IUPHAR/BPS Guide to Pharmacology CITE

Histamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

Paul Chazot1, Marlon Cowart2, Hiroyuki Fukui3, C. Robin Ganellin4, Ralf Gutzmer5, Helmut L. Haas6, Stephen J. Hill7, Rebecca Hills8, Rob Leurs9, Roberto Levi10, Steve Liu11, Pertti Panula12, Walter Schunack13, Jean-Charles Schwartz14, Roland Seifert15, Nigel P. Shankley16, Holger Stark17, Robin Thurmond16, Henk Timmerman9 and J. Michael Young18
  1. Durham University, UK
  2. Abbott Laboratories, USA
  3. University of Tokushima, Japan
  4. University College London, UK
  5. Hannover Medical School, Germany
  6. Heinrich Heine University, Germany
  7. University of Nottingham, UK
  8. University of Edinburgh, UK
  9. Vrije Universiteit Amsterdam, The Netherlands
  10. Cornell University, USA
  11. Pfizer, UK
  12. University of Helsinki, Finland
  13. Freie Universitat Berlin, Germany
  14. INSERM, France
  15. Medical School of Hannover, Germany
  16. Johnson & Johnson Pharmaceutical Research & Development, USA
  17. Goethe University, Germany
  18. University of Cambridge, UK


Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [75, 163]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [75]. The human and rat H3 receptor genes are subject to significant splice variance [12]. The potency order of histamine at histamine receptor subtypes is H3 = H4 > H2 > H1 [163]. Some agonists at the human H3 receptor display significant ligand bias [171]. 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) [163] and vestibular neuritis (AUV) (SENS-111 (Seliforant, previously UR-63325), entered and completed vestibular neuritis (AUV) Phase IIa efficacy and safety trials, respectively) [205, 8].


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Database links

Histamine receptors
Introduction to Histamine receptors
            H1 receptor
            H2 receptor
            H3 receptor
            H4 receptor


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