| Autor: |
J. Michael Young, Henk Timmerman, Robin Thurmond, Holger Stark, Nigel P. Shankley, Roland Seifert, Jean-Charles Schwartz, Walter Schunack, Pertti Panula, Steve Liu, Roberto Levi, Rob Leurs, Rebecca Hills, Stephen J. Hill, Helmut L. Haas, Ralf Gutzmer, C. Robin Ganellin, Hiroyuki Fukui, Marlon Cowart, Paul Chazot |
| Rok vydání: |
2023 |
| Předmět: |
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| Zdroj: |
IUPHAR/BPS Guide to Pharmacology CITE. 2023 |
| ISSN: |
2633-1020 |
| Popis: |
Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [80, 174]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [80]. 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 [174]. Some agonists at the human H3 receptor display significant ligand bias [183]. 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. adriforant; Phase IIa) [174] and vestibular neuritis (AUV) (SENS-111 (Seliforant, previously UR-63325), entered and completed vestibular neuritis (AUV) Phase IIa efficacy and safety trials, respectively) [217, 8]. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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