Antihistamines and Itch
Antihistamines and Itch
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DOI：
10.1007/978-3-662-44605-8_15
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发表时间：
2015-01-01
期刊：
影响因子：
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通讯作者：
Greenspan, Andrew J.
中科院分区：
文献类型：
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作者：
Thurmond, Robin L.;Kazerouni, Kayvan;Greenspan, Andrew J.
组胺是人体中最具特征的促炎原之一。已知其在与荨麻疹相关的瘙痒以及眼和鼻过敏反应中发挥作用。组胺通过四种受体介导其作用。阻断组胺H-1受体H1 R活化的抗组胺药已被证明是治疗荨麻疹、过敏性鼻炎和过敏性结膜炎相关瘙痒症的有效治疗剂。然而，它们对特应性皮炎和银屑病等其他瘙痒性疾病的疗效有限。除了组胺H-2受体H2 R外，其他组胺受体也可能在瘙痒中起作用。临床前证据表明，组胺H-3受体H3 R的局部拮抗作用可能通过阻断抑制性神经元信号而诱导抓挠。组胺H-4受体（H4 R）因其在介导瘙痒信号中的作用而受到广泛关注。事实上，现在已经表明，选择性H4 R拮抗剂可以抑制组胺诱导的人类瘙痒。该临床结果，结合在各种临床前瘙痒模型中的疗效，指出了H4 R拮抗剂用于治疗靶向H1 R的抗组胺药无法控制的瘙痒的治疗潜力。
Histamine is one of the best-characterized pruritogens in humans. It is known to play a role in pruritus associated with urticaria as well as ocular and nasal allergic reactions. Histamine mediates its effect via four receptors. Antihistamines that block the activation of the histamine H-1 receptor, H1R, have been shown to be effective therapeutics for the treatment of pruritus associated with urticaria, allergic rhinitis, and allergic conjunctivitis. However, their efficacy in other pruritic diseases such as atopic dermatitis and psoriasis is limited. The other histamine receptors may also play a role in pruritus, with the exception of the histamine H-2 receptor, H2R. Preclinical evidence indicates that local antagonism of the histamine H-3 receptor, H3R, can induce scratching perhaps via blocking inhibitory neuronal signals. The histamine H-4 receptor, H4R, has received a significant amount of attention as to its role in mediating pruritic signals. Indeed, it has now been shown that a selective H4R antagonist can inhibit histamine-induced itch in humans. This clinical result, in conjunction with efficacy in various preclinical pruritus models, points to the therapeutic potential of H4R antagonists for the treatment of pruritus not controlled by antihistamines that target the H1R.