muscarinic agonists

Summary

Summary: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.

Top Publications

  1. ncbi Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implications
    Jurgen 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
  2. ncbi New insights from the use of pilocarpine and kainate models
    J P Leite
    Department of Neurology, University of São Paulo School of Medicine at Ribeirão Preto, Campus Universitario, Ribeirao Preto, Brazil
    Epilepsy Res 50:93-103. 2002
  3. ncbi AKAP150 signaling complex promotes suppression of the M-current by muscarinic agonists
    Naoto Hoshi
    Department of Biophysical Genetics, Kanazawa University Graduate School of Medicine, 13 1 Takara machi, Kanazawa, Ishikawa 920 8640, Japan
    Nat Neurosci 6:564-71. 2003
  4. ncbi Muscarine reduces calcium-dependent electrical activity in substantia nigra dopaminergic neurons
    R S Scroggs
    Department of Anatomy and Neurobiology, Health Science Center, University of Tennessee, Memphis, Tennessee 38163, USA
    J Neurophysiol 86:2966-72. 2001
  5. ncbi 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 assay
    N W Delapp
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
    J Pharmacol Exp Ther 289:946-55. 1999
  6. ncbi Origin of spontaneous activity in neonatal and adult rat bladders and its enhancement by stretch and muscarinic agonists
    A Kanai
    Department of Medicine, University of Pittsburgh School of Medicine, A1224 Scaife Hall, Pittsburgh, PA 15261, USA
    Am J Physiol Renal Physiol 292:F1065-72. 2007
  7. ncbi Cholinergic inhibition of neocortical pyramidal neurons
    Allan T Gulledge
    Division of Neuroscience, John Curtin School of Medical Research, Australian National University, Canberra, Australia
    J Neurosci 25:10308-20. 2005
  8. ncbi Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor
    Carl P Nelson
    Department of Cell Physiology and Pharmacology, University of Leicester, University Road, Leicester LE1 9HN, UK
    J Pharmacol Exp Ther 316:279-88. 2006
  9. ncbi The effects of tertiapin-Q on responses of the sinoatrial pacemaker of the guinea-pig heart to vagal nerve stimulation and muscarinic agonists
    Chris P Bolter
    Department of Physiology, School of Medical Sciences, University of Otago, PO Box 913, Dunedin 9054, New Zealand
    Exp Physiol 93:53-63. 2008
  10. ncbi The M2 muscarinic receptor mediates contraction through indirect mechanisms in mouse urinary bladder
    Frederick J Ehlert
    Department of Pharmacology, College of Medicine, University of California Irvine, Irvine, CA 92697 4625, USA
    J Pharmacol Exp Ther 313:368-78. 2005

Research Grants

  1. Efficacy of GluR5 Antogonists Against Soman-Induced Seizures and Neuropathology
    MARIA BRAGA; Fiscal Year: 2007
  2. Atypical Antipsychotics: Effects on Hepatic Glucose and Lipid Metabolism in Human
    Karen Teff; Fiscal Year: 2009
  3. Atypical Antipsychotics: Effects on Hepatic Glucose and Lipid Metabolism in Human
    Karen L Teff; Fiscal Year: 2010
  4. REGULATION OF GLANDULAR MUCOUS CELL SECRETION
    DAVID CULP; Fiscal Year: 2001
  5. CELLULAR AND MOLECULAR STUDIES OF VESTIBULAR HAIR CELLS
    MANNING CORREIA; Fiscal Year: 2007
  6. The neurogenic potential of cholinergic activation in AD.
    Elizabeth Eckman; Fiscal Year: 2009
  7. The neurogenic potential of cholinergic activation in AD.
    ELIZABETH ADAMS ECKMAN; Fiscal Year: 2010
  8. EFFECTS OF LITHIUM ON CHOLINERGIC ACTIVITY
    RICHARD JOPE; Fiscal Year: 1990
  9. CHOLINERGIC MECHANISMS IN AGING AND AD
    LINCOLN POTTER; Fiscal Year: 2002
  10. Regulation of Airway Goblet Cell Mucin Secretion
    C Davis; Fiscal Year: 2007

Detail Information

Publications267 found, 100 shown here

  1. ncbi Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implications
    Jurgen 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...
  2. ncbi New insights from the use of pilocarpine and kainate models
    J P Leite
    Department of Neurology, University of São Paulo School of Medicine at Ribeirão Preto, Campus Universitario, Ribeirao Preto, Brazil
    Epilepsy Res 50:93-103. 2002
    ..Most of current tools used to quantify spontaneous seizure events need to be coupled to electrophysiology and more sophisticated systems for recording and analyzing behavior...
  3. ncbi AKAP150 signaling complex promotes suppression of the M-current by muscarinic agonists
    Naoto Hoshi
    Department of Biophysical Genetics, Kanazawa University Graduate School of Medicine, 13 1 Takara machi, Kanazawa, Ishikawa 920 8640, Japan
    Nat Neurosci 6:564-71. 2003
    ..These inhibitors also reduced muscarinic inhibition of M-current. Our data indicate that AKAP150-bound PKC participates in receptor-induced inhibition of the M-current...
  4. ncbi Muscarine reduces calcium-dependent electrical activity in substantia nigra dopaminergic neurons
    R S Scroggs
    Department of Anatomy and Neurobiology, Health Science Center, University of Tennessee, Memphis, Tennessee 38163, USA
    J Neurophysiol 86:2966-72. 2001
    ....
  5. ncbi 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 assay
    N 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...
  6. ncbi Origin of spontaneous activity in neonatal and adult rat bladders and its enhancement by stretch and muscarinic agonists
    A Kanai
    Department of Medicine, University of Pittsburgh School of Medicine, A1224 Scaife Hall, Pittsburgh, PA 15261, USA
    Am J Physiol Renal Physiol 292:F1065-72. 2007
    ..the origin of spontaneous activity in neonatal and adult rat bladders and the effect of stretch and muscarinic agonists and antagonists on spontaneous activity...
  7. ncbi Cholinergic inhibition of neocortical pyramidal neurons
    Allan T Gulledge
    Division of Neuroscience, John Curtin School of Medical Research, Australian National University, Canberra, Australia
    J Neurosci 25:10308-20. 2005
    ..These data demonstrate that acetylcholine can directly inhibit the output of neocortical pyramidal neurons...
  8. ncbi Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor
    Carl P Nelson
    Department of Cell Physiology and Pharmacology, University of Leicester, University Road, Leicester LE1 9HN, UK
    J Pharmacol Exp Ther 316:279-88. 2006
    ..This indicates that the N410Y mutation of the M(2) mACh receptor alters receptor-G-protein coupling in an agonist-dependent manner, in addition to generating a constitutively active receptor phenotype...
  9. ncbi The effects of tertiapin-Q on responses of the sinoatrial pacemaker of the guinea-pig heart to vagal nerve stimulation and muscarinic agonists
    Chris P Bolter
    Department of Physiology, School of Medical Sciences, University of Otago, PO Box 913, Dunedin 9054, New Zealand
    Exp Physiol 93:53-63. 2008
    ..IK,ACh, in the bradycardia produced by electrical stimulation of the vagus (parasympathetic) nerve and muscarinic agonists (ACh and bethanecol, bolus i.a.)...
  10. ncbi The M2 muscarinic receptor mediates contraction through indirect mechanisms in mouse urinary bladder
    Frederick J Ehlert
    Department of Pharmacology, College of Medicine, University of California Irvine, Irvine, CA 92697 4625, USA
    J Pharmacol Exp Ther 313:368-78. 2005
    ..We also show that it is difficult to detect M2 receptor function in competitive antagonism studies under conditions where a simultaneous activation of M2 and M3 receptors occurs...
  11. ncbi Preemptive pharmacologic intervention in radiation-induced salivary dysfunction
    S E Taylor
    Department of Oral and Maxillofacial Surgery and Pharmacology, Baylor College of Dentistry The Texas A and M University System, Dallas, Texas 75246, USA
    Proc Soc Exp Biol Med 221:14-26. 1999
    ..Finally, we describe encouraging results from early clinical trials suggesting that protection of salivary glands during therapeutic irradiation may be possible...
  12. ncbi Impaired M3 and enhanced M2 muscarinic receptor contractile function in a streptozotocin model of mouse diabetic urinary bladder
    K J Pak
    Department of Pharmacology, School of Medicine, University of California, Irvine, CA 92697 4625, USA
    Naunyn Schmiedebergs Arch Pharmacol 381:441-54. 2010
    ..M2 receptor activation opposes forskolin-induced relaxation of the urinary bladder, and this M(2) function is enhanced following streptozotocin treatment...
  13. ncbi No evidence for a role of muscarinic M2 receptors in functional antagonism in bovine trachea
    A F Roffel
    Groningen Utrecht Institute for Drug Exploration, Department of Medicinal Chemistry and Molecular Pharmacology, University of Groningen, The Netherlands
    Br J Pharmacol 115:665-71. 1995
    ..Furthermore,they stress the importance of taking into account non-cholinergic controls as well as contraction levels in these experiments...
  14. ncbi Cholinergic treatments with emphasis on m1 muscarinic agonists as potential disease-modifying agents for Alzheimer's disease
    Abraham Fisher
    Israel Institute for Biological Research, PO Box 19, Ness Ziona, Israel
    Neurotherapeutics 5:433-42. 2008
    ..the advantages and drawbacks of some cholinergic compounds, such as acetylcholinesterase inhibitors, M1 muscarinic agonists, M2 antagonists, and nicotinic agonists...
  15. ncbi Salivary gland dysfunction: a review of systemic therapies
    M M Grisius
    Department of Oral Medicine, University of Pennsylvania School of Dental Medicine, Philadelphia 19104 6003, USA
    Oral Surg Oral Med Oral Pathol Oral Radiol Endod 92:156-62. 2001
    ..The aim of this article is to briefly review salivary gland physiology and to summarize the suggested systemic treatment modalities for xerostomia that emphasize controlled clinical trials...
  16. ncbi Distinct muscarinic receptors enhance spontaneous GABA release and inhibit electrically evoked GABAergic synaptic transmission in the chick lateral spiriform nucleus
    J Guo
    Department of Pharmacology, School of Medicine and Health Sciences, The George Washington University, 2300 Eye Street N W, Washington, DC 20037, USA
    Neuroscience 104:1057-66. 2001
    The effects of muscarinic agonists on GABAergic synaptic transmission were examined using whole-cell patch-clamp recording in chick brain slices containing the lateral spiriform nucleus...
  17. ncbi Role of dopamine D1 receptors in the striatal and cortical fos expression induced by the muscarinic agonist pilocarpine
    David Wirtshafter
    Laboratory of Integrative Neuroscience, Department of Psychology, University of Illinois at Chicago, 1007 West Harrison, Chicago, IL 60607 7137, USA
    Eur J Pharmacol 488:85-90. 2004
    ..75-3.00 mg/kg) virtually abolished the Fos response at both sites. These results suggest that stimulation of dopamine D1 receptors may mediate the effects of muscarinic agonists on Fos expression in the striatum, but not the cortex.
  18. ncbi Presynaptic muscarinic receptor subtypes involved in the enhancement of spontaneous GABAergic postsynaptic currents in hippocampal neurons
    J C Gonzalez
    Instituto Teofilo Hernando, IIS Hospital Universitario de la Princesa, Facultad de Medicina, Universidad Autonoma de Madrid, Madrid, Spain
    Eur J Neurosci 33:69-81. 2011
    ....
  19. ncbi FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors
    Nicole Ziegler
    Department of Pharmacology and Toxicology, University of Wuerzburg, Versbacher Str 9, 97078 Wuerzburg, Germany
    Bioorg Med Chem 19:1048-54. 2011
    ..Taken together our data support the notion that orthosteric agonists behave similar at different muscarinic receptor subtypes but that kinetic differences can be observed for receptor activation...
  20. ncbi Muscarinic agonists for the treatment of cognition in schizophrenia
    Angela K Sellin
    Department of Psychiatry, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    CNS Spectr 13:985-96. 2008
    ..We present an overview of likely side effects of muscarinic agonists. We outline the anticholinergic activity of several available antipsychotics and review the available M1 ..
  21. ncbi A single point mutation (N514Y) in the human M3 muscarinic acetylcholine receptor reveals differences in the properties of antagonists: evidence for differential inverse agonism
    Mark R Dowling
    Department of Cell Physiology and Pharmacology, Maurice Shock Medical Sciences Building, University of Leicester, University Road, Leicester, LE1 9HN, UK
    J Pharmacol Exp Ther 317:1134-42. 2006
    ....
  22. ncbi Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity
    Joy E Marlo
    Department of Pharmacology, Vanderbilt University, Nashville, Tennessee 37232, USA
    Mol Pharmacol 75:577-88. 2009
    ..These data also suggest that structurally diverse M(1) potentiators may act by distinct mechanisms and differentially regulate receptor coupling to downstream signaling pathways...
  23. ncbi Temporal characterization of changes in hippocampal cannabinoid CB(1) receptor expression following pilocarpine-induced status epilepticus
    Katherine W Falenski
    Department of Neurology, Virginia Commonwealth University, PO Box 980599, Richmond, VA 23298, USA
    Brain Res 1262:64-72. 2009
    ..This suggests a role for dysregulation of the endocannabinoid system during epileptogenesis and indicates that the CB(1) receptor redistribution temporally correlates with the emergence of epileptic seizures...
  24. ncbi Dual effects of muscarinic M(2) acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: dependence on time, receptor density and receptor agonists
    P Michal
    Institute of Physiology, Academy of Sciences of the Czech Republic, Videnska 1083, 14220 Prague, Czech Republic
    Br J Pharmacol 132:1217-28. 2001
    ..It tends to be abolished by receptor internalization...
  25. ncbi Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development
    Jurgen Wess
    Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892 0810, USA
    Nat Rev Drug Discov 6:721-33. 2007
    ..Importantly, these studies have identified specific mAChR-regulated pathways as potentially novel targets for the treatment of various important disorders including Alzheimer's disease, schizophrenia, pain, obesity and diabetes...
  26. ncbi Two distinct classes of muscarinic action on hippocampal inhibitory synapses: M2-mediated direct suppression and M1/M3-mediated indirect suppression through endocannabinoid signalling
    Yuko Fukudome
    Department of Cellular Neurophysiology, Graduate School of Medical Science, Kanazawa University, 13 1 Takara machi, Kanazawa 920 8640, Japan
    Eur J Neurosci 19:2682-92. 2004
    ..Thus, the muscarinic system can influence hippocampal functions by controlling different subsets of inhibitory synapses through the two distinct mechanisms...
  27. ncbi Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders
    P Jeffrey Conn
    Department of Pharmacology, Vanderbilt Program in Drug Discovery, Vanderbilt Medical Center, Nashville, TN 37232, USA
    Trends Pharmacol Sci 30:148-55. 2009
    ....
  28. ncbi In vivo and in vitro effects of pilocarpine: relevance to ictogenesis
    Nicola Marchi
    Department of Cerebrovascular Research, The Cleveland Clinic Foundation, Cleveland, Ohio 44195, USA
    Epilepsia 48:1934-46. 2007
    ..The extent of such peripheral events and the contribution to SE are unknown and the possibility that pilocarpine also induces SE by peripheral actions is yet untested...
  29. ncbi Muscarinic acetylcholine receptors as CNS drug targets
    Christopher J Langmead
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, Third Avenue, Harlow, Essex, CM19 5AW, UK
    Pharmacol Ther 117:232-43. 2008
    ....
  30. ncbi Activation of the cholinergic system endows compositional properties to striatal cell assemblies
    Luis Carrillo-Reid
    Departamento de Biofisica, Instituto de Fisiologia Celular, Universidad Nacional Autónoma de México UNAM PO Box 70 253, Mexico City, DF 04510 Mexico
    J Neurophysiol 101:737-49. 2009
    ..Neuronal recurrent networks with the characteristics encountered in the present experiments are proposed to allow repeated sequences of activity to become memories and repeated memories to compose learned motor procedures...
  31. ncbi Identification of a ligand-dependent switch within a muscarinic receptor
    T A Spalding
    ACADIA Pharmaceuticals, Inc, San Diego, California 92121, USA
    J Biol Chem 273:21563-8. 1998
    ..These results suggest that TM6 is a switch that defines the activation state of the receptor, and that ligand interactions with TM6 stabilize the receptor in either an active or an inactive conformation...
  32. ncbi Gender comparison of muscarinic receptor expression and function in rat and human urinary bladder: differential regulation of M2 and M3 receptors?
    Christian Kories
    Department of Medicine, University of Essen, Germany
    Naunyn Schmiedebergs Arch Pharmacol 367:524-31. 2003
    ....
  33. ncbi Pilocarpine prevents age-related spatial learning impairments in rats
    Nelson De-Mello
    Departamento de Farmacologia, CCB, Universidade Federal de Santa Catarina, , , SC, Brazil
    Behav Brain Res 158:263-8. 2005
    ..These results indicate that a single administration of Pilo might prevent the age-related learning impairments in rats on a spatial task in the water maze...
  34. ncbi Reconstitution of muscarinic modulation of the KCNQ2/KCNQ3 K(+) channels that underlie the neuronal M current
    M S Shapiro
    Department of Physiology, University of Washington School of Medicine, Seattle, Washington 98195, USA
    J Neurosci 20:1710-21. 2000
    ..The M current is modulated by muscarinic agonists via G-proteins and an unidentified diffusible cytoplasmic messenger...
  35. ncbi Imaging of muscarinic acetylcholine receptor signaling in hippocampal neurons: evidence for phosphorylation-dependent and -independent regulation by G-protein-coupled receptor kinases
    Jonathon M Willets
    Department of Cell Physiology and Pharmacology, University of Leicester, Leicester LE1 9HN, United Kingdom
    J Neurosci 24:4157-62. 2004
    ..Together, our data suggest a role for both phosphorylation-dependent and -independent regulation of M1 mACh receptors in hippocampal neurons...
  36. ncbi Long-term changes in the muscarinic M1 receptor induced by instantaneous formation of wash-resistant xanomeline-receptor complex
    Kayla C De Lorme
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis, MN 55455, USA
    J Pharmacol Exp Ther 323:868-76. 2007
    ..Our results imply that brief exposure to xanomeline followed by washing and prolonged waiting may result in delayed receptor desensitization accompanied by internalization or down-regulation...
  37. ncbi Memory enhancement induced by post-training intrabasolateral amygdala infusions of beta-adrenergic or muscarinic agonists requires activation of dopamine receptors: Involvement of right, but not left, basolateral amygdala
    Ryan T Lalumiere
    Department of Neurobiology and Behavior, University of California, Irvine, CA 92697, USA
    Learn Mem 12:527-32. 2005
    ..Additionally, these findings indicate that the enhancement, but not impairment, of memory consolidation is lateralized to the right BLA...
  38. ncbi Survival of dentate hilar mossy cells after pilocarpine-induced seizures and their synchronized burst discharges with area CA3 pyramidal cells
    H E Scharfman
    Center for Neural Recovery and Rehabilitation Research, Helen Hayes Hospital, West Haverstraw, NY 10993 1195, USA
    Neuroscience 104:741-59. 2001
    ..The fact that mossy cells have epileptiform bursts, and that they are synchronized with area CA3, suggest a previously unappreciated substrate for hyperexcitability in this animal model...
  39. ncbi Differential coupling of muscarinic M1, M2, and M3 receptors to phosphoinositide hydrolysis in urinary bladder and longitudinal muscle of the ileum of the mouse
    John A Tran
    Department of Pharmacology, College of Medicine, University of California, Irvine, CA 92697-4625, USA
    J Pharmacol Exp Ther 318:649-56. 2006
    ..These data suggest a major role for the M3 receptor in eliciting phosphoinositide hydrolysis in the ileum and urinary bladder and minor roles for the M1 and M2 in ileum...
  40. ncbi Reduction of cerebrospinal fluid amyloid beta after systemic administration of M1 muscarinic agonists
    T G Beach
    Sun Health Research Institute, 10515 Santa Fe Drive, Sun City, AZ 85372, USA
    Brain Res 905:220-3. 2001
    ..Systemic administration of 3 M1-selective muscarinic agonists, AF102B, AF150S and AF267B, decreased cerebrospinal fluid (CSF) A beta concentrations; levels of CSF ..
  41. ncbi Therapeutic strategies in Alzheimer's disease: M1 muscarinic agonists
    A Fisher
    Israel Institute for Biological Research, Ness Ziona
    Jpn J Pharmacol 84:101-12. 2000
    ..The therapeutic potential of M1-selective muscarinic agonists including AF102B, AF150(S), AF267B (the AF series) is evaluated and compared, when possible, with several ..
  42. ncbi Inhibition of KCNQ1-4 potassium channels expressed in mammalian cells via M1 muscarinic acetylcholine receptors
    A A Selyanko
    Department of Pharmacology, University College London, UK
    J Physiol 522:349-55. 2000
    ..4. It is concluded that M1 receptors couple to all known KCNQ subunits and that inhibition of KCNQ2 + KCNQ3 channels, like that of native M-channels, requires a diffusible second messenger...
  43. ncbi Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist
    Christopher J Langmead
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, Third Ave, Harlow, Essex, CM19 5AW, UK
    Mol Pharmacol 69:236-46. 2006
    ..These data provide the first direct evidence that AC-42 is an allosteric agonist that activates M(1) receptors in the absence of the orthosteric agonist...
  44. ncbi Regulation of Kv7 (KCNQ) K+ channel open probability by phosphatidylinositol 4,5-bisphosphate
    Yang Li
    Department of Physiology, University of Texas Health Science Center, San Antonio, Texas 78229, USA
    J Neurosci 25:9825-35. 2005
    ..Divergent apparent affinities of Kv7.2-7.4 channels for PIP2 may underlie their highly differential maximal Po observed in cell-attached patches...
  45. ncbi On the physiological relevance of muscarinic acetylcholine receptors in Alzheimer's disease
    H J Koch
    University Clinic of Neurology, Universitatsstrasse 84, 93053 Regensburg, Germany
    Curr Med Chem 12:2915-21. 2005
    ..Experimental results postulate a positive long lasting modulation of the pathological neuronal protein pattern in addition to their cholinomimetic effect...
  46. ncbi Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation
    Tracy A Spalding
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Boulevard, San Diego, CA 92121, USA
    Mol Pharmacol 70:1974-83. 2006
    ..crucial role mediating muscarinic acetylcholine receptor activation by acetylcholine, carbachol, and other muscarinic agonists. We compared the effects of point mutations throughout TM3 on the interactions of carbachol, 4-n-butyl-1-[4-..
  47. ncbi Repeated low-dose treatment of rats with pilocarpine: low mortality but high proportion of rats developing epilepsy
    M Glien
    Department of Pharmacology, Toxicology and Pharmacy, School of Veterinary Medicine, , D-30559 Hannover, Germany
    Epilepsy Res 46:111-9. 2001
    ..The present study demonstrates that systemic treatment of lithium-pretreated rats with several low doses of pilocarpine efficiently produces SE and chronic epilepsy with much lower mortality rates than single-dose pilocarpine...
  48. ncbi Effect of urothelium on bladder contractility in diabetic rats
    Murat Kosan
    Second Urology Clinic, Ankara Numune Education and Research Hospital, Ankara, Turkey
    Int J Urol 12:677-82. 2005
    ..It is known that physiopathological changes in diabetes affect the function of the bladder. In this study, we aimed to demonstrate the possible effects of diabetes on the urothelium during this physiopathological process...
  49. ncbi M1 muscarinic agonists can modulate some of the hallmarks in Alzheimer's disease: implications in future therapy
    Abraham Fisher
    Israel Institute for Biological Research, 74100 Ness Ziona, Israel
    J Mol Neurosci 20:349-56. 2003
    ..We evaluated the M1 muscarinic agonists AF102B (Cevimeline, EVOXAC trade mark : prescribed for Sjøgren's syndrome), AF150(S), and AF267B on some ..
  50. ncbi Postsynaptic M1 and M3 receptors are responsible for the muscarinic enhancement of retrograde endocannabinoid signalling in the hippocampus
    Takako Ohno-Shosaku
    Department of Cellular Neurophysiology, Graduate School of Medical Science, Kanazawa University, 13 1 Takara machi, Kanazawa 920 8640, Japan
    Eur J Neurosci 18:109-16. 2003
    ..These results indicate that the activation of postsynaptic M1 and M3 receptors facilitates the depolarization-induced release of endocannabinoids...
  51. ncbi Experiments to test the role of phosphatidylinositol 4,5-bisphosphate in neurotransmitter-induced M-channel closure in bullfrog sympathetic neurons
    Christopher P Ford
    Centre for Neuroscience, University of Alberta, Edmonton, Alberta, Canada T6G 2H7
    J Neurosci 23:4931-41. 2003
    ..These are the results that might be expected if agonist-induced activation of PLC and the concomitant depletion of PIP2 contribute to the excitatory action of neurotransmitters that suppress gM...
  52. ncbi Regulation of muscarinic acetylcholine receptor signaling
    Chris J van Koppen
    Institut fur Pharmakologie, Universitatsklinikum Essen, Hufelandstrasse 55, D 45122, Essen, Germany
    Pharmacol Ther 98:197-220. 2003
    ..In this review, our current understanding of the complex regulatory processes that underlie signaling of mAChR is summarized...
  53. ncbi Role of receptor protein and membrane lipids in xanomeline wash-resistant binding to muscarinic M1 receptors
    Jan Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague
    J Pharmacol Exp Ther 308:105-10. 2004
    ..We suggest that the binding of xanomeline involves interhelical penetration of M1 muscarinic receptor by xanomeline's O-alkyl chain and interaction with membrane lipids surrounding the receptor...
  54. ncbi Cholinergic targets for cognitive enhancement in schizophrenia: focus on cholinesterase inhibitors and muscarinic agonists
    Joseph I Friedman
    Department of Psychiatry, The Mount Sinai School of Medicine, One Gustave L Levy Place, Box 1230, New York, NY 10029, USA
    Psychopharmacology (Berl) 174:45-53. 2004
    ..Therefore, pharmacological treatments that enhance central cholinergic function may be useful as cognitive enhancers in schizophrenia...
  55. ncbi Subunit-specific modulation of KCNQ potassium channels by Src tyrosine kinase
    Nikita Gamper
    Department of Physiology, University of Texas Health Science Center at San Antonio, San Antonio, Texas 78229, USA
    J Neurosci 23:84-95. 2003
    ..Finally, experiments using cloned KCNQ2/3 channels, Src and M(1) muscarinic receptors, and sympathetic neurons demonstrated that the actions on KCNQ channels by Src and by muscarinic agonists use distinct mechanisms.
  56. ncbi Effects of Ba-Wei-Die-Huang-Wan on the cholinergic function and protein expression of M2 muscarinic receptor of the urinary bladder in diabetic rats
    Yat Ching Tong
    Department of Urology, College of Medicine, National Cheng Kung University, Tainan City, 70101, Taiwan, ROC
    Neurosci Lett 330:21-4. 2002
    ..In conclusion, there was an over-expression of M(2) receptor resulting in hyper-contractility in the bladder of diabetic rats. Ba-Wei-Die-Huang-Wan significantly alleviated the alterations...
  57. ncbi Recovery from muscarinic modulation of M current channels requires phosphatidylinositol 4,5-bisphosphate synthesis
    Byung-Chang Suh
    Department of Physiology and Biophysics, University of Washington School of Medicine, Seattle, WA 98195, USA
    Neuron 35:507-20. 2002
    ..Lipid phosphorylation by PI 4-kinase is required for recovery from muscarinic modulation of M current...
  58. ncbi Allosteric modulation by persistent binding of xanomeline of the interaction of competitive ligands with the M1 muscarinic acetylcholine receptor
    Jan Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic
    J Pharmacol Exp Ther 301:1033-41. 2002
    ..Our findings are best interpreted in terms of allosteric interactions between xanomeline-persistent binding to the M(1) muscarinic receptor and competitive ligands bound to the classical receptor binding site...
  59. ncbi Discovery of an ectopic activation site on the M(1) muscarinic receptor
    Tracy A Spalding
    ACADIA Pharmaceuticals, Inc, San Diego, California 92121, USA
    Mol Pharmacol 61:1297-302. 2002
    ....
  60. ncbi Nuclear calcium signaling evoked by cholinergic stimulation in hippocampal CA1 pyramidal neurons
    John M Power
    Division of Neuroscience, John Curtin School for Medical Research, Australian National University, Canberra, ACT 0200, Australia
    J Neurosci 22:3454-62. 2002
    ..Because rises in nuclear calcium are known to initiate the transcription of novel genes, we suggest that these actions of cholinergic stimulation may underlie its effects on learning and memory...
  61. ncbi Regulation of acetylcholine release by muscarinic receptors at the mouse neuromuscular junction depends on the activity of acetylcholinesterase
    Jasmina Minic
    Institut Fédératif de Neurobiologie Alfred Fessard, Laboratoire de Neurobiologie Cellulaire et Moleculaire, C N R S, U P R 9040, 1 Avenue de la Terrasse, 91198 Gif sur Yvette Cedex, France
    Eur J Neurosci 15:439-48. 2002
    ....
  62. ncbi Homologous mutations near the junction of the sixth transmembrane domain and the third extracellular loop lead to constitutive activity and enhanced agonist affinity at all muscarinic receptor subtypes
    Diane J Ford
    Department of Pharmacology, The Pennsylvania State University College of Medicine, Hershey, Pennsylvania 17033, USA
    J Pharmacol Exp Ther 300:810-7. 2002
    ..Based on the results of the present study, it is possible that TM6 represents a general switch for the activation of the muscarinic receptor family...
  63. ncbi NMDA-receptor regulation of muscarinic-receptor stimulated inositol 1,4,5-trisphosphate production and protein kinase C activation in single cerebellar granule neurons
    Kenneth W Young
    Department of Cell Physiology and Pharmacology, University of Leicester, Medical Sciences Building, University Road, Leicester LE1 9HN, UK
    J Neurochem 89:1537-46. 2004
    ..Thus, NMDA-mediated Ca2+ influx and PLC activation may represent a coincident-detection system whereby ionotropic and metabotropic signals combine to stimulate InsP(3) production and PKC-mediated phosphorylation events in CGNs...
  64. ncbi Cholinergic dilation of cerebral blood vessels is abolished in M(5) muscarinic acetylcholine receptor knockout mice
    M Yamada
    Laboratory of Bioorganic Chemistry National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
    Proc Natl Acad Sci U S A 98:14096-101. 2001
    ....
  65. ncbi Relationship between membrane phosphatidylinositol-4,5-bisphosphate and receptor-mediated inhibition of native neuronal M channels
    Joanna S Winks
    1Ion Channel Pharmacology Group, IPC 388, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, United Kingdom
    J Neurosci 25:3400-13. 2005
    ....
  66. ncbi Muscarinic agonist-mediated heterologous desensitization in isolated ileum requires activation of both muscarinic M2 and M3 receptors
    Michael T Griffin
    Department of Physical Sciences, Chapman University, Orange, California, USA
    J Pharmacol Exp Ther 308:339-49. 2004
    ....
  67. ncbi A critical role for beta cell M3 muscarinic acetylcholine receptors in regulating insulin release and blood glucose homeostasis in vivo
    Dinesh Gautam
    Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, Maryland 20892, USA
    Cell Metab 3:449-61. 2006
    ..These findings indicate that beta cell M3 muscarinic receptors play a key role in maintaining proper insulin release and glucose homeostasis...
  68. ncbi Two-state models and the analysis of the allosteric effect of gallamine at the M2 muscarinic receptor
    Frederick J Ehlert
    Department of Pharmacology, School of Medicine, University of California, Irvine, CA 92697 4625, USA
    J Pharmacol Exp Ther 325:1039-60. 2008
    ..If it is assumed that allosterism occurs at the relay site and not the activation site, then this model can account for affinity-only modulation in a manner consistent with the allosteric ternary complex model...
  69. ncbi Insulin, IGF-1, and muscarinic agonists modulate schizophrenia-associated genes in human neuroblastoma cells
    C Anthony Altar
    Psychiatric Genomics, Inc, Gaithersburg, Maryland, USA
    Biol Psychiatry 64:1077-87. 2008
    ..We determined with human SH-SY5Y neuroblastoma and astrocyte cell lines whether insulin or other molecules could modulate genes opposite to their change reported in schizophrenia brain...
  70. ncbi Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects
    F P Bymaster
    Lilly Neuroscience Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Brain Res 795:179-90. 1998
    ..to stimulate in vivo phosphoinositide (PI) hydrolysis and compared it to a number of direct acting muscarinic agonists, two cholinesterase inhibitors and a putative m1 agonist/muscarinic m2 antagonist...
  71. ncbi On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor
    A Christopoulos
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis, Minnesota 55455, USA
    Mol Pharmacol 53:1120-30. 1998
    ....
  72. ncbi Diabetes mellitus and responses of the urinary bladder to acetylcholine: an in vitro study
    Abdon M Nsabimana
    Department of Pharmacology, School of Pharmacy and Pharmacology, Faculty of Health Sciences, University of KwaZulu Natal, Durban, South Africa
    J Smooth Muscle Res 44:143-50. 2008
    ..on the responses of diabetic bladder strips to cholinergic nerve stimulation or exogenously-administered muscarinic agonists, especially acetylcholine (ACh)...
  73. ncbi G protein coupling and signaling pathway activation by m1 muscarinic acetylcholine receptor orthosteric and allosteric agonists
    Rachel L Thomas
    Department of Cell Physiology and Pharmacology, University of Leicester, Room 4 04, Henry Wellcome Building, Lancaster Road, Leicester LE19HN, UK
    J Pharmacol Exp Ther 327:365-74. 2008
    ..77-LH-28-1 (1-[3-(4-butyl-1-piperidinyl)propyl]-3,4-dihydro-2(1H)-quinolinone), and a range of orthosteric muscarinic agonists [oxotremorine-M (oxo-M), arecoline, and pilocarpine] in Chinese hamster ovary cells recombinantly ..
  74. ncbi Activation of muscarinic acetylcholine receptors via their allosteric binding sites
    J Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic
    Proc Natl Acad Sci U S A 93:8705-9. 1996
    ..of the classical-binding sites of these receptors and either diminish or increase their affinity for muscarinic agonists and classical antagonists...
  75. ncbi Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia
    Anantha Shekhar
    Department of Psychiatry, Indiana University School of Medicine, 1111 West 10th St, Suite 313, Indianapolis, IN 46202, USA
    Am J Psychiatry 165:1033-9. 2008
    ..The authors studied xanomeline, a relatively selective muscarinic type 1 and type 4 (M(1) and M(4)) receptor agonist, to determine if this agent is effective in the treatment of schizophrenia...
  76. ncbi Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists
    M H Richards
    Marion Merrell Dow Research Center, Strasbourg, France
    Br J Pharmacol 114:1241-9. 1995
    1. A comparative study of receptor activation by ten full and partial muscarinic agonists was undertaken on the five subtypes of human muscarinic receptors expressed at similar receptor densities in Chinese hamster ovary (CHO-K1) cells...
  77. ncbi Novel persistent activation of muscarinic M1 receptors by xanomeline
    A Christopoulos
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis 55455, USA
    Eur J Pharmacol 334:R3-4. 1997
    The muscarinic agonists, xanomeline and carbachol, displayed similar intrinsic activities in stimulating neuronal nitric oxide synthase at muscarinic M1 receptors in Chinese hamster ovary (CHO) cells, with xanomeline being more potent...
  78. ncbi Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1
    C J Langmead
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, Harlow, Essex, UK
    Br J Pharmacol 154:1104-15. 2008
    ..However, studies with this compound have been limited to recombinantly expressed mAChRs...
  79. ncbi Cyclicity of spontaneous recurrent seizures in pilocarpine model of temporal lobe epilepsy in rat
    Karolien Goffin
    Katholieke Universiteit Leuven, Leuven, Belgium
    Exp Neurol 205:501-5. 2007
    ..Finally, our data suggest that the model can be used for studies aiming at identifying the mechanisms of seizure clustering...
  80. ncbi Effects of an agonist, allosteric modulator, and antagonist on guanosine-gamma-[35S]thiotriphosphate binding to liposomes with varying muscarinic receptor/Go protein stoichiometry
    J Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, 14220 Prague, Czechia
    Mol Pharmacol 54:899-906. 1998
    ..This suggests that the receptors and G proteins are located in microdomains in which their concentrations remain constant, despite variations in the amounts of lipidic membranes in the system...
  81. ncbi Long-term wash-resistant effects of brief interaction of xanomeline at the M1 muscarinic receptor
    Kayla C De Lorme
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Mayo Mail Code 392, 420 Delaware St. SE, Minneapolis, MN 55455, USA
    Neurosci Lett 410:11-4. 2006
    ..However, possible involvement of other mechanisms of long-term receptor regulation cannot be discounted...
  82. ncbi The guinea pig ileum lacks the direct, high-potency, M(2)-muscarinic, contractile mechanism characteristic of the mouse ileum
    Michael T Griffin
    Department of Chemistry, Chapman University, Orange, CA, USA
    Naunyn Schmiedebergs Arch Pharmacol 380:327-35. 2009
    ..The guinea pig ileum, therefore, lacks a direct, highly potent, M(2)-contractile component but may have a direct, lower potency M(2) component...
  83. ncbi Assessment of the progressive nature of cell damage in the pilocarpine model of epilepsy
    L Covolan
    Departamento de Fisiologia, , , SP, Brasil
    Braz J Med Biol Res 39:915-24. 2006
    ..As a consequence of both mechanisms, subsequent insults after an initial insult result in very little damage regardless of their intensity...
  84. ncbi Three distinct muscarinic signalling pathways for cationic channel activation in mouse gut smooth muscle cells
    Takashi Sakamoto
    Department of Pathogenetic Veterinary Science, United Graduate School of Veterinary Science, Gifu University, 1 1 Yanagido, Gifu 501 1193, Japan
    J Physiol 582:41-61. 2007
    ..The delineation of this pathway is consistent with the formation of a functional unit by the M2-Go protein and the M3-PLC systems predicted to control cationic channels...
  85. ncbi Muscarinic receptor function, density and G-protein coupling in the overactive diabetic rat bladder
    L A Stevens
    Biomedical Research Centre, Sheffield Hallam University, Sheffield S1 1WB, UK
    Auton Autacoid Pharmacol 26:303-9. 2006
    1 Bladder smooth muscle sensitivity to muscarinic agonists is increased in the overactive bladder...
  86. ncbi Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands
    Christopher N Davis
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    BMC Pharmacol 9:14. 2009
    ..The focus of the present study was to determine if M1 receptors activated by allosteric agonists undergo the same regulatory fate as M1 receptors activated by orthosteric agonists...
  87. ncbi Regulation of bladder muscarinic receptor subtypes by experimental pathologies
    M R Ruggieri
    Department of Urology, Temple University, Philadelphia, PA, USA
    Auton Autacoid Pharmacol 26:311-25. 2006
    ..This finding has substantial implications for the clinical treatment of abnormal bladder contractions...
  88. ncbi Acute induction of epileptiform discharges by pilocarpine in the in vitro isolated guinea-pig brain requires enhancement of blood-brain barrier permeability
    L Uva
    Unit of Experimental Neurophysiology and Epileptology, Fondazione Istituto Neurologico, Via Celoria 11, 20133 Milan, Italy
    Neuroscience 151:303-12. 2008
    ..Pilocarpine accumulation secondary to BBB permeability changes may contribute to in vivo ictogenesis in the pilocarpine epilepsy model...
  89. ncbi Muscarinic M3 receptor inactivation reveals a pertussis toxin-sensitive contractile response in the guinea pig colon: evidence for M2/M3 receptor interactions
    G W Sawyer
    Department of Pharmacology, College of Medicine, University of California, Irvine, USA
    J Pharmacol Exp Ther 289:464-76. 1999
    ..This model predicts that a response mediated by both the M2 and M3 receptor can be pertussis toxin sensitive yet exhibit an antagonistic profile indicative of an M3 response...
  90. ncbi Cholinergic regulation of the evoked quantal release at frog neuromuscular junction
    Eugeny E Nikolsky
    Institute of Biochemistry and Biophysics, Russian Academy of Sciences, Kazan, Russia
    J Physiol 560:77-88. 2004
    ..The muscarinic agonists, oxotremorine and the propargyl ester of arecaidine, as well as antagonists such as pirenzepine, AF-DX 116 ..
  91. ncbi Both endogenous and exogenous ACh plays antinociceptive role in the hippocampus CA1 of rats
    X 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...
  92. ncbi PMA decreases the proliferation of retinal cells in vitro: the involvement of acetylcholine and BDNF
    Aline 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...
  93. ncbi Role of muscarinic acetylcholine receptors in a guinea pig model of asthma
    Yuji Tohda
    Fourth Department of Internal Medicine, Kinki University School of Medicine, Osakasayama, Osaka, Japan
    Int Immunopharmacol 2:1521-7. 2002
    ..These results suggest that, in OA-sensitized guinea pigs, a dysfunction of M2R leads to the abnormal density of M3R...
  94. ncbi Subtype-specific regulation of the expression and function of muscarinic acetylcholine receptors in embryonic chicken retinal cells
    Juan 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...
  95. ncbi Chronotropic response of beta-adrenergic-, muscarinic-, and calcitonin gene-related peptide-receptor agonists in right atria from neonatal capsaicin-treated rats
    Alessandra L Gasparetti
    Department of Pharmacology, Faculty of Medical Sciences, UNICAMP, P.O. Box 6111, 13081-970, Campinas (SP, Brazil
    Neurosci Lett 325:147-50. 2002
    ..In summary, capsaicin treatment in newborn rats produces a desensitization of chronotropic response mediated by beta-adrenoceptors in isolated right atria from 30-day-old rats possibly due to a massive release of catecholamines...
  96. ncbi Activation of muscarinic acetylcholine receptors elicits pigment granule dispersion in retinal pigment epithelium isolated from bluegill
    Alfredo Gonzalez
    Department of Biology, Texas State University San Marcos, Texas 78666, USA
    BMC Neurosci 5:23. 2004
    ..To determine the receptor pathway involved in eliciting pigment granule migration, we isolated retinal pigment epithelium from bluegill and subjected it to a battery of cholinergic agents...
  97. ncbi Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors
    Thomas M Böhme
    Department of Medicinal Chemistry, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    J Med Chem 45:3094-102. 2002
    ..This is evidence that suggests that agonist-induced increase in catecholamine synthesis observed in these regions is mediated by M(4) receptors...
  98. ncbi Multiple muscarinic acetylcholine receptor subtypes modulate striatal dopamine release, as studied with M1-M5 muscarinic receptor knock-out mice
    Weilie Zhang
    Laboratory of Bioorganic Chemistry, National Institutes of Diabetes and Digestive and Kidney Diseases, Bethesda, Maryland 20892 0810, USA
    J Neurosci 22:6347-52. 2002
    ..These findings should contribute to a better understanding of the important functional roles that the muscarinic cholinergic system plays in striatal function...
  99. ncbi Muscarinic receptors of the neostriatum--their role in controlling operant behavior in dogs
    K B Shapovalova
    I. P. Pavlov Institute of Physiology, Russian Academy of Sciences, St. Petersburg
    Neurosci Behav Physiol 32:389-99. 2002
    ....
  100. ncbi Salivary gland-sparing prophylactic pilocarpine treatment has no effect on tumor regrowth after irradiation
    R Licht
    Department of Radiation and Stress Cell Biology, University of Groningen, 9713 AV Groningen, The Netherlands
    Radiat Res 157:596-8. 2002
    ..Use of this drug therefore may lead to therapeutic gain in the treatment of head and neck cancer...
  101. ncbi Effects of N-ethylmaleimide on conformational equilibria in purified cardiac muscarinic receptors
    Chi Shing Sum
    Department of Pharmacology and Faculty of Pharmacy, University of Toronto, Toronto, Ontario M5S 2S2, Canada
    J Biol Chem 277:36188-203. 2002
    ..Similarities with constitutively active receptors suggest that R and R* are akin to the inactive and active states, respectively. Purified M(2) receptors therefore appear to exist predominantly in their active state...

Research Grants72

  1. Efficacy of GluR5 Antogonists Against Soman-Induced Seizures and Neuropathology
    MARIA BRAGA; Fiscal Year: 2007
    ....
  2. Atypical Antipsychotics: Effects on Hepatic Glucose and Lipid Metabolism in Human
    Karen Teff; Fiscal Year: 2009
    ..Findings from these studies will have important clinical relevance to the treatment of schizophrenia. ..
  3. Atypical Antipsychotics: Effects on Hepatic Glucose and Lipid Metabolism in Human
    Karen L Teff; Fiscal Year: 2010
    ..Findings from these studies will have important clinical relevance to the treatment of schizophrenia. ..
  4. REGULATION OF GLANDULAR MUCOUS CELL SECRETION
    DAVID CULP; Fiscal Year: 2001
    ..Results will provide specific information for determination of the dose and temporal administration of agonist in future clinical trials to treat patients with salivary hypofunction. ..
  5. CELLULAR AND MOLECULAR STUDIES OF VESTIBULAR HAIR CELLS
    MANNING CORREIA; Fiscal Year: 2007
    ..The two specific aims of this project are linked in that one drives studies of the the effector pKir2.1 and the second directs studies the msucarinic receptors in the pathway proposed above. ..
  6. The neurogenic potential of cholinergic activation in AD.
    Elizabeth Eckman; Fiscal Year: 2009
    ..Early preliminary data indicate that muscarinic agonists do indeed increase cytogenesis in a manner very similar to that initially observed with D3 agonist ..
  7. The neurogenic potential of cholinergic activation in AD.
    ELIZABETH ADAMS ECKMAN; Fiscal Year: 2010
    ..Early preliminary data indicate that muscarinic agonists do indeed increase cytogenesis in a manner very similar to that initially observed with D3 agonist ..
  8. EFFECTS OF LITHIUM ON CHOLINERGIC ACTIVITY
    RICHARD JOPE; Fiscal Year: 1990
    ..Attainment of these goals will increase our understanding of the effects of lithium that may be related to its therapeutic effect in mania and may generate hypotheses as to the underlying causes of bipolar affective disorders...
  9. CHOLINERGIC MECHANISMS IN AGING AND AD
    LINCOLN POTTER; Fiscal Year: 2002
    ..hemi-PD, but is expected to alter responses to apomorphine (dopamine agonist), pilocarpine and xanomeline (muscarinic agonists). At the least, the results will show whether a specific m1 antagonist can be used to control seizures...
  10. Regulation of Airway Goblet Cell Mucin Secretion
    C Davis; Fiscal Year: 2007
    ..For instance, the effects of muscarinic agonists are highly controversial, there are no data relevant to the mechanisms and pathways underlying the ..
  11. Prostanoid modulators that reduce brain injury and inflammation after seizures
    Raymond Dingledine; Fiscal Year: 2007
    ....
  12. Muscarinic regulation of plasticity in the brain
    Gene Robinson; Fiscal Year: 2007
    ..Our results will also suggest directions for the development of treatments for the decline in mental function that accompanies human aging. ..
  13. Muscarinic regulation of plasticity in the brain
    Gene Robinson; Fiscal Year: 2009
    ..Our results will also suggest directions for the development of treatments for the decline in mental function that accompanies human aging. ..
  14. Molecular mechanism of regulation of mI(CAT) in intestinal smooth muscle cells
    MICHAEL ZHU; Fiscal Year: 2009
    ..In the smooth muscle cells, co-stimulation of M2R and M3R by muscarinic agonists activates a cation current, mICAT...