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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 .
Cetirizine crosses the blood–brain barrier only slightly, and for this reason, produces minimal sedation compared to many other antihistamines. [29] A positron emission tomography (PET) study found that brain occupancy of the H 1 receptor was 12.6% for 10 mg cetirizine, 25.2% for 20 mg cetirizine, and 67.6% for 30 mg hydroxyzine. [30]
Histamine receptors are proteins that bind with histamine, a neurotransmitter involved in various physiological processes. There are four main types: H1, H2, H3, and H4. H1 receptors are linked to allergic responses, H2 to gastric acid regulation, H3 to neurotransmitter release modulation, and H4 to immune system function.
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It is classified as a second-generation antihistamine and works by blocking histamine H 1-receptors. [6] [3] Levocetirizine was approved for medical use in the United States in 2007, [3] and is available as a generic medication. [4] In 2022, it was the 152nd most commonly prescribed medication in the United States, with more than 3 million ...
These agents also commonly have action at α-adrenergic receptors and/or 5-HT receptors. This lack of receptor selectivity is the basis of the poor tolerability profile of some of these agents, especially when compared with the second-generation H 1-antihistamines. Patient response and occurrence of adverse drug reactions vary greatly between ...
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 ...
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