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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).

Overview

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Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [15,37]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [15]. The human and rat H3 receptor genes are subject to significant splice variance [3]. The potency order of histamine at histamine receptor subtypes is H3 = H4 > H2 > H1 [37]. Some agonists at the human H3 receptor display significant ligand bias [41]. 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) [37] and vestibular neuritis (AUV) (SENS-111 (Seliforant, previously UR-63325), entered and completed vestibular neuritis (AUV) Phase IIa efficacy and safety trials, respectively) [1,47].

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 (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. Br J Pharmacol. 176 Issue S1: S21-S141.