Abstract
Muscarinic receptors are widely distributed throughout the body and play a key role in numerous vital functions.1 Activation of muscarinic receptors decreases the rate and force of contraction of the heart, relaxes peripheral blood vessels, constricts the airways of the lung, increases the secretions or motility of various organs of the gastrointestinal tract, increases the secretions of the lacrimal, salivary and sweat glands, and constricts the iris sphincter and ciliary muscles of the eye. Muscarinic receptors also participate in important functions within the brain including learning, memory and the control of posture.1
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
G. Pepeu and H. Ladinsky, eds., “Cholinergic Mechanisms,” Plenum Press, New York (1981).
T.-P. Lee, J. F. Kuo, and P. Greengard, Role of muscarinic cholinergic receptors in regulation of guanosine 3’:5’-cyclic monophosphate content in mammalian brain, heart muscle, and intestinal smooth muscle, Proc. Natl. Acad. Sci. U.S.A. 69: 3287 (1972).
J. Van Sande, C. Erneux, and J. E. Dumont, Negative control of TSH action by iodide and acetylcholine: mechanism of action in intact thyroid cells, J. Cyclic Nucleotide Res. 3: 335 (1977).
F. Murad, Y.-M. Chi, T. W. Rall, and E. W. Sutherland, The effect of catecholamines and choline esters on the formation of adenosine 3’,5’-cyclic phosphate by preparations from cardiac muscle and liver, J. Biol. Chem. 237: 1233 (1962).
H. Kurose, T. Katada, T. Amano, and M. Ui, Specific uncoupling by islet-activating protein, pertussis toxin, of negative signal transduction via a-adrenergic, cholinergic, and opiate receptors in euroblastoma x glioma hybrid cells, J. Biol. Chem. 258: 4870 (1983).
B. Sakmann, A. Noma, and W. Trautwein, Acetylcholine activation of single muscarinic K+ channels in isolated pacemaker cells of the mammalian heart, Nature 303: 250 (1983).
A. Constanti and D. A. Brown, M-currents in voltage-clamped mammalian sympathetic neurones, Neurosci. Lett. 24: 289 (1981).
J. V. Halliwell and P. R. Adams, Voltage-clamp analysis of muscarinic excitation in hippocampal neurons, Brain Res. 250: 71 (1982).
A. Yatani, J. Codina, A. M. Brown, and L. Birnbaumer, Direct activation of mammalian atrial muscarinic potassium channels by GTP regulatory protein Gk, Science 235: 207 (1987).
M. R. Hokin and L.E. Hokin, Effects of acetylcholine on phospholipids in the pancreas, J. Biol. Chem. 209: 549 (1954).
M. J. Berridge, Rapid accumulation of inositol trisphosphate reveals that agonists hydrolyse polyphosphoinositides instead of phosphatidylinositol, Biochem. J. 212: 849 (1983).
H. Streb, R. F. Irvine, M. J. Berridge, and I. Schultz, Release of CA+2 from a nonmitochondrial intracellular store in pancreatic acinar cells by inositol-1,4,5-trisphosphate, Nature, 306: 67 (1983).
A. Kishimoto, Y. Takai, T. Mori, U. Kikkawa, and Y. Nishizuka, Activation of calcium and phospholipid-dependent protein kinase by diacylglycerol, its possible relation to phosphatidylinositol turnover, J. Biol. Chem. 255: 2273 (1980).
M. Kuno and P. Gardner, Ion channels activated by inositol 1,4,5trisphosphate in plasma membrane of human T-lymphocytes, Nature 326: 301 (1987).
D. O. Lucas, S. M. Bajjalieh, J. A. Kowalchyk, and T. J. F. Martin, Direct stimulation by thyrotropin-releasing hormone (TRH) of polyphosphoinositide hydrolysis in GH3 cell membranes by a guanine nucleotide-modulated mechanism, Biochem. Biophys. Res. Comm. 132: 721 (1985).
G. S. Johnson and V. R. Mukku, Evidence in intact cells for an involvement of GTP in the activation of adenylate cyclase, J. Biol. Chem. 254: 95 (1979).
C. M. Smith, J. F. Henderson, and H. P. Baer, Effect of GTP on cyclic AMP concentrations in intact Ehrlich ascites tumor cells, J. Cyclic Nucleotide Res. 3: 347 (1977).
R. B. Meeker and T. K. Harden, Muscarinic receptor-mediated control of cyclic AMP metabolism, Mol. Pharmacol. 23: 384 (1983).
A. M. Watanabe, M. M. McConnaughey, R. A. Strawbridge, J. W. Fleming, L. R. Jones, and H. R. Besch, Muscarinic cholinergic receptor modulation of ß-adrenergic receptor affinity for catecholamines, J. Biol. Chem. 253: 4833 (1978).
J. H. Brown, Cholinergic inhibition of catecholamine-stimulable cyclic AMP accumulation in murine atria, J. Cyclic Nucleotide Res. 5: 423 (1979).
M. C. Olianas, P. Onali, N. Y. Neff, and E. Costa, Adenylate cyclase activity of synaptic membranes from rat striatum, inhibition by muscarinic agonists, Mol. Pharmacol. 29: 393 (1983).
T. Evans, M. M. Smith, L. T. Tanner, and T. K. Harden, Muscarinic cholinergic receptors of two cell lines that regulate cyclic AMP metabolism by different molecular mechanisms. Mol. Pharmacol. 26: 395 (1984).
K. H. Jakobs, K. Aktories, and G. Schultz, GTP-dependent inhibition of cardiac adenylate cyclase by muscarinic cholinergic agonists, N. S. Arch. Pharmacol. 310: 113 (1979).
N. M. Nathanson, Molecular properties of the muscarinic acetylcholine receptor, Ann. Rev. Neurosci. 10: 195 (1987).
F. J. Ehlert, The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium, Mol. Pharmacol. 28: 410 (1985).
R. F. Furchgott and P. Bursztyn, Comparison of dissociation constants and relative efficacies of selected agonists acting on parasympathetic receptors, Ann. N. Y. Acad. Sci. 144: 882 (1967).
F. J. Ehlert, Coupling of muscarinic receptors to adenylate cyclase in the rabbit myocardium: effects of receptor inactivation, J. Pharmacol. Ex. Ther. 240: 23 (1987).
J. H. Brown and D. Goldstein, Differences in muscarinic receptor reserve for inhibition of adenylate cyclase and stimulation of phosphor inositide hydrolysis in chick heart cells, Mol. Pharmacol. 30: 566 (1986).
A. De Lean, J. M. Stadel, and R. J. Lefkowitz, A ternary complex model explains the agonist-specific binding properties of adenylate cyclasecoupled ß-adrenergic receptor, J. Biol. Chem. 255: 7108 (1980).
G. Weber, Energetics of ligand binding to proteins, Adv. Prot. Chem. 29: 1 (1975).
T. W. T. Lee, M. J. Sole, and J. W. Wells, Assessment of a ternary complex model for the binding of agonists to neurohumoral receptors, Biochemistry 25: 7009 (1986).
C. P. Berrie, N. J. M. Birdsall, E. C. Hulme, M. Keen, and J. M. Stockton, Solubilization and characterization of guanine neucleotidesensitive muscarinic agonist binding sites from rat myocardium, Br. J. Pharmacol. 82: 853 (1984).
N. J. M. Birdsall, A. S. V. Burgen, and E. C. Hulme, The binding of agonists to brain muscarinic receptors, Mol. Pharmacol. 14: 723 (1987).
H.-M. S. Wong, M. J. Sole, and J. W. Wells, Assessment of mechanistic proposals for the binding of agonists to cardiac muscarinic receptors, Biochemistry 25: 6995 (1986).
F. J. Ehlert, W. R. Roeske, L. B. Rosenberger, and H. I. Yamamura, The influence of guanyl-5’-yl imidodiphosphate and sodium on muscarinic receptor binding in the rat brain and longitudinal muscle of the rat ileum, Life Sci. 26: 245 (1980).
M. Waelbroeck, P. Robberecht, P. Cuatelain, and J. Cristophe, Rat cardiac muscarinic receptors. 1. Effects of guanine nucleotides on high-and low-affinity binding sites, Mol. Pharmacol. 21: 581 (1982).
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1988 Springer Science+Business Media New York
About this chapter
Cite this chapter
Ehlert, F.J. (1988). Correlation between the Binding Parameters of Muscarinic Agonists and thier Inhibition of Adenylate Cyclase Activity. In: Kito, S., Segawa, T., Kuriyama, K., Tohyama, M., Olsen, R.W. (eds) Neuroreceptors and Signal Transduction. Advances in Experimental Medicine and Biology, vol 236. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-5971-6_21
Download citation
DOI: https://doi.org/10.1007/978-1-4757-5971-6_21
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4757-5973-0
Online ISBN: 978-1-4757-5971-6
eBook Packages: Springer Book Archive