Histamine receptors C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

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Overview

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Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [14,36]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [14]. The human and rat H3 receptor genes are subject to significant splice variance [2]. The potency order of histamine at histamine receptor subtypes is H3 = H4 > H2 > H1 [36]. Some agonists at the human H3 receptor display significant ligand bias [40]. Antagonists of all 4 histamine receptors have clinical uses: H1 antagonists for allergies (e.g. cetirizine), H2 antagonists for acid-reflux diseases (e.g. ranitidine), H3 antagonists for narcolepsy (e.g. pitolisant/WAKIX; Registered) and H4 antagonists for atopic dermatitis (e.g. ZPL-3893787; Phase IIa) [36].

Receptors

H1 receptor C Show summary » More detailed page

H2 receptor C Show summary » More detailed page

H3 receptor C Show summary » More detailed page

H4 receptor C Show summary » More detailed page

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Paul Chazot, Rob Leurs, Stephen J. Hill, Hiroyuki Fukui, C. Robin Ganellin, Helmut L. Haas, Roberto Levi, Walter Schunack, Jean-Charles Schwartz, Nigel P. Shankley, Henk Timmerman, J. Michael Young, Rebecca Hills. Histamine receptors. Accessed on 25/11/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=33.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Davenport AP, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors. Br J Pharmacol. 172: 5744-5869.