IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F33/2019.4
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
- Durham University, UK
- Abbott Laboratories, USA
- University of Tokushima, Japan
- University College London, UK
- Hannover Medical School, Germany
- Heinrich Heine University, Germany
- University of Nottingham, UK
- University of Edinburgh, UK
- Vrije Universiteit Amsterdam, The Netherlands
- Cornell University, USA
- Pfizer, UK
- University of Helsinki, Finland
- Freie Universitat Berlin, Germany
- INSERM, France
- Medical School of Hannover, Germany
- Johnson & Johnson Pharmaceutical Research & Development, USA
- Goethe University, Germany
- University of Cambridge, UK
Abstract
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].
Contents
This is a citation summary for Histamine receptors in the
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Database links
Histamine receptors
http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=33
Introduction to Histamine receptors
http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=33
Receptors
H1 receptor
http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=262
H2 receptor
http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=263
H3 receptor
http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=264
H4 receptor
http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=265
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