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WEN Lei-lei, HU Su-juan, CUI Yong. Institute of Dermatology, Department of Dermatology and venereology, First Affiliated Hospital, Anhui Medical University, Hefei 230032, China Corresponding author: CUI Yong�� Email: wuhucuiyong@vip.163.com ��Abstract�� The binding of histamine to its receptors can induce the release of inflammatory mediators predominated by histamine followed by the development of allergic diseases. H1-receptor antagonists, as a kind of antihistamine, can inhibit the biological effects of histamine by blocking its binding to H1 receptor, and are mainly used to treat allergic diseases which are induced by the release of histamine. First-generation antihistamines have a short duration of action and an obvious sedative effect on central nervous system. Compared with first-generation antihistamines, second-generation antihistamines show a similar or stronger efficacy, longer duration of action and less sedative effects. However, cardiac toxicity has been observed in second-generation antihistamines, which has warranted the development of new antihistamine agents. ��Key words�� Histamine; Histamine H1 antagonists; Research