Antidepressant derivatives of cis-4-phenyl-1,2,3,4-tetrahydro-1-naphthalenamine and pharmaceutical compositions thereof
申请人:PFIZER INC.
公开号:EP0030081A1
公开(公告)日:1981-06-10
Novel cis-isomeric derivatives of 4-phenyl-1,2,3,4-tetrahydro-1-naphthalenamine of the formula:
wherein R is hydrogen or normal alkyl or from 1 to 3 carbon atoms, R2 is normal alkyl of from 1 to 3 carbon atoms, Z is phenyl substituted by X and Y where X and Y are each hydrogen, fluoro, chloro, bromo, trifluoromethyl, alkoxy of from 1 to 3 carbon atoms or cyano, with at least one of X and Y being other than hydrogen, and W is hydrogen, fluoro, chloro, bromo, trifluoromethyl or alkoxy of from 1 to 3 carbon atoms, and the pharmaceutically acceptable acid addition salts and pharmaceutical compositions thereof are useful as antidepressant agents.
These compounds act to block the synaptosomal uptake of serotonin (5-hydroxy-tryptamine), thereby alleviating serotonin abnormalities at central receptor sites.
式中 4-苯基-1,2,3,4-四氢-1-萘胺的新型顺式异构体衍生物:
其中 R 是氢或 1 至 3 个碳原子的正烷基,R2 是 1 至 3 个碳原子的正烷基,Z 是被 X 和 Y 取代的苯基,其中 X 和 Y 分别是氢、氟、氯、溴、三氟甲基、1 至 3 个碳原子的烷氧基或氰基、其中 X 和 Y 至少有一个不是氢,W 是氢、氟、氯、溴、三氟甲基或 1 至 3 个碳原子的烷氧基,其药学上可接受的酸加成盐及其药物组合物可用作抗抑郁剂。
这些化合物的作用是阻断突触体对血清素(5-羟色胺)的摄取,从而缓解中枢受体部位的血清素异常。