muscarinic receptors in the mesopontine tonically influence SNc basal dopamine cell activity and striatal dopamine release.
- Nucleus accumbens acetylcholine regulates appetitive learning and motivation for food via activation of muscarinic receptorsWayne E Pratt
Wisconsin Psychiatric Institute and Clinics, Department of Psychiatry, University of Wisconsin Madison Medical School, Madison, WI 53719, USA
Behav Neurosci 118:730-9. 2004..These novel results implicate nucleus accumbens muscarinic receptors in the modulation of appetitive learning, performance, and motivation for food.
- Regulation of IPSP theta rhythm by muscarinic receptors and endocannabinoids in hippocampusChristian G Reich
Department of Physiology, Program in Neuronscience, University of Maryland School of Medicine, Baltimore, 21201, USA
J Neurophysiol 94:4290-9. 2005..Simultaneous recordings from pyramidal cell pairs reveal synchronous theta-frequency IPSPs in neighboring pyramidal cells, suggesting that these IPSPs may help entrain or modulate small groups of pyramidal cells...
- Muscarinic receptors, leukotriene B4 production and neutrophilic inflammation in COPD patientsM Profita
Institute of Biomedicine and Molecular Immunology, Italian National Research Council, Palermo, Italy
Allergy 60:1361-9. 2005..CONCLUSIONS: The results obtained show that muscarinic receptors may be involved in airway inflammation in COPD subjects through ACh-induced, ERK1/2-dependent LTB4 release...
- Endogenous ACh enhances striatal NMDA-responses via M1-like muscarinic receptors and PKC activationP Calabresi
Clinica Neurologica, Dip Neuroscienze, Universita di Roma Tor Vergata, Rome, Italy
Eur J Neurosci 10:2887-95. 1998..were antagonized either by scopolamine (3 microM) or by pirenzepine (10-100 nM), an antagonist of M1-like muscarinic receptors, but not by methoctramine (300 nM), an antagonist of M2-like muscarinic receptor...
- Striatal muscarinic receptors promote activity dependence of dopamine transmission via distinct receptor subtypes on cholinergic interneurons in ventral versus dorsal striatumSarah Threlfell
Department of Physiology, Anatomy and Genetics, University of Oxford, Oxford, United Kingdom
J Neurosci 30:3398-408. 2010..How DA signaling is regulated by striatal muscarinic receptors (mAChRs) is unresolved; contradictory reports indicate suppression or facilitation, implicating several ..
- Activation of M1-like muscarinic receptors is required for the induction of corticostriatal LTPP Calabresi
Clinica Neurologica, Dipartimento di Neuroscienze, Universita degli Studi di Roma, Italy
Neuropharmacology 38:323-6. 1999..receptor antagonists scopolamine and pirenzepine fully prevented the induction of LTP suggesting that the activation of M1-like muscarinic receptors is a crucial event in the conditioning phase of this form of synaptic plasticity.
- Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and beta-adrenoceptorsElfaridah P Frazier
Department of Pharmacology and Pharmacotherapy, Academic Medical Center, University of Amsterdam, Meibergdreef 15, 1105 AZ, Amsterdam, The Netherlands
Naunyn Schmiedebergs Arch Pharmacol 377:449-62. 2008..contraction of the urinary bladder, which is required for voiding, is predominantly mediated by muscarinic receptors, primarily the M3 subtype, with the M2 subtype providing a secondary backup role...
- Activation of sphingosine kinase by muscarinic receptors enhances NO-mediated and attenuates EDHF-mediated vasorelaxationArthur C M Mulders
Department of Pharmacology and Pharmacotherapy, Academic Medical Center, Meibergdreef 15, Amsterdam, The Netherlands
Basic Res Cardiol 104:50-9. 2009..Moreover, a disturbed regulation of sphingolipid metabolism in the vascular wall may therefore play a role in the aetiology/pathology of disease states characterized by endothelial dysfunction...
- Determination of [35S]guanosine-5'-O-(3-thio)triphosphate binding mediated by cholinergic muscarinic receptors in membranes from Chinese hamster ovary cells and rat striatum using an anti-G protein scintillation proximity assayN W Delapp
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
J Pharmacol Exp Ther 289:946-55. 1999..Antibody capture GTPgamma35S binding using scintillation proximity assay technology provides a convenient, productive alternative to immunoprecipitation for exploration of receptor-G protein interaction in cells and tissues...
- Blockade of M2-like muscarinic receptors enhances long-term potentiation at corticostriatal synapsesP Calabresi
Clinica Neurologica, Dip Neuroscienze, Universita di Roma Tor Vergata, Rome, Italy
Eur J Neurosci 10:3020-3. 1998..We have investigated the role of M2-like muscarinic receptors in striatal LTP by utilizing intracellular recordings in vitro from a rat corticostriatal slice preparation...
- Fluorescence changes reveal kinetic steps of muscarinic receptor-mediated modulation of phosphoinositides and Kv7.2/7.3 K+ channelsJill B Jensen
Department of Physiology and Biophysics, University of Washington School of Medicine, Seattle, WA 98195, USA
J Gen Physiol 133:347-59. 2009..0 s) to become nearly contemporaneous with Galpha(q)/PLC interaction. Evidently, channel release of PIP(2) and closure are rapid, and the availability of active PLC limits the rate of M current suppression...
- Phosphorylation-dependent activation of the Ras-GRF/CDC25Mm exchange factor by muscarinic receptors and G-protein beta gamma subunitsR R Mattingly
Department of Pathology, University of Vermont College of Medicine, Burlington 05405, USA
Nature 382:268-72. 1996b>Muscarinic receptors activate Ras through a pathway distinct from that mediated through translocation of the exchange factor mSos1 by receptor tyrosine kinases...
- Qualitative and quantitative expression profile of muscarinic receptors in human urothelium and detrusorShachi Tyagi
Department of Urology, University of Pittsburgh, Pittsburgh, Pennsylvania 15213, USA
J Urol 176:1673-8. 2006..RESULTS: All 5 muscarinic receptors were detected in fresh human bladder tissue by reverse transcriptase-polymerase chain reaction RNA...
- Muscarinic receptors induce LTD of NMDAR EPSCs via a mechanism involving hippocalcin, AP2 and PSD-95Jihoon Jo
Henry Wellcome Laboratories for Integrative Neuroscience and Endocrinology, Faculty of Medicine and Dentistry, University of Bristol, Bristol, UK
Nat Neurosci 13:1216-24. 2010..We found that stimulation of muscarinic receptors, either by an agonist or by the synaptic release of acetylcholine, led to long-term depression (LTD) of ..
- Nonselective cation channels activated by the stimulation of muscarinic receptors in mammalian gastric smooth muscleInsuk So
Department of Physiology and Biophysics, Seoul National University College of Medicine, 28 Yongon-dong, Chongno-gu, Seoul 110-799, Korea
J Smooth Muscle Res 39:231-47. 2003b>Muscarinic receptors play key roles in the control of gastrointestinal smooth muscle activity. However, specific physiological functions of each subtype remain to be determined...
- Recombinant expression of a selective blocker of M(1) muscarinic receptorsJ Nasman
Department of Physiology, Uppsala University, BMC, Uppsala, S 751 23, Sweden
Biochem Biophys Res Commun 271:435-9. 2000Mamba venoms contain peptides with high selectivity for muscarinic receptors. Due to the limited availability of the M(1) muscarinic receptor-selective MT7 or m1-toxin 1, the peptide was expressed in Sf9 cells using a synthetic cDNA and ..
- Simultaneous modulation of retrieval by dopaminergic D(1), beta-noradrenergic, serotonergic-1A and cholinergic muscarinic receptors in cortical structures of the ratD M Barros
, Centro de Memoria, , Universidade Federal do Rio Grande do Sul, Ramiro Barcellos 2600, 90035-003 Porto Alegre, RS, Brazil
Behav Brain Res 124:1-7. 2001..enzymatic activities are known to be modulated by dopamine D(1), beta-noradrenergic, 5HT1A and cholinergic muscarinic receptors. Here we study the effect on retrieval of this task of well-known agonists and antagonists of these ..
- The relationship between agonist intrinsic activity and the rate of endocytosis of muscarinic receptors in a human neuroblastoma cell lineP G Szekeres
Department of Pharmacology, University of Cambridge, United Kingdom
Mol Pharmacol 53:759-65. 1998..An important implication of this analysis is that extremely weak partial agonists (which may in practice be indistinguishable from antagonists) may produce significant receptor internalization...
- G-protein-gated TRP-like cationic channel activated by muscarinic receptors: effect of potential on single-channel gatingAlexander V Zholos
Laboratory of Molecular Pharmacology of Cellular Receptors and Ion Channels, A A Bogomoletz Institute of Physiology, Kiev, 01024 Ukraine
J Gen Physiol 123:581-98. 2004..1, 3, 24, and 73%) as P(O) increased 525-fold in three stages...
- Spinal alpha(2)-adrenergic and muscarinic receptors and the NO release cascade mediate supraspinally produced effectiveness of gabapentin at decreasing mechanical hypersensitivity in mice after partial nerve injuryKeiko Takasu
Laboratory of CNS Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya 467-8603, Japan
Br J Pharmacol 148:233-44. 2006..on mechanical hypersensitivity involves activation of spinal alpha(2)-adrenergic receptors followed by muscarinic receptors (most likely M(1)) and the NO cascade...
- Both nicotinic and muscarinic receptors in ventral tegmental area contribute to brain-stimulation rewardJ Yeomans
Department of Psychology, University of Toronto, Canada
Pharmacol Biochem Behav 57:915-21. 1997..activate dopamine neurons of the substantia nigra and ventral tegmental area (VTA) via nicotinic and muscarinic receptors. The nicotinic receptors near the VTA have been proposed to be important for nicotine self-administration ..
- Pathways modulating neural KCNQ/M (Kv7) potassium channelsPatrick Delmas
Laboratoire de Neurophysiologie Cellulaire, UMR 6150 CNRS, Faculte de Medecine, IFR Jean Roche, Bd Pierre Dramard, 13916 Marseille Cedex 20, France
Nat Rev Neurosci 6:850-62. 2005..However, until recently, the link between the receptors and the channels has remained elusive. Here, we summarize recent developments that have begun to clarify this link and discuss their implications for physiology and medicine...
- Involvement of M3 muscarinic receptors of the spinal cord in formalin-induced nociception in miceK Honda
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan
Brain Res 859:38-44. 2000..that endogenous ACh in the spinal cord acts as a transmitter anti-nociception, and that ACh release regulated by presynaptic M(3) muscarinic receptors in the spinal cord is involved in the second phase of nociception induced by formalin.
- Coupling of M(2) muscarinic receptors to Src activation in cultured canine colonic smooth muscle cellsCherie A Singer
Department of Pharmacology, University of Nevada School of Medicine, Reno, Nevada 89557 0046, USA
Am J Physiol Gastrointest Liver Physiol 282:G61-8. 2002..Together these results indicate that M(2) receptors are coupled to Src tyrosine kinase and subsequent activation of ERK in cultured CSMC...
- Phosphorylation of serine 916 of Ras-GRF1 contributes to the activation of exchange factor activity by muscarinic receptorsR R Mattingly
Department of Pharmacology, Wayne State University, Program in Molecular Biology and Genetics, Barbara Ann Karmanos Cancer Institute, Detroit, Michigan 48201, USA
J Biol Chem 274:37379-84. 1999..Co-expression of Ras-GRF1 with subtype 1 human muscarinic receptors in COS-7 cells allowed mapping of a carbachol-stimulated phosphorylation site to a region composed of ..
- Interaction of the chiral forms of ketamine with opioid, phencyclidine, sigma and muscarinic receptorsO Hustveit
Department of Pharmacology, University of Oslo, Norway
Pharmacol Toxicol 77:355-9. 1995..the binding of the chiral forms of ketamine to opioid (mu, delta and kappa), phencyclidine, sigma and muscarinic receptors and we have performed detailed concentration-response experiments in the guinea-pig ileum preparation...
- Enhanced cholinergic-mediated increase in the pro-inflammatory cytokine IL-6 in irritable bowel syndrome: role of muscarinic receptorsTimothy G Dinan
Alimentary Pharmabiotic Centre, University College Cork, Cork, Ireland
Am J Gastroenterol 103:2570-6. 2008..We tested the hypothesis that the pro-inflammatory cytokine profile in IBS is driven by the cholinergic system and determined if the responses are mediated by muscarinic receptors.
- Two types of cation channel activated by stimulation of muscarinic receptors in guinea-pig urinary bladder smooth muscleMasayuki Yamamoto
Department of Pathogenic Veterinary Science, United Graduate School of Veterinary Science, Gifu University, Gifu, Japan
J Pharmacol Sci 108:248-57. 2008....
- Muscarinic receptors and ligands in cancerNirish Shah
Division of Gastroenterology and Hepatology, Univ of Maryland School of Medicine, 22 South Greene St, N3W62, Baltimore, MD 21201, USA
Am J Physiol Cell Physiol 296:C221-32. 2009Emerging evidence indicates that muscarinic receptors and ligands play key roles in regulating cellular proliferation and cancer progression...
- Elucidating the role of muscarinic receptors in psychosisC C Felder
Neuroscience Division, Eli Lilly Research Laboratories, Indianapolis, IN 46285, USA
Life Sci 68:2605-13. 2001b>Muscarinic receptors have been implicated in the regulation of cognition and psychosis based on pharmacological evidence from pre-clinical and clinical studies...
- Expression of muscarinic receptors in human and mouse sclera and their role in the regulation of scleral fibroblasts proliferationV A Barathi
Singapore Eye Research Institute, Singapore
Mol Vis 15:1277-93. 2009....
- Muscarinic receptors in psychiatric disorders - can we mimic 'health'?E Scarr
Centre for Neuroscience, The University of Melbourne, and Rebecca L Cooper Research Laboratories, Mental Health Research Institute, Parkville, Vic, Australia
Neurosignals 17:298-310. 2009..New compounds are now being developed that have the potential to selectively target individual muscarinic receptors in the central nervous system...
- M2 muscarinic receptors induce airway smooth muscle activation via a dual, Gbetagamma-mediated inhibition of large conductance Ca2+-activated K+ channel activityXiao Bo Zhou
Institut für Pharmakologie für Pharmazeuten, Universitatsklinikum Hamburg Eppendorf, Martinistrasse 52, Hamburg, Germany
J Biol Chem 283:21036-44. 2008Airway smooth muscle is richly endowed with muscarinic receptors of the M(2) and M(3) subtype...
- Use of knockout mice reveals involvement of M2-muscarinic receptors in control of the kinetics of acetylcholine releaseI Slutsky
The Otto Loewi Minerva Center for Cellular and Molecular Neurobiology, Department of Neurobiology, The Hebrew University, Jerusalem 91904, Israel
J Neurophysiol 89:1954-67. 2003We have previously suggested that presynaptic M(2)-muscarinic receptors (M(2)R) are involved in the control of the time course of evoked acetylcholine release in the frog neuromuscular junction...
- Mediation by M3-muscarinic receptors of both endothelium-dependent contraction and relaxation to acetylcholine in the aorta of the spontaneously hypertensive ratC M Boulanger
Center for Experimental Therapeutics, Baylor College of Medicine, Houston, Texas 77030
Br J Pharmacol 112:519-24. 1994..15 +/- 0.23 and 9.63 +/- 0.28, respectively. These results suggest that the muscarinic M3 receptor subtype mediates both endothelium-dependent relaxation and contraction to acetylcholine in SHR aorta...
- Altered hippocampal muscarinic receptors in acetylcholinesterase-deficient miceLaura A Volpicelli-Daley
Center for Neurodegenerative Disease and Department of Neurology, Emory University School of Medicine, Atlanta, GA 30322, USA
Ann Neurol 53:788-96. 2003..The alterations of mAChRs in AChE -/- mice suggest that mAChR downregulation may contribute to the limited efficacy of AChE inhibitors in Alzheimer's disease treatment...
- Impaired modulation of GABAergic transmission by muscarinic receptors in a mouse transgenic model of Alzheimer's diseasePing Zhong
Department of Physiology and Biophysics, State University of New York at Buffalo, School of Medicine and Biomedical Sciences, Buffalo, New York 14214, USA
J Biol Chem 278:26888-96. 2003..These results show that the muscarinic regulation of GABA transmission is impaired in the AD model, probably due to the Abeta-mediated interference of mAChR activation of PKC...
- Evidence that M1 muscarinic receptors enhance noradrenaline release in mouse atria by activating protein kinase CM Costa
Prince Henry s Institute of Medical Research, Clayton, Victoria, Australia
Br J Pharmacol 110:910-6. 1993..This has been found previously to be due to activation of muscarinic receptors of the M1 subtype, probably located on sympathetic nerve terminals...
- Cooperativity manifest in the binding properties of purified cardiac muscarinic receptorsK A Wreggett
Faculty of Pharmacy, University of Toronto, Ontario, Canada
J Biol Chem 270:22488-99. 1995b>Muscarinic receptors were solubilized from porcine atria in digitonin-cholate and were purified by chromatography on DEAE-Sepharose and 3-(2'-aminobenzhydryloxy)tropane-Sepharose...
- Role of muscarinic receptors in the regulation of immune and inflammatory responsesSeddigheh Razani-Boroujerdi
Immunology Program, Lovelace Respiratory Research Institute, 2425 Ridgecrest Dr SE, Albuquerque, NM 87108, United States
J Neuroimmunol 194:83-8. 2008Leukocytes contain both nicotinic and muscarinic receptors, and while activation of nicotinic receptors suppresses immune/inflammatory responses, the role of muscarinic receptors in immunity is unclear...
- Motor activity-induced dopamine release in the substantia nigra is regulated by muscarinic receptorsDaniel R Andersson
Department of Pharmacology, Institute of Neuroscience and Physiology, the Sahlgrenska Academy at University of Gothenburg, Goteborg, Sweden
Exp Neurol 221:251-9. 2010....
- Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implicationsJurgen Wess
Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, DHHS, Bethesda, Maryland 20892, USA
Annu Rev Pharmacol Toxicol 44:423-50. 2004..The novel insights gained from these studies should prove instrumental for the development of novel classes of muscarinic drugs...
- Regulation of muscarinic cationic current in myocytes from guinea-pig ileum by intracellular Ca2+ release: a central role of inositol 1,4,5-trisphosphate receptorsD V Gordienko
Department of Basic Medical Sciences Pharmacology, St George s Hospital Medical School, Cranmer Terrace, London SW17 0RE, UK
Cell Calcium 36:367-86. 2004....
- Effects of muscarinic cholinergic receptor antagonists on postnatal eye growth of rhesus monkeysM Tigges
Yerkes Regional Primate Research Center, Department of Ophthalmology, Emory University, Atlanta, Georgia 30322, USA
Optom Vis Sci 76:397-407. 1999To study a potential role for muscarinic receptors in the inhibition of deprivation-induced excessive axial elongation and myopia in a monkey model.
- Cholinergic activity modulates the survival of retinal ganglion cells in culture: the role of M1 muscarinic receptorsS P Pereira
Departamento de Neurobiologia, Programa de Neuroimunologia, Instituto de Biologia, Universidade Federal Fluminense, Caixa Postal 100180, 24001-970, RJ, , Brazil
Int J Dev Neurosci 19:559-67. 2001..Taken together our results indicate that muscarinic activity controls the survival of retinal ganglion cells through a mechanism involving the release of polypeptides and activation of Irk receptors...
- Presence of nerves and their receptors in mouse and human conjunctival goblet cellsY Diebold
Schepens Eye Research Institute, Department of Ophthalmology, Harvard Medical School, Boston, Massachusetts 02114, USA
Invest Ophthalmol Vis Sci 42:2270-82. 2001..RESULTS: Western blot demonstrated PGP 9.5, M(1), M(2), and M(3) muscarinic receptors and alpha(1A)-, beta(1)-, beta(2)-, and beta(3)-adrenergic receptors in mouse conjunctiva...
- Increased function of inhibitory neuronal M2 muscarinic receptors in trachea and ileum of diabetic ratsFiona R Coulson
Division of Physiology, Department of Environmental Health Sciences, Bloomberg School of Public Health, Johns Hopkins University, Baltimore, Maryland, MD 21205, USA
Br J Pharmacol 135:1355-62. 20021. Release of acetylcholine from parasympathetic nerves is inhibited by neuronal M(2) muscarinic receptors. The effects of streptozotocin-induced diabetes on prejunctional M(2) and postjunctional M(3) muscarinic receptor function in rat ..
- Differential modulation of CaV2.3 Ca2+ channels by Galphaq/11-coupled muscarinic receptorsR A Bannister
Department of Biology, Utah State University, Logan, Utah 84322, USA
Mol Pharmacol 65:381-8. 2004..In the present study, we compared modulation of CaV2.3 by the three Galphaq/11-coupled muscarinic receptors (M1, M3, and M5). Our data indicate that these receptors trigger comparable stimulation of CaV2.3...
- Role of sorbitol in the up-regulation of urinary bladder M(2) muscarinic receptors in streptozotocin-induced diabetic ratsYat-Ching Tong
Department of Urology, College of Medicine, National Cheng Kung University, Tainan, Taiwan, ROC
Neurourol Urodyn 21:154-9. 2002..The findings suggest that sorbitol plays a role in the pathogenesis of diabetic cystopathy in rats rendered diabetic by streptozotocin. Aldose reductase inhibitors may be useful in the treatment and prevention of diabetic cystopathy...
- Muscarinic receptors in basal ganglia in dementia with Lewy bodies, Parkinson's disease and Alzheimer's diseaseMargaret A Piggott
MRC University of Newcastle Centre in Clinical Brain Ageing, MRC Building, Newcastle General Hospital, Westgate Road, NE4 6BE, Newcastle upon Tyne, UK
J Chem Neuroanat 25:161-73. 2003..QNB), particularly [123I]-(R,R)-I-QNB, are currently being assessed as in vivo ligands to monitor muscarinic receptors in Alzheimer's disease (AD) and dementia with Lewy bodies (DLB), relating changes to disease symptoms and ..
- The presence and functions of muscarinic receptors in human T cells: the involvement in IL-2 and IL-2 receptor systemJun Nomura
Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo 060-0812, Japan
Life Sci 72:2121-6. 2003..Oxo-M stimulated IL-2 receptor mRNA expression and DNA synthesis. Our results suggest that muscarinic receptors, perhaps M(1) receptors are involved in the enhancement of TCR-induced IL-2 production and IL-2 receptor ..
- Acetylcholine affects rat liver metabolism via type 3 muscarinic receptors in hepatocytesM Z Vatamaniuk
Biochemistry and Biophysics Department, University of Pennsylvania, 501 Stemmler Hall, 36th and Hamilton Walk, Philadelphia, PA 19104, USA
Life Sci 72:1871-82. 2003..Elimination of the described effects of Ach by atropine, the antagonist of muscarinic receptors, and identification of the type 3 muscarinic receptors (m3) in isolated hepatocytes as well as in whole ..
- Competitive and allosteric interactions of 6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)acetyl]-11H-di benzo[b,e][1, 4]diazepine-11-one hydrochloride (UH-AH 37) at muscarinic receptors, via distinct epitopesJ Ellis
Department of Psychiatry, The Pennsylvania State University College of Medicine, Hershey 17033, USA
Biochem Pharmacol 57:181-6. 1999..The present study was carried out with wild-type and chimeric muscarinic receptors to determine whether UH-AH 37 might also have an allosteric mode of action...
- Comparative pharmacology of recombinant human M3 and M5 muscarinic receptors expressed in CHO-K1 cellsN Watson
Urogenital Pharmacology, Center for Biological Research, Neurobiology Unit, Roche Bioscience, Palo Alto, California 94304, USA
Br J Pharmacol 127:590-6. 1999..Collectively, these data show that in the absence of a high affinity M5 selective antagonist, affinity data for a large range of antagonists is critical to define operationally the M5 receptor subtype...
- Primary structure and functional expression of a rat G-protein-coupled muscarinic potassium channelY Kubo
Howard Hughes Medical Institute, University of California, San Francisco 94143 0724
Nature 364:802-6. 1993Parasympathetic nerve stimulation causes slowing of the heart rate by activation of muscarinic receptors and the subsequent opening of muscarinic K+ channels in the sinoatrial node and atrium...
- Conversion of N-(2-chloroethyl)-4-piperidinyl diphenylacetate (4-DAMP mustard) to an aziridinium ion and its interaction with muscarinic receptors in various tissuesE A Thomas
Department of Pharmacology, College of Medicine, University of California, Irvine 92717
Mol Pharmacol 41:718-26. 1992..diphenylacetate (4-DAMP) was synthesized, and its conversion to an aziridinium ion and interaction with muscarinic receptors was investigated. When dissolved in aqueous solution at pH 7...
- Acetylcholine modulates cortical synaptic transmission via different muscarinic receptors, as studied with receptor knockout miceNicola Kuczewski
Cognitive Neuroscience Sector, International School for Advanced Studies SISSA, Via Beirut 2 4, 34014 Trieste, Italy
J Physiol 566:907-19. 2005..The present data suggest that local ACh, acting through mAChRs, regulates the cortical dynamics making cortical circuits respond to specific stimuli...
- Muscarinic acetylcholine receptor knockout mice show distinct synaptic plasticity impairments in the visual cortexNicola Origlia
Institute of Neuroscience (CNR, 56100 Pisa, Italy
J Physiol 577:829-40. 2006..Our results indicate that different mAChR subtypes regulate different forms of long-term synaptic plasticity in the mouse visual cortex, activating specific G proteins and downstream intracellular mechanisms...
- Modulation of neuritogenesis by astrocyte muscarinic receptorsMarina Guizzetti
Department of Environmental and Occupational Health Sciences, University of Washington, Seattle, Washington 98105, USA
J Biol Chem 283:31884-97. 2008..Astrocytes express muscarinic receptors whose activation stimulates a robust intracellular signaling, although the role of these receptors in glial ..
- Does phospholipase C mediate muscarinic receptor-induced rat urinary bladder contraction?Elfaridah P Frazier
Department of Pharmacology and Pharmacotherapy, University of Amsterdam, The Netherlands
J Pharmacol Exp Ther 322:998-1002. 2007..We conclude that previously reported differences relate to the use of inhibitors rather than experimental protocols and that the overall data do not support a role for PLC in M(3) muscarinic receptor-mediated rat bladder contraction...
- Both endogenous and exogenous ACh plays antinociceptive role in the hippocampus CA1 of ratsX F Yang
Department of Physiology, Harbin Medical University, Harbin, China
J Neural Transm 115:1-6. 2008..5 microg/1 microl) produced opposite response. On the basis of the above findings, we can deduce that ACh and mAChRs are involved in the modulation of nociceptive information transmission in the hippocampal CA1...
- Effects of imidafenacin (KRP-197/ONO-8025), a new anti-cholinergic agent, on muscarinic acetylcholine receptors. High affinities for M3 and M1 receptor subtypes and selectivity for urinary bladder over salivary glandFumiyoshi Kobayashi
Research Department I, Research Center, Kyorin Pharmaceutical Co, Ltd, Tochigi, Japan
Arzneimittelforschung 57:92-100. 2007..Therefore, imidafenacin will have higher affinities for M3 and M1 receptors and higher selectivity for the urinary bladder than for the salivary gland...
- 6beta-acetoxy nortropane regulated processing of amyloid precursor protein in CHOm1 cells and rat brainYu Qiu
Department of Pharmacology, Drug Research Institute, Shanghai Second Medical University, Shanghai 200025, China
Eur J Pharmacol 468:1-8. 2003..These results suggest that 6beta-acetoxy nortropane could exert a beneficial effect on the progress of Alzheimer's disease by promoting amyloid precursor protein processing through alpha-secretase...
- Aging-induced decrease of cholinergic response and calcium sensitivity on rat jejunum contractionsGuiomar Silva Lopes
Department of Pharmacology, Federal University of Sao Paulo, Sao Paulo, Brazil
J Gerontol A Biol Sci Med Sci 62:264-70. 2007..Changes were not detected for relaxation by adrenergic agonists. In conclusion, aging caused a decrease of MCh potency, which is probably related to the reduction of calcium sensitivity in jejunum...
- Expression of muscarinic acetylcholine receptors (M1-, M2-, M3- and M4-type) in the neuromuscular junction of the newborn and adult ratN Garcia
Histology and Neurobiology Unit, Faculty of Medicine and Health Sciences, Rovira i Virgili University, , 43201 Reus, Spain
Histol Histopathol 20:733-43. 2005..the presence of these receptors in the motor endplates and conclude that M1-, M2-, M3- and M4-type muscarinic receptors are present in all the neuromuscular junctions of the rat muscle both in newborn and adult animals...
- Distinct pathways of ERK activation by the muscarinic agonists pilocarpine and carbachol in a human salivary cell lineAlan L Lin
Department of Dental Diagnostic Science, University of Texas Health Science Center, San Antonio, TX, USA
Am J Physiol Cell Physiol 294:C1454-64. 2008....
- A muscarinic cholinergic mechanism underlies activation of the central pattern generator for locust flightEdgar Buhl
University of Leipzig, Institute of Biology II, Talstr 33, 04103 Leipzig, Germany
J Exp Biol 211:2346-57. 2008..We conclude that acetylcholine acting via muscarinic receptors is the key neurotransmitter in the mechanism underlying the natural activation of the locust flight CPG...
- Role of Na+/H+ exchanger in acetylcholine-mediated pulmonary artery contraction of spontaneously hypertensive ratsWing Han Chau
School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, PR China
Eur J Pharmacol 464:177-87. 2003....
- Role of muscarinic receptors in the activation of the ventral subiculum and the consequences for dopamine release in the nucleus accumbensSarah Moss
Eli Lilly and Company Ltd, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK
Eur J Pharmacol 460:117-25. 2003..of the ventral subiculum by carbachol increases dopamine efflux in the nucleus accumbens by stimulation of muscarinic receptors, and that the ventral subiculum-nucleus accumbens projection system is sensitive to muscarinic M(2)/M(4) ..
- Modulation of ACh release by presynaptic muscarinic autoreceptors in the neuromuscular junction of the newborn and adult ratManel M Santafe
Unitat d Histologia i Neurobiologia UHN Facultat de Medicina i Ciències de la Salut, Universitat Rovira i Virgili, carrer St Llorenç num 21, 43201 Reus, Spain
Eur J Neurosci 17:119-27. 2003..We show that the way in which M1 and M2 muscarinic receptors modulate neurotransmission can differ between the developing and adult rat neuromuscular synapse.
- Low concentrations of pyridostigmine prevent soman-induced inhibition of GABAergic transmission in the central nervous system: involvement of muscarinic receptorsMariton D Santos
Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, Baltimore, Maryland 21201, USA
J Pharmacol Exp Ther 304:254-65. 2003..Therefore, PB, acting via m3 receptors, can effectively counteract effects arising from the interactions of soman with m2 receptors in the brain...
- PMA decreases the proliferation of retinal cells in vitro: the involvement of acetylcholine and BDNFAline Araujo dos Santos
Programa de Neuroimunologia, Departamento de Neurobiologia, Instituto de Biologia, Centro de Estudos Gerais, Universidade Federal Fluminense, , Rio de Janeiro 24001-970, Brazil
Neurochem Int 42:73-80. 2003..Our results suggest that PKC activation leads to a decrease in retinal cells proliferation through the release of acetylcholine and brain derived neurotrophic factor in the culture, and activation of M1 and TrkB receptors, respectively...
- Subtype-specific regulation of the expression and function of muscarinic acetylcholine receptors in embryonic chicken retinal cellsJuan C Goin
Department of Pharmacology, University of Washington School of Medicine, Seattle, Washington 98195, USA
J Neurochem 83:964-72. 2002..These data demonstrate subtype-specific regulation of the expression and function of muscarinic receptors in the retina.
- Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonistKunrong Cheng
Division of Gastroenterology and Hepatology, Central Arkansas Veterans Healthcare System and University of Arkansas for Medical Sciences, Little Rock, USA
J Pharmacol Exp Ther 303:29-35. 2002..work from our laboratory indicates that bile acids, specifically lithocholic acid conjugates, interact with muscarinic receptors on gastric chief cells...
- Muscarinic and nicotinic responses in the developing pedunculopontine nucleus (PPN)Cameron H Good
Center for Translational Neuroscience, Department of Neurobiology and Developmental Sciences, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, AR 72205 7199, USA
Brain Res 1129:147-55. 2007..We conclude that, while the nicotinic inputs to the PPN may help modulate the developmental decrease in REM sleep, the muscarinic inputs appear to modulate different types of cells differentially...
- Nicotinic enhancement of the noradrenergic inhibition of sleep-promoting neurons in the ventrolateral preoptic areaBenoît Saint-Mleux
Departement de Physiologie, Centre Medical Universitaire, 1211 Geneva 4, Switzerland
J Neurosci 24:63-7. 2004..Such dual complementary actions allow ACh and nicotine to enhance wakefulness by inhibiting sleep-promoting systems while facilitating other wake-promoting systems...
- Regulation of glutamate release from primary afferents and interneurons in the spinal cord by muscarinic receptor subtypesHong Mei Zhang
Department of Anesthesiology and Pain Medicine, The University of Texas M D Anderson Cancer Center, 1400 Holcombe Blvd, Unit 409, Houston, TX 77030, USA
J Neurophysiol 97:102-9. 2007..The M(3) and M(2)/M(4) subtypes on a subpopulation of interneurons are important for regulation of glutamate release from interneurons in the spinal dorsal horn...
- Characterization of functional effects of Z-338, a novel gastroprokinetic agent, on the muscarinic M1, M2, and M3 receptors expressed in Xenopus oocytesY Doi
Department of Pharmacology Nagasaki University Graduate School of Biomedical Sciences, 1-12-4 Sakamoto, Nagasaki 852-8523, Japan
Eur J Pharmacol 505:31-5. 2004..These results indicate that Z-338 is a potent antagonist not for muscarinic M3 receptor but for both muscarinic M1 and M2 receptors. Thus, Z-338 is a gastrokinetic agent with a unique profile...
- Opposing muscarinic and nicotinic modulation of hypoglossal motor output to genioglossus muscle in rats in vivoXia Liu
Department of Medicine, University of Toronto, Ontario, Canada, M5S 1A8
J Physiol 565:965-80. 2005..The results suggest that acetylcholine has mixed effects at the HMN with muscarinic-mediated GG suppression masking nicotinic excitation...
- Differential modulation by carbachol of four separate excitatory afferent systems to the rat subiculum in vitroAyumi Kunitake
Department of Physiology and Pharmacology, State University of New York, Downstate Medical Center, Brooklyn, New York 11203, USA
Hippocampus 14:986-99. 2004....
- Differential effects on [35S]GTPgammaS binding using muscarinic agonists and antagonists in the gerbil brainFuencisla Pilar-Cuéllar
Dpto Biología Celular, Facultad de Ciencias Biologicas y Ambientales, Campus de Vegazana s n, Universidad de Leon, Spain
J Chem Neuroanat 30:119-28. 2005..OXO and Cch suggested that OXO is able to detect differences in the response of structures enriched in M(4) muscarinic receptors, showing a lower potency to stimulate these brain areas...
- Preparation and biological effects of pure stereoisomeric novel soft anticholinergicsE Tóth-Sarudy
IVAX Drug Research Institute Ltd, Budapest, Hungary
Pharmazie 61:90-6. 2006..In vitro isolated organ experiments correlated well with the receptor binding results, and in vivo investigations indicated the soft character of the compounds...
- Cholinergic regulation of the evoked quantal release at frog neuromuscular junctionEugeny E Nikolsky
Institute of Biochemistry and Biophysics, Russian Academy of Sciences, Kazan, Russia
J Physiol 560:77-88. 2004..It follows that the mechanisms regulating the amount and the time course of transmitter release are different and that, among other factors, they are altered by presynaptic nicotinic receptors...
- Activation of muscarinic acetylcholine receptors elicits pigment granule dispersion in retinal pigment epithelium isolated from bluegillAlfredo Gonzalez
Department of Biology, Texas State University San Marcos, Texas 78666, USA
BMC Neurosci 5:23. 2004..Acetylcholine receptors are of two main types, nicotinic and muscarinic. Muscarinic receptors are in the G-protein coupled receptor superfamily, and five different muscarinic receptors have been ..
- Nicotinic and muscarinic acetylcholine receptors are essential for the long-term response of tyrosine hydroxylase gene expression to chronic nicotine treatment in rat adrenal medullaReiji Yoshimura
Department of Pharmacology and Physiology, University of Rochester Medical Center, P.O. Box 711, 601 Elmwood Avenue, Rochester, NY 14642, USA
Brain Res Mol Brain Res 126:188-97. 2004..The results also suggest that both transcriptional and post-transcriptional mechanisms may potentially need to be regulated to induce TH protein in response to some stimuli...
- Intraseptal muscarinic ligands and galanin: influence on hippocampal acetylcholine and cognitionE Elvander
Department of Neuroscience, Division of Behavioral Neuroscience, Karolinska Institutet, , SE-171 77 Stockholm, Sweden
Neuroscience 126:541-57. 2004..Stimulation of septal muscarinic receptors by carbachol also increased hippocampal ACh release...
- Evoked slow muscarinic acetylcholinergic synaptic potentials in rat hippocampal interneuronsH Widmer
Division of Neuroscience and Biomedical Systems, IBLS, University of Glasgow, Glasgow, United Kingdom
Hippocampus 16:617-28. 2006..The current study suggests that synaptic release of ACh results in a complex and differential mAChR-mediated modulation of cellular excitability within the hippocampal interneuron population...
- Effect of estrogen on muscarinic acetylcholine receptor expression in rat myometriumFernando M F Abdalla
Laboratory of Pharmacology, Instituto Butantan, Sao Paulo, SP, Brazil
Mol Cell Endocrinol 213:139-48. 2004..In conclusion, these results provide evidence for the presence of M(2)- and M(3)-mAChR, at the mRNA and protein level, in the rat myometrium and indicate that estrogen induces an increase in myometrial responsiveness to mAChR agonists...
- Muscarinic cholinoceptor activation modulates DNA synthesis and CD40 expression in fibroblast cellsM Casanova
Argentine National Research Council (CONICET, Buenos Aires, Argentina
Auton Autacoid Pharmacol 26:293-301. 2006..4 These results may contribute to a better understanding of the modulatory role of the parasympathetic muscarinic system on normal human fibroblast function...
- Muscarinic receptor function, density and G-protein coupling in the overactive diabetic rat bladderL A Stevens
Biomedical Research Centre, Sheffield Hallam University, Sheffield S1 1WB, UK
Auton Autacoid Pharmacol 26:303-9. 2006..The overactivity is associated with an enhanced sensitivity to carbachol, which is partly explained by an increase in receptor density, but there appears to be no change in receptor/G-protein coupling...
- The use of the isolated mouse whole bladder for investigating bladder overactivityAdebola C Fabiyi
Oxford Continence Group, University Department of Pharmacology, University of Oxford, UK
J Pharmacol Exp Ther 319:1386-94. 2006..The isolated mouse whole bladder has proved a viable, robust model in which to demonstrate the pharmacological characteristic of the bladder and adds to the repertoire of in vitro tools for investigating potential therapeutic agents...
- Selective antagonism activity of alkaloids from bulbs Fritillariae at muscarinic receptors: functional studiesBao qin Lin
Key Laboratory of Modern Chinese Medicines, Ministry of Education of PRC and Department of Pharmacognosy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, PR China
Eur J Pharmacol 551:125-30. 2006....
- Antimuscarinic agents exhibit local inhibitory effects on muscarinic receptors in bladder-afferent pathwaysYongTae Kim
Department of Urology, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania 15213, USA
Urology 65:238-42. 2005..To investigate the potential of antimuscarinic agents for sensory mechanisms in overactive bladder using intravesical instillation...
- Interaction between muscarinic receptor subtype signal transduction pathways mediating bladder contractionAlan S Braverman
Department of Urology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
Am J Physiol Regul Integr Comp Physiol 283:R663-8. 2002M(3) muscarinic receptors mediate cholinergic-induced contraction in most smooth muscles...
- Muscarinic signalling affects intracellular calcium concentration during the first cell cycle of sea urchin embryosP K Harrison
Department of Physiological Sciences, Medical School, University of Newcastle upon Tyne, UK
Cell Calcium 31:289-97. 2002..The hypothesis is proposed that muscarinic receptors may be involved in the (presumably Ca(2+)-dependent) modulation of the nuclear status during the first cell ..
- Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-aminesR Budriesi
Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
Br J Pharmacol 132:1009-16. 2001..27+/-0.09 (spirotramine) and 8.51+/-0.02 (AM170). Competition radioligand binding studies, using native muscarinic receptors from rat tissues (M(1), cortex; M(2), heart; M(3), submaxillary gland) or from NG 108-15 cells (M(4)) and ..
- Cortico-hippocampal APP and NGF levels are dynamically altered by cholinergic muscarinic antagonist or M1 agonist treatment in normal miceHyemyung Seo
Neuroregeneration Laboratories, Harvard Medical School, McLean Hospital, 115 Mill Street, Belmont, MA 02478, USA
Eur J Neurosci 15:498-506. 2002....
- Acetylcholine release in human heart atrium: influence of muscarinic autoreceptors, diabetes, and ageV Oberhauser
, Innere Medizin IV, Freiburg, Germany
Circulation 103:1638-43. 2001..Locally impaired cardiac acetylcholine release may therefore represent a pathophysiological link to sudden cardiac death in elderly and diabetic patients...
- Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypesYufu Sagara
Banyu Tsukuba Research Institute, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan
J Med Chem 45:984-7. 2002..Compound 14a showed high selectivity for M(3) receptors over the other muscarinic receptor subtypes (M(1)/M(3) = 380-fold, M(2)/M(3) = 98-fold, M(4)/M(3) = 45-fold, M(5)/M(3) = 120-fold)...
- Role of M3 muscarinic receptors in bile acid-induced colon cancerJean Pierre Raufman; Fiscal Year: 2010..present line of investigation was initiated by our unanticipated observation that bile acids interact with muscarinic receptors. M3 muscarinic receptors (M3R), which are over-expressed in most colon cancers, are key players in colon ..
- Role of Sterols and Insulin in Cardiac Autonomic ResponseJONAS BERNARD GALPER; Fiscal Year: 2010....
- REGULATION OF GLANDULAR MUCOUS CELL SECRETIONDAVID CULP; Fiscal Year: 2001..Given the importance of mucins in protection of the oral cavity and the primary role of muscarinic receptors in eliciting mucous cell secretion, studies are proposed to determine the regulation by agonist of ..
- GENETICS OF NEMATODE PHARYNGEAL MUSCLE EXCITABILITYLeon Avery; Fiscal Year: 2003..We will measure the effect of acetylcholine agonists specific for nicotinic or muscarinic receptors on myogenic activity (hypothesis 4)...
- Next Generation Oxime Therapeutic for Chemical Agent Inhibited CNS (Brain) ChEsRichard Gordon; Fiscal Year: 2007....
- Bile acid-induced colon cancer cell proliferationJean Pierre Raufman; Fiscal Year: 2009..be tested in this proposal is that bile acids induce colon cancer cell proliferation by interaction with M3 muscarinic receptors (M3R), thereby causing transactivation of epidermal growth factor receptors (EGFR)...
- Role of M3 muscarinic receptors in bile acid-induced colon cancerJean Pierre Raufman; Fiscal Year: 2009..present line of investigation was initiated by our unanticipated observation that bile acids interact with muscarinic receptors. M3 muscarinic receptors (M3R), which are over-expressed in most colon cancers, are key players in colon ..
- Neuromuscular blocker-induced asthma during anesthesiaCharles Emala; Fiscal Year: 2006..During intubation of the trachea, parasympathetic nerves release acetylcholine that act on M3 muscarinic receptors on airway smooth muscle to promote bronchoconstriction...
- M1 and M4 mAChRs in striatum-implication in treatment of movement disordersZixiu Xiang; Fiscal Year: 2010....
- Canonical Transient Receptor Potential (TRPC) subfamily function in Hippocampus.David E Clapham; Fiscal Year: 2010..In particular, Gq/11-linked receptors such as the type 1 metabotropic glutamate and M1, M3, and M5 muscarinic receptors, activate these currents by altering plasma membrane PIP2 and increasing intracellular Ca2+ concentrations...
- MUSCARINIC RECEPTOR SUBTYPES ON CULTURED CELLST Harden; Fiscal Year: 1991..Rational therapy of a number of pathophysiological conditions, e.g. Alzheimer's disease, can ultimately benefit from this knowledge...
- Interaction of RGS Protein with G beta subunit G beta 5.Vladlen Z Slepak; Fiscal Year: 2010..A family of GPCRs that mediates the action of acetylcholine includes five members called muscarinic receptors (M1R-M5R)...
- XENIN-25: NOVEL REGULATOR OF INSULIN SECRETION AND B-CELL FUNCTIONBurton M Wice; Fiscal Year: 2010..but stimulates acetylcholine release from cholinergic neurons that innervate the islets thereby activating muscarinic receptors on the pancreatic -cell...
- MUSCARINIC RECEPTOR COUPLING TO INOSITIDES IN CNSStephen Fisher; Fiscal Year: 2006..Accordingly, knowledge of the signal transduction pathways that regulate VSOAC is an essential prerequisite for the rational design of therapeutic agents. ..
- CHOLINERGIC MECHANISMS IN AGING AND ALZHEIMER'S DISEASELINCOLN POTTER; Fiscal Year: 1993..Novel morphological data should be obtained for AD and PD, and these data should provide a good basis for physiological work with the toxin, and for understanding which cells are most likely to be controllable with muscarinic ligands...
- GALLBLADDER MUSCARINIC RECEPTORS IN ACUTE CHOLECYSTITISStuart Myers; Fiscal Year: 2001..The results from the proposed studies will identify future studies on ways to prevent the motor dysfunction that occurs with gallbladder inflammation. ..
- MODULATION OF MUSCARINIC RESPONSES BY INOSITOL LIPIDSESAM EL FAKAHANY; Fiscal Year: 1991..Activation of muscarinic receptors in mouse neuroblastoma cells results in Ca2+ release and cyclic GMP formation; with the latter response ..