Serotonin discovery and stepwise disclosure of 5-HT receptor complexity over four decades. Part I. General background and discovery of serotonin as a basis for 5-HT receptor identification

Pharmacological Reports

Volumn 65, Issue 4, 2013, Pages 771-786

  Göthert, Manfred ^a  

^a Institute of Pharmacology and Toxicology   (Germany)

Author keywords

5,7 dihydroxytryptamine; Contemporary Witness Report; Maurice Rapport; Novel type of review; Serotonin discovery; Serotonin neurotoxins; Serotonin receptors; Vittorio Erspamer

Indexed keywords

5,6 DIHYDROXYTRYPTAMINE; 5,7 DIHYDROXYTRYPTAMINE; CATECHOLAMINE; IMIPRAMINE; NEUROTOXIN; NEUROTRANSMITTER; POSTSYNAPTIC RECEPTOR; PRESYNAPTIC RECEPTOR; SEROTONIN; SEROTONIN RECEPTOR;

ALLOSTERISM; BINDING SITE; BODY FLUID; BRAIN MAPPING; CARDIOVASCULAR SYSTEM; CENTRAL NERVOUS SYSTEM FUNCTION; CHEMICAL REACTION; DOG; ENTEROCHROMAFFIN CELL; GASTROINTESTINAL TRACT; GENETIC VARIABILITY; MEDICAL LITERATURE; NONHUMAN; RABBIT; RAT; REVIEW; SEROTONINERGIC SYSTEM; STOMACH MUCOSA;

ANIMALS; CENTRAL NERVOUS SYSTEM; HISTORY, 20TH CENTURY; MODELS, NEUROLOGICAL; MOLLUSCA; NEUROTOXINS; PERIPHERAL NERVOUS SYSTEM; RECEPTORS, SEROTONIN; REVIEW LITERATURE AS TOPIC; SEROTONIN;

EID: 84886526901     PISSN: 22995684     EISSN: 22995684     Source Type: Journal    
DOI: 10.1016/S1734-1140(13)71059-4     Document Type: Review

References (105)

1. Anden NE, Dahlström A, Fuxe K, Larsson K: Mapping out of catecholamine and 5-hydroxytryptamine neurons innervating the telencephalon and diencephalon. Life Sci, 1965, 4, 1275-1279.
2. Barnes NM, Hales TG, Lummis SC, Peters JA: The 5-HT3 receptor - the relationship between structure and function. Neuropharmacology, 2009, 56, 273-284.
3. Barnes NM, Sharp T: Areview of central 5-HT receptors and their function. Neuropharmacology, 1999, 38, 1083-1152.
4. Baumgarten HG, Björklund A, Lachenmayer L, Nobin A, Stenevi U: Long-lasting selective depletion of brain serotonin by 5,6-dihydroxytryptamine. Acta Physiol Scand Suppl, 1971, 373, 1-15.
5. Baumgarten HG, Göthert M Eds: Serotoninenergic neurons and 5-HT receptors in the CNS. Handbook of Experimental Pharmacology, Vol. 129, Springer, Berlin, Heidelberg, New York, 1997, 1-750.
6. BaumgartenHG,GöthertM,HolsteinAF, SchlossbergerHG: Chemical sympathectomy induced by 5,6-dihydroxytryptamine. Z ZellforschMikroskAnat, 1972a, 128, 115-134.
7. Baumgarten HG, Göthert M, Schlossberger HG, Tuchinda P: Mechanism of pressor effect of 5,6- dihydroxytryptamine in pithed rats. Naunyn- Schmiedeberg's Arch Pharmacol, 1972b, 274, 375-384.
8. Baumgarten HG, Grozdanovic Z: Anatomy of the central serotoninergic projection systems. In Serotonergic Neurons and 5-HT receptors in the CNS, Handbook of Experimental Pharmacology, Vol. 129, Eds Baumgarten HG and Göthert M, Springer, Berlin, Heidelberg, New York, 1997, 41-89.
9. Baumgarten HG, Lachenmayer L: 5,7-dihydroxytryptamine: improvement in chemical lesioning of indoleamine neurons in the mammalian brain. Z Zellforsch Mikrosk Anat, 1972, 135, 399-414.
10. Baumgarten HG, Lachenmayer L, Schlossberger HG: Evidence for a degeneration of indoleamine containing nerve terminals in rat brain, induced by 5,6-dihydroxytryptamine. Z ZellforschMikrosk Anat, 1972c, 125, 553-569.
11. Beaudet A, Descarries L: The monoamine innervation of rat cerebral cortex: synaptic and nonsynaptic axon terminals. Neuroscience, 1978, 3, 851-860.
12. Bertler A, Carlsson A, Rosengren E: A method for the fluorimetric determination of adrenaline and noradrenaline in tissues. Acta Physiol Scand, 1958, 44, 273-292.
13. Björklund A, Baumgarten HG, Rensch A: 5,7-Dihydroxytryptamine: improvement of its selectivity for serotonin neurons in the CNS by pretreatment with desipramine. J Neurochem, 1975, 24, 833-835.
14. Bockaert J, Claeysen S, Becamel C, Dumuis A, Marin P: Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation. Cell Tissue Res, 2006, 326, 553-572.
15. Bockaert J, Claeysen S, Compan V, Dumuis A: 5-HT4 receptors: history, molecular pharmacology and brain functions: Neuropharmacology, 2008, 55, 922-931.
16. Bowman RL, Caulfield PA, Udenfriend S: Spectrophotofluorometric assay in the visible and ultraviolet. Science, 1955, 122, 32-33.
17. Carlsson A: A half-century of neurotransmitter research: impact on neurology and psychiatry. Nobel lecture. Chembiochem. 2001, 2, 484-493.
18. Colowick SP: Arda Alden Green, Protein Chemist. Science, 1958, 8, 519-521.
19. Corrodi H, Jonsson G: Fluorescence method for the histochemical demonstration of biogenic monoamines. A review on the methodology. J Histochem Cytochem, 1967, 15, 65-78.
20. Dahlström A, Fuxe K: Evidence for the existence of monoamine-containing neurons in the central nervous system. I. Demonstration of monoamines in the cell bodies of brain stem neurons. Acta Physiol Scand Suppl, 1964a, 232, 1-55.
21. Dahlström A, Fuxe K: Localization of monoamines in the lower brain stem. Experientia, 1964b, 20, 398-399.
22. Erspamer V: Pharmakologische Studien über Enteramin. I. Mitteilung: Uber die Wirkung von Acetonextrakten der Kaninchenmagenschleimhaut auf den Blutdruck und auf isolierte überlebende Organe. Naunyn-Schmiedebergs Arch exp Pathol Pharmakol, 1940a, 196, 343-365.
23. Erspamer V: Pharmakologische Studien über Enteramin. II. Mitteilung: Uber einige Eigenschaften des Enteramins sowie über die Abgrenzung des Enteramins von den anderen kreislaufwirksamen Gewebeprodukten. Naunyn- Schmiedebergs Arch exp Pathol Pharmakol, 1940b, 196, 366-390.
24. Erspamer V: Pharmakologische Studien über Enteramin. III. Mitteilung: Uber das Vorhandensein eines enteraminähnlichen Stoffes in Milzextrakten. Naunyn- Schmiedebergs Arch exp Pathol Pharmakol, 1940c, 196, 391-407.
25. Erspamer V: Pharmakologische Studien über Enteramin. IV. Mitteilung: Uber die Inaktivierung von Enteramin durch tierisches Gewebe. Naunyn-Schmiedebergs Arch Exp Pathol Pharmakol, 1942, 200, 43-59.
26. Erspamer V: Pharmacology of indole-Alkylamines. Pharmacol Rev, 1954, 6, 425-487.
27. Erspamer V, Asero B: Identification of enteramine, the specific hormone of the enterochromaffin cell system, as 5-hydroxytryptamine. Nature, 1952, 169, 800-801.
28. Erspamer V, Ghiretti F: The action of enteramine on the heart of molluscs. J Physiol, 1951, 115, 470-481.
29. Erspamer V, Vialli M: Ricerche sul secreto delle cellule enterocromaffini. Boll Soc Med-chir Pavia, 1937, 51, 357-363.
30. Falck B, Hillarp N. A, Thieme G, Torp A: Fluorescence of catechol amines and related compounds condensed with formaldehyde. J Histochem Cytochem, 1962, 10, 348-354.
31. Filip M, Bader M: Overview on 5-HT receptors and their role in physiology and pathology of the central nervous system. Pharmacol Rep, 2009, 61, 761-777.
32. Fillion GM, Rousselle JC, Fillion MP, Beaudoin DM, Goiny MR, Deniau JM, Jacob JJ: High-Affinity binding of [3H]5-hydroxytryptamine to brain synaptosomal membranes: comparison with [3H]lysergic acid diethylamide binding. Mol Pharmacol, 1978, 14, 50-59.
33. Fink KB, Göthert M: 5-HT receptor regulation of neurotransmitter release. Pharmacol Rev, 2007, 59, 360-417.
34. Folk GE, Mora F: Serotonin and the last great bioassays. J Biol Sci, 2003, 3, 951-960.
35. Fone KC: An update on the role of the 5-hydroxytryptamine 6 receptor in cognitive function. Neuropharmacology, 2008, 55, 1015-1022.
36. Fozard JR, Ed: The peripheral actions of 5-hydroxytryptamine. Oxford University Press, Oxford, New York, Tokyo, 1989, 1-410.
37. Frohlich ED, Dustan HP, Bumpus FM: Irvine H, Page: 1901-1991. The celebration of a leader. Hypertension, 1991, 18, 443-445.
38. Fuder H, Muscholl E: Heteroreceptor-mediated modulation of noradrenaline and acetylcholine release from peripheral nerves. Rev Physiol Biochem Pharmacol, 1995, 126, 265-412.
39. Fuller RW: Structure-Activity relationships among the halogenated amphetamines. Ann NY Acad Sci, 1978a, 305, 147-157.
40. Fuller RW: Neurochemical effects of serotonin neurotoxins: an introduction. Ann NYAcad Sci, 1978b, 305, 178-181.
41. Fuller RW: Effects of p-chloroamphetamine on brain serotonin neurons. Neurochem Res, 1992, 17, 449-456.
42. Fuller RW, Perry KW, Molloy BB: Reversible and irreversible phases of serotonin depletion by 4-chloroamphetamine. Eur J Pharmacol, 1975, 33, 119-124.
43. Gaddum JH, Picarelli ZP: Two kinds of tryptamine receptor. Br J Pharmacol, 1957, 12, 134-139.
44. GershonMD, Tack J: The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gastroenterology, 2007, 132, 397-414.
45. Gifford R: Profiles in cardiology. Irvine H. Page. Clin Cardiol, 1987, 10, 68-69.
46. Göthert M: Effects of halothane on the sympathetic nerve terminal of the rabbit heart. Difference in membrane actions of halothane and tetracaine. Naunyn- Schmiedeberg's Arch Pharmacol, 1974, 286, 125-143.
47. Göthert M: Modulation of serotonin release in the brain via presynaptic receptors. Trends Pharmacol Sci, 1982, 3, 437-440.
48. Göthert M: Presynaptic serotonin receptors in the central nervous system. Ann NY Acad Sci, 1990, 604, 102-12.
49. GöthertM: 5-Hydroxytryptamine receptors. An example for the complexity of chemical transmission of information in the brain. Arzneimittelforschung, 1992, 42, 238-246.
50. Göthert M: Development of 5-HT receptor complexity within 39 years - from drugs as tools to new therapeutics. Pharmacol Rep, 2010, 62, 3.
51. Göthert M, Dührsen U: Effects of 5-hydroxytryptamine and related compounds on the sympathetic nerves of the rabbit heart. Naunyn-Schmiedeberg's Arch Pharmacol, 1979, 308, 9-18.
52. Göthert M, Dührsen U, Rieckesmann JM: Ethanol, anaesthetics and other lipophilic drugs preferentially inhibit 5-hydroxytryptamine and acetylcholine-induced noradrenaline release from sympathetic nerves. Arch Int Pharmacodyn Ther, 1979, 242, 196-209.
53. Göthert M, Thielecke G: Inhibition by ethanol of noradrenaline output from peripheral sympathetic nerves: possible interaction of ethanol with neuronal receptors. Eur J Pharmacol, 1976, 37, 321-328.
54. Göthert M, Tuchinda P, Baumgarten HG: Pressor effect of indolethylamines. Eur J Pharmacol, 1973, 21, 242-245.
55. Green AR: Neuropharmacology of 5-hydroxytryptamine. Br J Pharmacol, 2006, 147, Suppl 1, S145-S152.
56. Green AR: Gaddum and LSD: the birth and growth of experimental and clinical neuropharmacology research on 5-HT in the UK. Br J Pharmacol, 2008, 154, 1583-1599.
57. Gross G, Göthert M, Ender HP, Schumann HJ: [3H]Imipramine binding sites in the rat brain. Selective localization on serotoninergic neurones. Naunyn-Schmiedeberg's Arch Pharmacol, 1981, 317, 310-314.
58. Hannon J, Hoyer D: Molecular biology of 5-HT receptors. Behav Brain Res, 2008, 195, 198-213.
59. Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP: International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol Rev, 1994, 46, 157-203.
60. Hoyer D, Hannon JP, Martin GR: Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav, 2002, 71, 533-554.
61. Jacoby JH, Lytle LD Eds.: Serotonin Neurotoxins. Ann NY Acad Sci, 1978, 1-702.
62. Koe BK, Weissman A: p-Chlorophenylalanine: a specific depletor of brain serotonin. J Pharmacol Exp Ther, 1966, 154, 499-516.
63. Langer SZ, Moret C, Raisman R, Dubocovich ML, Briley M: High-Affinity [3H]imipramine binding in rat hypothalamus: association with uptake of serotonin but not of norepinephrine. Science, 1980, 210, 1133-1135.
64. Ludwig C, Schmidt A: Das Verhalten der Gase, welche mit dem Blut durch den reizbaren Säugethiermuskel strömen. Arbeiten aus der physiologischen Anstalt zu Leipzig, 1868, 3, 1-61.
65. Malinowska B, Göthert M, Przegaliñski E, Schlicker E: Report on the German-Polish symposium " Thirty years of cooperation between German and Polish pharmacologists. New perspectives in the Common Europe" , Bialowiea, September 2003, 18-21. Pol J Pharmacol, 2003, 55, 807-810.
66. Martin GR, Eglen RM, Hoyer D, Hamblin MW, Yocca F: Advances in serotonin receptor research: molecular biology, signal transduction, and therapeutics. Ann NY Acad Sci, 1998, 861, 1-297.
67. Miner WD, Sanger GJ: Inhibition of cisplatin-induced vomiting by selective 5-hydroxytryptamine M-receptor antagonism. Br J Pharmacol 1986, 88, 497-499.
68. Mutt V: An appreciation of the work of Vittorio Erspamer. Peptides, 1981, 2, Suppl, 3-6.
69. Negri L: Vittorio Erspamer (1909-1999). Med Secoli, 2006, 18, 97-113.
70. Nichols DE, Nichols CD: Serotonin receptors. Chem Rev, 2008, 108, 1614-1641.
71. O'Connor JM: Uber den Adrenalingehalt des Blutes. Arch exp Pathol Pharmakol (founding name of " Naunyn- Schmiederberg's Arch Pharmacol" ), 1912, 67, 195-232.
72. Peroutka SJ, Snyder SH: Multiple serotonin receptors: differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol. Mol Pharmacol, 1979, 16, 687-699.
73. Pineyro G, Blier P: Autoregulation of serotonin neurons: role in antidepressant drug action. Pharmacol Rev, 1999, 51, 533-591.
74. Pithadia AB, Jain SM: 5-Hydroxytryptamine receptor subtypes and their modulators with therapeutic potentials. J Clin Med Res, 2009, 1, 72-80.
75. Pletscher A, Shore PA, Brodie BB: Serotonin release as a possible mechanism of reserpine action. Science, 1955, 122, 374-375.
76. Raisman R, Briley M, Langer SZ: Specific tricyclic antidepressant binding sites in rat brain. Nature, 1979, 281, 148-150.
77. Raisman R, Briley MS, Langer SZ: Specific tricyclic antidepressant binding sites in rat brain characterised by high-Affinity [3H]imipramine binding. Eur J Pharmacol, 1980, 61, 373-380.
78. Rapport MM: Serum vasoconstrictor (serotonin). V. The presence of creatinine in the complex: a proposed structure of the vasoconstrictor principle. J Biol Chem, 1949, 180, 961-969.
79. Rapport MM: The discovery of serotonin. Perspect Biol Med, 1997, 40, 260-273.
80. Rapport MM, Green AA, Page IH: Partial purification of the vasoconstrictor in beef serum. J Biol Chem, 1948a, 174, 735-741.
81. Rapport MM, Green AA, Page IH: Crystalline serotonin. Science, 1948b, 108, 329-330.
82. Renda TG: Vittorio Erspamer: a true pioneer in the field of bioactive peptides. Peptides, 2000, 21, 1585-1586.
83. Rojas C, Slusher B S: Pharmacological mechanisms of 5-HT3 and tachykinin NK1 receptor antagonism to prevent chemotherapy-induced nausea and vomiting. Eur J Pharmacol, 2012, 684, 1-7.
84. Schlossberger HG: Synthesis and chemical properties of some indole derivatives. Ann NY Acad Sci, 1978, 305, 25-35.
85. Schlossberger HG, Kuch H: Sythese des 5,6-Dihydroxytryptamins. Chem Ber, 1960, 93, 1318-1323.
86. Starke K: Selectivity of ethanol on ligand-gated ion channels. Trends Pharmacol Sci, 1991, 12, 182.
87. Starke K: A history of Naunyn-Schmiedeberg's Archives of Pharmacology. Naunyn-Schmiedeberg's Arch Pharmacol, 1998, 358, 1-109.
88. Starke K, Göthert M, Kilbinger H: Modulation of neurotransmitter release by presynaptic autoreceptors. Physiol Rev, 1989, 69, 864-989.
89. Steranka LR, Sanders-Bush E: Long-term reduction of brain serotonin by p-chloroamphetamine: effects of inducers and inhibitors of drug metabolism. J Pharmacol Exp Ther, 1978, 206, 460-467.
90. Thoenen H, Tranzer JP: Chemical sympathectomy by selective destruction of adrenergic nerve endings with 6-hydroxydopamine. Naunyn-Schmiedebergs Arch Pharmakol, 1968, 261, 271-288.
91. Timmermans PB, Thoolen MJ: Autoreceptors in the central nervous system. Med Res Rev, 1987, 7, 307-332.
92. Törk I: Anatomy of the serotonergic system. Ann NY Acad Sci, 1990, 600, 9-34.
93. Trendelenburg P: Bestimmung des Adrenalingehaltes im normalen Blut sowie beim Abklingen der Wirkung einer einmaligen intravenösen Adrenalininjektion mittels physiologischer Messmethode. Arch exp Pathol Pharmakol (founding name of " Naunyn-Schmiederberg's Arch Pharmacol" ), 1910, 63, 161-176.
94. Twarog BM: Responses of a molluscan smooth muscle to acetylcholine and 5-hydroxytryptamine. J Cell Physiol, 1954, 44, 141-163.
95. Twarog BM, Page IH: Serotonin content of some mammalian tissues and urine and a method for its determination. Am J Physiol, 1953, 175, 157-161.
96. Vialli M, Erspamer V: Caratteristiche istochimiche delle cellule enterocromaffini. Boll Soc Ital Biol Sper, 1933, 8, 885-887.
97. Vizi ES, Kiss JP: Neurochemistry and pharmacology of the major hippocampal transmitter systems: synaptic and nonsynaptic interactions. Hippocampus, 1998, 8, 566-607.
98. Walstab J, Rappold G, Niesler B: 5-HT3 receptors: role in disease and target of drugs. Pharmacol Ther, 2010, 128, 146-169.
99. Welsh JH: Excitation of the heart of Venus mercenaria. Naunyn-Schmiedebergs Arch Exp Pathol Pharmakol, 1953, 219, 23-29.
100. Welsh JH, Taub R: The action of acetylcholine antagonists on the heart of Venus mercenaria. Br J Pharmacol Chemother, 1953, 8, 327-333.
101. Wesolowska A: Potential role of the 5-HT6 receptor in depression and anxiety: an overview of preclinical data. Pharmacol Rep, 2010, 62, 564-577.
102. Whitaker-Azmitia PM: The discovery of serotonin and its role in neuroscience. Neuropsychopharmacology, 1999, 21, 2S-8S.
103. Whitaker-Azmitia PM, Peroutka J: The neuropharmacology of serotonin. Ann NY Acad Sci, 1990, 600, 1-715.
104. Wolfarth S, Bijak M, Diak J, Maj J, Szczepanik J: 20 years of collaboration between Polish and German pharmacologists (Polish-German). Institute of Pharmacology of the Polish Academy of Sciences, Kraków, 1994, 1-259.
105. Zifa E, Fillion G: 5-Hydroxytryptamine receptors. Pharmacol Rev, 1992, 44, 401-458.