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Target intelligence / Profile preview
Histamine Receptor H1 (H1R)
- Target
- H1R
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The histamine H1 receptor (H1R) is a G protein-coupled receptor activated by histamine. It plays a crucial role in allergic reactions, inflammation, and neurotransmission. Activation leads to increased intracellular calcium levels and various physiological effects, including smooth muscle contraction and increased vascular permeability. Antihistamines targeting H1R are used for allergy relief, with first-generation drugs causing sedation and second-generation drugs being less sedating. Recent research suggests a potential role in SARS-CoV-2 infection.
- Other names
- HRH1
02
Mechanism of action
Antagonism of histamine binding to H1R, leading to decreased downstream signaling via Gq/11 proteins and reduced IP3/DAG/Ca2+ production.
03
Biological functions
Signal transductionSmooth muscle contractionRegulation of vascular permeabilitySensory nerve stimulationRegulation of inflammatory processesSleep-wake cycle regulationImmune responseNeurotransmissionPhysiological regulation
04
Disease associations
Allergic reactionsAllergic rhinitisAsthmaAtopic dermatitisConjunctivitisCOVID-19 (potential role)
05
Safety considerations
First-generation antihistamines: Sedation/drowsiness due to CNS penetration.Potential off-target effects of antihistamines.
06
Interacting drugs
Antihistamines (First-generation)
2 more in the full profile.
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