Abstract
In this introductory chapter, we revisit some of the landmarks in the history of histamine research. Since histamine was first synthesized (1907) and isolated as a bacterial contaminant of an extract of ergot (1910), the elucidation of its role in health and disease and its molecular mechanism of action have been continuous, reflecting the application of advances in scientific knowledge, technology and therapeutics over the last 100 years.1 It appears that the research will continue indefinitely as the nature of the problem is inherently fractal. First, there was a single chemical entity, described in terms of state-of-the-art, two-dimensional projections of structures introduced by Fischer in 1891, and an idea that such potent chemicals produced their effects on biological systems as a consequence of an exquisite interaction with a receptive substance, the revolutionary concept of (1905).2 Today, we recognize four receptor subtypes with multiple activation states and multiple coupling to intracellular effector systems, so that we are no longer able to reliably and in all instances classify compounds interacting with the histamine receptors simply as agonists or antagonists. The complexity is potentially overwhelming, but the promise of value to patients beyond that already provided by the first approved generations of histamine receptor blockers is a compelling driver.
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References
Dale HH. Adventures in Physiology. Pergamon Press, Ltd., 1953.
Langley JN. On the reaction of cells and of nerve endings to certain poisons, chiefly as regards the reaction of striated muscle to nicotine and to curate. J Physiol 1905; 33:374–413.
Delvincourt R. Vie et oeuvre de Charles Tanret. Thesis d’Universite Paris 1980; 5:548.
Barger G, Dale HH. 4-b-Aminoethylglyoxaline (b-Aminazolylethylamine) and the other active principles of ergot. J Chem Soc Trans 1910; 97:2592–2595.
Windhaus A, Vogt W. Synthese des imidazolyl-athylamins. Ber Dtsch Chem Ges 1907; 40:3691–3695
Dale HH, Laidlaw PP. The physiological action of b-iminazolyethylamine. J Physiol 1910; 16(5):318–344.
Best CH, Dale HH, Dudley HW et al. The nature of the vaso-dilator constituents of certain tissue extracts. J Physiol 1927; 62(4):397–417.
Bovet D. Introduction to antihistamine agents and antergan derivative. Ann NY Acad Sci 1950; 50(9):1089–1126.
Parsons E, Ganellin CG. Histamine and its receptors. Br J Pharmacol 2006; 147:S127–S135.
Wells J, Morris H, HB. B et al. Observations on the nature of antagonism of histamine by β-dimethylaminoethyl bezhydryl ether. J Pharmacol Exp Ther 1945; 85:122–128.
Folkow B, Heger K, Kahlson G. Observations on reactive hyperaemia as related to histamine on drugs antagonising vasodilation induced by histamine and on vasodilator properties of adenosine triphosphate. Acta Physiol Scan 1948; 15:264–278.
Aranlakshan O, Schild H. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother 1959; 14:48–58.
Trendelenburg U. The action of histamine and 5-hydroxytryptamine on isolated mammalian atria. J Pharmacol Exp Ther 1960; 130(4):450–460.
Ash A, Schild H. Receptors mediating some actions of histamine. Br J Pharmacol Chemother 1966; 27(2):427–439.
Black J. A personal view of pharmacology. Annu Rev Pharmacol Toxicol 1996; 36:1–33.
Black J, Duncan W, Durant C et al. Definition and antagonism of histamine H2-receptors. Nature 1972; 236:385–390.
Arrang J, Garbarg M, Schwartz J. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 1983; 302(5911):832–837.
Trzeciakowski JP. Inhibition of guinea pig ileum contractions mediated by a class of histamine receptor resembling the H3 subtype. J Pharmacol Exp Ther 1987; 243(3):874–880.
Raible D, Lenahan T, Fayvilevich Y et al. Pharmacologic characterization of a novel histamine receptor on human eosinophils. Am J Respir Crit Care Med 1996; 149(6): 1506–1511.
Thurmond RL, Gelfand EW, Dunford PJ. The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov 2008; 7(1):41–53.
Gantz I, Schaffer M, DelValle J et al. Molecular cloning of a gene encoding the histamine H2 receptor. Proc Natl Acad Sci USA 1991; 88(2):429–433.
Libert F, Parmentier M, Lefort A et al. Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science 1989; 244(4904):569–572.
Ganz PR et al. Molecular cloning of the human histamine H2 receptor. Biochem Biophys Res Comm 1991; 178:1386
Ruat M, Traiffort E, Arrang J-M et al. Cloning and tissue expression of a rat histamine H2-receptor gene. Biochem Biophys Res Commun 1991; 179(3):1470–1478.
Yamashita M, Fukui H, Sugama K et al. Expression cloning of a cDNA encoding the bovine histamine H1 receptor. Proc Natl Acad Sci USA 1991; 88(24): 11515–11519.
Debacker MD, Gommeren W, Moereels H et al. Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. Biochem Biophys Res Commun 1993; 197(3):1601–1608.
Fujimoto K, Horio Y, Sugama K et al. Genomic cloning of the rat histamine H1 receptor. Biochem Biophys Res Commun 1993; 190(1):294–301.
Lovenberg TW, Roland BL, Wilson SJ et al. Accelerated communication: cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol 1999; 55(6):1101–1107.
Morse KL, Behan J, Laz TM et al. Cloning and characterization of a novel human histamine receptor. J Pharmacol Exp Ther 2001; 296(3):1058–1066.
Lovenberg TW, Pyati J, Chang H et al. Cloning of rat histamine H3 receptor reveals distinct species pharmacological profiles. J Pharmacol Exp Ther 2000; 293(3):771–778.
Chen J, Liu C, Lovenberg TW. Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol 2003; 467(1–3):57–65.
Nakamura T, Itadani H, Hidaka Y et al. Molecular cloning and characterization of a new human histamine receptor, HH4R. Biochem Biophys Res Commun 2000; 279(2):615–620.
Nguyen T, Shapiro DA, George SR et al. Discovery of a novel member of the histamine receptor family. Mol Pharmacol 2001; 59(3):427–433.
Oda T, Morikawa N, Saito Y et al. Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes. J Biol Chem 2000; 275(47):36781–36786.
Liu C, Ma X-J, Jiang X et al. Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol Pharmacol 2001; 59(3):420–426.
Rall TW, Sutherland EW. Formation of a cyclic adenine ribonucleotide by tissue particles. J Biol Chem 1958; 232(2):1065–1076.
Karppanen H, Westermann E. Increased production of cyclic AMP in gastric tissue by stimulation of histamine2 (H2)-receptors. Naunyn Schmiedebergs Arch Pharmacol 1973; 279(1):83–87.
Gillespie E, Lichtenstein L. Pharmacologic control of IgE-mediated histamine release from human leukocytes. Int Arch Allergy Appl Immunol 1973; 45(1):95–97.
Li H, Choe N, Wright D et al. Histamine provokes turnover of inositol phospholipids in guinea pig and human airway epithelial cells via an H1-receptor/G protein-dependent mechanism. Am J Respir Cell Mol Biol 1995; 12(4):416–424.
Gantz I, Munzert G, Tashiro T et al. Molecular cloning of the human histamine H2 receptor. Biochem Biophys Res Commun 1991; 178(3):1386–1392.
Maruko T, Nakahara T, Sakamoto K et al. Involvement of the βγ subunits of G proteins in the cAMP response induced by stimulation of the histamine H1 receptor. Naunyn Schmiedebergs Arch Pharmacol 2005; 372(2):153–159.
Yanai K, Son LZ, Endou M et al. Behavioural characterization and amounts of brain monoamines and their metabolites in mice lacking histamine H1 receptors. Neuroscience 1998; 87(2):479–487.
Kobayashi T, Tonai S, Ishihara Y et al. Abnormal functional and morphological regulation of the gastric mucosa in histamine H2 receptor-deficient mice. J Clin Invest 2000; 105(12):1741–1749.
Clark EA, Hill SJ. Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTP[gamma][S]binding to pertussis toxin. Eur J Pharmacol 1996; 296(2):223–225.
Toyota H, Dugovic C, Koehl M et al. Behavioral characterization of mice lacking histamine H3 receptors. Mol Pharmacol 2002; 62(2):389–397.
Hofstra CL, Desai PJ, Thurmond RL et al. Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells. J Pharmacol Exp Ther 2003; 305(3):1212–1221.
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Figueroa, K., Shankley, N. (2010). One Hundred Years of Histamine Research. In: Thurmond, R.L. (eds) Histamine in Inflammation. Advances in Experimental Medicine and Biology, vol 709. Springer, Boston, MA. https://doi.org/10.1007/978-1-4419-8056-4_1
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DOI: https://doi.org/10.1007/978-1-4419-8056-4_1
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