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长效抗精神病药物氟奋乃静庚酸酯和氟奋乃静癸酸酯在小鼠中产生的僵住症。

Catalepsy produced by long-acting neuroleptics, fluphenazine enanthate and fluphenazine decanoate, in mice.

作者信息

Yamada K, Furukawa T

出版信息

Pharmacology. 1982;24(3):147-55. doi: 10.1159/000137589.

Abstract

The cataleptic state induced by the depot-type preparations of fluphenazine (FZ) was investigated in mice. Intramuscular injections of FZ-enanthate or FZ-decanoate produced a marked and long-lasting catalepsy, which was antagonized by trihexyphenidyl, biperiden and promethazine but not by l-dopa. These anticataleptic effects disappeared after several hours and catalepsy occurred again. The cataleptic effects of FZ-enanthate and FZ-decanoate were increased by (D-Ala2, MePhe4, Met(0)5-ol)-enkephalin, aminooxyacetic acid and haloperidol. The results indicate that the cataleptic effects of FZ-enanthate and FZ-decanoate correspond with their long duration of antipsychotic effects and that the catalepsy may involve enkephalinergic, GABAergic and cholinergic as well as dopaminergic neuron activity.

摘要

在小鼠中研究了氟奋乃静(FZ)长效制剂诱导的僵住症状态。肌肉注射庚酸氟奋乃静或癸酸氟奋乃静会产生显著且持久的僵住症,这可被苯海索、安坦和异丙嗪拮抗,但不能被左旋多巴拮抗。这些抗僵住症作用数小时后消失,僵住症会再次出现。(D - 丙氨酸2,甲基苯丙氨酸4,蛋氨酸(0)5 - 醇) - 脑啡肽、氨氧乙酸和氟哌啶醇可增强庚酸氟奋乃静和癸酸氟奋乃静的僵住症作用。结果表明,庚酸氟奋乃静和癸酸氟奋乃静的僵住症作用与其持久的抗精神病作用相对应,且僵住症可能涉及脑啡肽能、γ - 氨基丁酸能、胆碱能以及多巴胺能神经元活性。

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