Synonyms
Antihistamines; Histamine receptor agonists
Definition
Histaminic agonists and antagonists are drugs that mimic or antagonize the actions of histamine at one of its four G-protein-coupled receptors (H1–H4).
Pharmacological Properties
Histamine is a biogenic amine that is widely distributed in the body and is involved in a number of physiological and pathophysiological functions (Hill et al. 1997; Parsons and Ganellin 2006). These include allergic inflammation, cardiovascular regulation, gastric acid secretion, and neuromodulatory functions within the central nervous system (CNS). Histamine is produced by decarboxylation of the amino acid l-histidine and is metabolized by histamine NÏ„-methyltransferase (HMT) and diaminoxidases. In the case of its neurotransmitter role within the CNS, histamine-containing neurons are characterized by a high level of histidine decarboxylase activity and removal of synaptic histamine is mainly via metabolism (as a consequence of HMT activity)....
This is a preview of subscription content, log in via an institution to check access.
References
Arrang JM, Morisset S, Gbahou F (2007) Constitutive activity of the histamine H3 receptor. Trends Pharmacol Sci 28:350–357
Bakker RA, Weiner DM, ter Laak T, Beuming T, Zuiderveld OP, Edelbroek M, Hacksell U, Timmerman H, Brann MR, Leurs R (2004) 8R-Lisuride is a potent stereospecific histamine H1-receptor partial agonist. Mol Pharmacol 65:538–549
Bongers G, Bakker R, Leurs R (2007) Molecular aspects of the histamine H3 receptor. Biochem Pharmacol 73:1195–1204
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 49:253–278
Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (2005) Evaluation of histamine H1-, H2- and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 314:1310–1321
Parsons ME, Ganellin CR (2006) Histamine and its receptors. Br J Pharmacol 147:S127–S135
Sander K, Kottke T, Stark H (2008) Histamine H3 receptor antagonists go to clinics. Biol Pharm Bull 31:2163–2181
Thurmond RL, Desai PJ, Dunford PJ, Fung-Leung WP, Hofsta CL, Jiang W et al (2004) A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 309:404–413
Thurmond RL, Gelfand EW, Dunford PJ (2008) The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov 7:41–53
Zhang M, Thurmand RL, Dunford PJ (2007) The histamine H4 receptor: a novel modulator of inflammatory and immune disorders. Pharmacol Ther 113:594–606
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2014 Springer-Verlag Berlin Heidelberg
About this entry
Cite this entry
Hill, S.J. (2014). Histaminic Agonists and Antagonists. In: Stolerman, I., Price, L. (eds) Encyclopedia of Psychopharmacology. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27772-6_294-2
Download citation
DOI: https://doi.org/10.1007/978-3-642-27772-6_294-2
Received:
Accepted:
Published:
Publisher Name: Springer, Berlin, Heidelberg
Online ISBN: 978-3-642-27772-6
eBook Packages: Springer Reference Biomedicine and Life SciencesReference Module Biomedical and Life Sciences