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Azelastine, sold under the brand name Astelin among others, is a H 1 receptor-blocking medication primarily used as a nasal spray to treat allergic rhinitis (hay fever) and as eye drops for allergic conjunctivitis. [5] [6] Other uses may include asthma and skin rashes for which it is taken by mouth. [7]
H 1 antagonists, also called H 1 blockers, are a class of medications that block the action of histamine at the H 1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines ; other agents may have antihistaminergic action but are ...
H 1-antihistamines work by binding to histamine H 1 receptors in mast cells, smooth muscle, and endothelium in the body as well as in the tuberomammillary nucleus in the brain. Antihistamines that target the histamine H 1-receptor are used to treat allergic reactions in the nose (e.g., itching, runny nose, and
The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand. [1] [2] Histamine is a neurotransmitter involved in various physiological processes. There are four main types of histamine receptors: H1, H2, H3, and H4.
The H 1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is activated by the biogenic amine histamine . It is expressed in smooth muscles , on vascular endothelial cells , in the heart, and in the central nervous system .
H 1-receptor antagonists are competitive inhibitor of histamine receptor H 1 and are used to treat allergies. This group is often referred simply as antihistamines . Wikimedia Commons has media related to H1 receptor antagonists .
In addition, subjective sleepiness correlated well with the brain H 1 receptor occupancy. [45] PET studies with antihistamines have found that brain H 1 receptor occupancy of more than 50% is associated with a high prevalence of somnolence and cognitive decline , whereas brain H 1 receptor occupancy of less than 20% is considered to be non ...
Diphenhydramine, while traditionally known as an antagonist, acts primarily as an inverse agonist of the histamine H 1 receptor. [70] It is a member of the ethanolamine class of antihistaminergic agents. [53] By reversing the effects of histamine on the capillaries, it can reduce the intensity of allergic symptoms.