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Questions: What are the pharmacologic actions, clinical uses and adverse effects of H1 receptor antagonists and H2 receptor antagonists? Chapter 34 Drugs Affecting Autacoids影响自体活性物质的药物 School of Pharmaceutical Sciences Chen Nana Autacoids have been described as local hormones. They are grouped together in large part because they participate, at least in some settings, in physiological or pathophysiological response to injury. Autacoids includs : prostaglandins histamine 5-hydroxytryptamine leukotrienes vasoactive peptides, etc Histamine and Antihistamine Drugs 组胺和抗组胺药 I. Histamine(组胺) Histamine is an autacoid and released mainly from mast cells or basophils Marked species variation is observed, but in humans histamine is an important mediator of immediate allergic and inflammatory reactions; has an important role in gastric acid secretion; and functions as a neurotransmitter and neuromodulator Most tissue histamine is bound in granules in mast cells or basophils The bound form of histamine is biologically inactive, but many stimuli can trigger the release of mast cell histamine, allowing the free amine to exert its actions on surrounding tissues Mast cells are especially rich at sites of potential tissue injury—nose, mouth, and feet; internal body surfaces; and blood vessels Non-mast cell histamine is found in several tissues, including the brain, where it functions as a neurotransmitter. Another important site of histamine storage and release is the enterochromaffin-like (ECL) cell of the fundus of the stomach. These cells release histamine to activate the acid-producing parietal cells of the mucosa. Histamine exerts its biologic actions by combining with specific cellular receptors: H1 receptor H2 receptor H3 receptor H4 receptor The structures of the H1 and H2 receptors differ significantly and appear to be more closely related to muscarinic and 5-HT1 receptors, respectively, than t
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