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• W3176552657 abstract "Histamine has long been known to be an inflammatory mediator in allergic and associated diseases. Following their discovery in the 1930s, H1-antihistamines were first introduced into clinical practice in the 1940s. Since that time three further histamine receptors, H2, H3 and H4, have been discovered and drugs to prevent their effects introduced. H1- antihistamines, the mainstay of treatment for urticaria and allergic rhinitis, act as inverse agonists rather than antagonists of histamine H1-receptors which are members of the G-protein family. The older first generation H1- antihistamines penetrate readily into the brain to cause sedation, drowsiness, fatigue and impaired concentration. Their use should be discouraged. The newer second-generation H1-antihistamines are safer, cause less sedation and are more efficacious. Two more recent H1- antihistamines, fexofenadine and bilastine, do not enter the brain as they are substrates for p-glycoprotein, a proton pump in the blood brain barrier. The H2-receptor is also highly expressed in many cells where it is mainly anti-inflammatory. Its primary role appears to be in stimulating gastric acid secretion. The H3-receptor exclusively expressed in neurones. Perhaps the most exciting research, which is at presence in its infancy, is in H4-receptors which are present on many cells and has proinflammatory effects." @default.
• W3176552657 created "2021-07-05" @default.
• W3176552657 creator A5005311406 @default.
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• W3176552657 creator A5091156366 @default.
• W3176552657 date "2022-01-01" @default.
• W3176552657 modified "2023-10-16" @default.
• W3176552657 title "The Pharmacology of Antihistamines" @default.
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