将赛庚啶与在10,11-亚乙烯基桥上稠合有呋喃核的类似物的抗血清素、抗组胺和抗胆碱能活性进行比较。
A comparison of the antiserotonin, antihistamine, and anticholinergic activity of cyproheptadine with analogues having furan nuclei fused to the 10,11-vinylene bridge.
作者信息
Remy D C, Raab A W, Rittle K E, Engelhardt E L, Scriabine A, Lotti V J
出版信息
J Med Chem. 1977 Jun;20(6):836-8. doi: 10.1021/jm00216a020.
A series of cyproheptadine derivatives having furan nuclei fused to the 10,11-vinylene bridge has been prepared. None of the compounds retain the potent antiserotonin and antihistaminic actions of cyproheptadine. 1-methyl-4-(1-methyl-8H-dibenzo[a,e]furo[3,4-c]cyclohepten-8-ylidene)piperidine (7), 1-methyl-4-(1,3-dihydro-1-oxo-8H-[3,4:6,7]cycloheptal[1,2-c]furan-8-ylidene)piperidine (10), and its reduction product 11 retained the peripheral anticholinergic activity of cyproheptadine.
已制备出一系列在10,11 - 亚乙烯基桥上稠合有呋喃核的赛庚啶衍生物。这些化合物均未保留赛庚啶强大的抗血清素和抗组胺作用。1 - 甲基 - 4 -（1 - 甲基 - 8H - 二苯并[a,e]呋喃并[3,4 - c]环庚烯 - 8 - 亚基）哌啶（7）、1 - 甲基 - 4 -（1,3 - 二氢 - 1 - 氧代 - 8H - [3,4:6,7]环庚并[1,2 - c]呋喃 - 8 - 亚基）哌啶（10）及其还原产物11保留了赛庚啶的外周抗胆碱能活性。
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