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Histamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
- Source :
- IUPHAR/BPS Guide to Pharmacology CITE. 2019
- Publication Year :
- 2019
- Publisher :
- Edinburgh University Library, 2019.
-
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].
- Subjects :
- 0303 health sciences
Allergy
Pitolisant
business.industry
Pharmacology
Ligand (biochemistry)
medicine.disease
Cetirizine
3. Good health
Ranitidine
03 medical and health sciences
chemistry.chemical_compound
Histamine receptor
0302 clinical medicine
chemistry
030220 oncology & carcinogenesis
Medicine
Histamine H3 receptor
business
Histamine
030304 developmental biology
medicine.drug
Subjects
Details
- ISSN :
- 26331020
- Volume :
- 2019
- Database :
- OpenAIRE
- Journal :
- IUPHAR/BPS Guide to Pharmacology CITE
- Accession number :
- edsair.doi...........909fa860575554046685bc146f90b913