Binding Tests in Respiratory System

Living reference work entry

Abstract

Histamine receptors have been classified on the basis of pharmacological analysis (Hill et al. 1997). Histamine exerts its action via at least four receptor subtypes. The H1 receptor couples mainly to Gq/11, thereby stimulating phospholipase C, whereas the H2 receptor interacts with Gs to activate adenylyl cyclase. The histamine H3 and H4 receptors couple to Gi proteins to inhibit adenylyl cyclase and to stimulate MAPK (Hough 2001).

Keywords

Chronic Obstructive Pulmonary Disease Muscarinic Receptor Adenylyl Cyclase Histamine Receptor Tiotropium Bromide 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

References and Further Reading

Histamine (H1) Receptor Binding

  1. Bryce PJ, Mathias CB, Harrison KL, Watanabe T, Geha RS, Oettgen HC (2006) The H1 histaminic receptor regulates allergic lung responses. J Clin Invest 116(6):1624–1632PubMedCentralPubMedCrossRefGoogle Scholar
  2. Carswell H, Nahorski SR (1982) Distribution and characteristics of histamine H1-receptors in guinea-pig airways identified by [3H]mepyramine. Eur J Pharmacol 81:301–307PubMedCrossRefGoogle Scholar
  3. Chang RSL, Tran VT, Snyder SH (1979) Heterogeneity of histamine H1-receptors: species variations in [3H]mepyramine binding of brain membranes. J Neurochem 32:1653–1663PubMedCrossRefGoogle Scholar
  4. De Backer MD, Gommeren W, Moereels H, Nobels G, Van Gompel P, Leysen JE, Luyten WH (1993) Genomic cloning, heterologous expression and pharmacological characterization of a human H1-receptor. Biochem Biophys Res Commun 197:1601–1608PubMedCrossRefGoogle Scholar
  5. Hill SJ, Emson PC, Young JM (1978) The binding of [3H]mepyramine to histamine H1 receptors in guinea-pig brain. J Neurochem 31:997–1004PubMedCrossRefGoogle Scholar
  6. Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997) International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 49:253–278PubMedGoogle Scholar
  7. Hough LB (2001) Genomics meets histamine receptors: new subtype, new receptor. Mol Pharmacol 59:415–419PubMedGoogle Scholar
  8. Ruat M, Schwartz JC (1989) Photoaffinity labeling and electrophoretic identification of the H1-receptor: comparison of several brain regions and animal species. J Neurochem 53:335–339PubMedCrossRefGoogle Scholar

Muscarinic Receptor Binding

  1. Alabaster VA (1997) Discovery and development of selective M3 antagonists for clinical use. Life Sci 60:1053–1060PubMedCrossRefGoogle Scholar
  2. Barnes PJ (1993) Muscarinic receptor subtypes: implications for therapy. Agents Actions Suppl 43:243–252PubMedGoogle Scholar
  3. Barnes PJ (2001) Tiotropium bromide. Expert Opin Investig Drugs 10:733–740PubMedCrossRefGoogle Scholar
  4. Barnes PJ (2004) Distribution of receptor targets in the lung. Proc Am Thorac Soc 1:345–351PubMedCrossRefGoogle Scholar
  5. Barnes PJ, Belvisi MG, Mak JCW, Haddad EB, O’Connor B (1995) Tiotropium bromide (Ba 679 BR), a novel long-acting muscarinic antagonist for the treatment of obstructive airway disease. Life Sci 56:853–859PubMedCrossRefGoogle Scholar
  6. Barnes PJ, Haddad EB, Rousell J (1997) Regulation of muscarinic M2 receptors. Life Sci 60:1015–1021PubMedCrossRefGoogle Scholar
  7. Chelala JL, Kilani A, Miller JM, Martin RJ, Ernsberger P (1998) Muscarinic receptor binding sites of the M4 subtype in porcine lung parenchyma. Pharmacol Toxicol 83:200–207PubMedCrossRefGoogle Scholar
  8. Cheng YC, Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099–3108PubMedCrossRefGoogle Scholar
  9. Costello RW, Jacoby DB, Fryer AD (2006) Pulmonary neuronal M2 muscarinic receptor function in asthma and animal models of hyperreactivity. Thorax 53:613–618CrossRefGoogle Scholar
  10. Disse B (2001) Antimuscarinic treatment for lung diseases. From research to clinical practice. Life Sci 68:2557–2564PubMedCrossRefGoogle Scholar
  11. Disse B, Reichl R, Speck G, Traunecker W, Ludwig-Romminger KL, Hammer R (1993) Ba 679 BR, a novel long-acting anticholinergic bronchodilator. Life Sci 52:537–544PubMedCrossRefGoogle Scholar
  12. Disse B, Speck GA, Rominger KL, Witek TJ Jr, Hammer R (1999) Tiotropium (Spiriva™): mechanistical considerations and clinical profile in obstructive lung disease. Life Sci 64:457–464PubMedCrossRefGoogle Scholar
  13. Haddad EB, Mak JC, Barnes PJ (1994) Characterization of [3H]Ba 679 BR, a slowly dissociating muscarinic antagonist, in human lung: radioligand and autoradiographic mapping. Mol Pharmacol 45:899–907PubMedGoogle Scholar
  14. Hirose H, Aoki I, Kimura T, Fujikawa T, Numazawa T, Sasaki K, Sato A, Hasegawa T, Nishikibe M, Mitsuya M, Ohtake N, Mase T, Noguchi K (2001) Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel muscarinic antagonist with M2-sparing antagonistic activity. J Pharmacol Exp Ther 297:790–797PubMedGoogle Scholar
  15. Hislop AA, Mak JCW, Reader JA, Barnes PJ, Haworth SG (1998) Muscarinic receptor subtypes in the porcine lung during postnatal development. Eur J Pharmacol 359:211–221PubMedCrossRefGoogle Scholar
  16. Mak JC, Barnes PJ (1990) Autoradiographic visualization of muscarinic receptor subtypes in human and guinea pig lung. Am Rev Respir Dis 141:1559–1568PubMedCrossRefGoogle Scholar
  17. Matsumoto S (1997) Functional evidence of excitatory M1 receptors in the rabbit airway. J Pharmacol Exp Ther 281:531–539PubMedGoogle Scholar
  18. Nathanson NM (2000) A multiplicity of muscarinic mechanisms: enough signaling pathways to take your breath away. Proc Natl Acad Sci U S A 97:6245–6247PubMedCentralPubMedCrossRefGoogle Scholar
  19. Nishikibe M, Ohta H, Ishikawa K, Hayama T, Fukuroda T, Noguchi K, Saito M, Kanoh T, Ozaki S, Kamei T, Hara K, William D, Kivlighn S, Krause S, Gabel R, Zingaro G, Nolan N, O’Brien J, Clayton F, Lynch J, Pettibone D, Siegl P (1999) Pharmacological properties of J-104132 (L-753,037), a potent orally active, mixed ETA/ETB endothelin receptor antagonist. J Pharmacol Exp Ther 289:1262–1270PubMedGoogle Scholar
  20. Okazawa A, Cui ZH, Lötvall J, Yoshihara S, Skoogh BE, Kashimoto K, Lindén A (1998) Effect of a novel PACAP-27 analogue on muscarinic airway responsiveness in guinea-pigs in vivo. Eur Respir J 12:1062–1066PubMedCrossRefGoogle Scholar
  21. Patel HJ, Barnes PJ, Takahashi T, Tadjikarimi S, Yacoub MH, Belvisi MG (1995) Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea. Am J Respir Crit Care Med 152:872–878PubMedCrossRefGoogle Scholar
  22. Peták F, Hantos Z, Adamicza A, Asztalos T, Sly PD (1996) Metacholine-induced bronchoconstriction in rats: effects of intravenous vs. aerosol delivery. J Appl Physiol 80:1841–1849PubMedGoogle Scholar
  23. Rees PJ (2002) Tiotropium in the management of chronic obstructive pulmonary disease. Eur Respir J 19:205–206PubMedCrossRefGoogle Scholar
  24. Sarria B, Naline E, Zhang Y, Cortijo J, Molimard M, Moreau J, Therond P, Avenier C, Morcillo EJ (2002) Muscarinic M2 receptors in acetylcholine-isoproterenol functional antagonism in human isolated bronchus. Am J Physiol 283:L1125–L1132Google Scholar
  25. Struckmann N, Schwering S, Wiegand S, Gschnell A, Yamada M, Kummer W, Wess J, Haberberger RV (2003) Role of muscarinic receptor subtypes in the constriction of peripheral airways: studies on receptor deficient mice. Mol Pharmacol 64:1444–1451PubMedCrossRefGoogle Scholar
  26. Tohda Y, Haraguchi R, Itoh M, Ohkawa K, Kubo H, Fukuoka M, Nakajima S (2002) Role of muscarinic receptors in a guinea pig model of asthma. Int Immunopharmacol 2:1521–1527PubMedCrossRefGoogle Scholar
  27. Wale JL, Peták F, Sly PD (1999) Muscarinic blockade of methacholine induced airway and parenchymal lung responses in anaesthetized rats. Thorax 54:531–537PubMedCentralPubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  1. 1.Integrated Physiology & Pharmacology Consulting, LLCPoughkeepsieUSA

Personalised recommendations