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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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].


Targets of relevance to immunopharmacology are highlighted in blue

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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Further reading

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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 24/03/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=33.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: G protein-coupled receptors. Br J Pharmacol. 174 Suppl 1: S17-S129.