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Target intelligence / Profile preview
Histamine H1 Receptor (H1R)
- Target
- H1R
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The Histamine H1 receptor is a ubiquitously expressed GPCR essential for mediating immediate hypersensitivity reactions—including most classic allergy symptoms—as well as playing roles in neurophysiology related to arousal/wakefulness cycles within the CNS. Its pharmacological blockade underpins one of medicine’s most common therapeutic strategies against allergies.
- Other names
- HRH1
02
Mechanism of action
Inverse agonists that stabilize the inactive state of the receptor.
03
Biological functions
Signal transductionSmooth muscle contractionRegulation of vascular permeabilityNeurotransmissionImmune responseAllergic inflammationSleep-wake cycle regulation
04
Disease associations
Allergic rhinitisUrticariaConjunctivitisAtopic dermatitisAsthmaInflammation
05
Safety considerations
Sedation (first-generation antihistamines)May not fully control all aspects of acute pruritus or severe atopic dermatitis/allergic asthma
06
Interacting drugs
Doxepin
2 more in the full profile.
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