摘要
简介组胺H1受体活性及结合位点,综述二苯并[a,d][7]轮烯-5-胺类、1,2,4-三唑并[4,3-a]喹唑啉-5(4H)-酮类、咪唑[1,2-a]吡咯[3,2-d]氮杂类、苯并[5,6]环庚基[1,2-b]吡啶类、(ω、ω-二苯烷基)-1H-咪唑类、4-吲哚基哌啶取代苯甲酸类以及N-羟基氨基甲酸酯类H1受体拮抗剂的作用机制和构效关系。作为抗过敏性疾病的主要药物之一,H1受体拮抗剂能竞争性地与H1受体结合,阻断组胺与H1受体作用,从而抑制组胺的生物学效应。
The activity and binding site of histamine H1 receptor were briefly introduced. the action mechanism and structure-activity relationship of some H1 receptor antagonists, such as dibenzo [ a, d ] [ 7 ] annulene-5-amines, 1,2, 4-triazolo [ 4,3- a ] quinazolin-5 （4 n）-ones, imidazo [ 1,2- a ] pyrrolo [ 3,2-d ] azepines, benzo[ 5, 6 ] cyclohepta [ 1, 2-b ] pyridines, （ ω, ω-diphenylalkyl ）-1 H-imidazoles, 4- indolypipefidinyl benzoic acids and N-hydroxycarbamates were reviewed. As one of the most important antiinflammatory medicines, H1 receptor antagonists can bind to H1 receptor competitively to block the mutual action of histamine and its H1 receptor, thus inhibiting the biological effects of histamine.
出处
《药学进展》
CAS
2006年第7期289-294,共6页
Progress in Pharmaceutical Sciences
关键词
组胺受体
H1受体拮抗剂
作用机制
构效关系
Histamine receptor
H1 receptor antagonist
Action mechanism
Structure-activity relationship
