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

  • Paul Chazot Durham University https://orcid.org/0000-0002-5453-0379
  • Marlon Cowart Abbott Laboratories
  • Hiroyuki Fukui University of Tokushima
  • C. Robin Ganellin University College London
  • Ralf Gutzmer Hannover Medical School
  • Helmut L. Haas Heinrich Heine University
  • Stephen J. Hill University of Nottingham
  • Rebecca Hills University of Edinburgh
  • Rob Leurs Vrije Universiteit Amsterdam
  • Roberto Levi Cornell University
  • Steve Liu Pfizer
  • Pertti Panula University of Helsinki
  • Walter Schunack Freie Universitat Berlin
  • Jean-Charles Schwartz INSERM
  • Roland Seifert Medical School of Hannover
  • Nigel P. Shankley Johnson & Johnson Pharmaceutical Research & Development
  • Holger Stark Goethe University
  • Robin Thurmond Johnson & Johnson Pharmaceutical Research & Development
  • Henk Timmerman Vrije Universiteit Amsterdam
  • J. Michael Young University of Cambridge


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].
How to Cite
Chazot, P., Cowart, M., Fukui, H., Ganellin, C. R., Gutzmer, R., Haas, H. L., Hill, S. J., Hills, R., Leurs, R., Levi, R., Liu, S., Panula, P., Schunack, W., Schwartz, J.-C., Seifert, R., Shankley, N. P., Stark, H., Thurmond, R., Timmerman, H. and Young, J. M. (2019) “Histamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database”, IUPHAR/BPS Guide to Pharmacology CITE, 2019(4). doi: 10.2218/gtopdb/F33/2019.4.