Deprenyl (selegiline): the history of its development and pharmacological action

Deprenyl (selegiline): the history of its development and pharmacological action
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Deprenyl(司来吉兰):其发展历史和药理作用

DOI:
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发表时间:
1983
期刊:
Acta Neurologica Scandinavica, Supplementum
影响因子:
--
通讯作者:
Joseph Knoll
Joseph Knoll
中科院分区:
--
文献类型:
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作者:
Joseph Knoll

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摘要-丙炔苯丙胺在不同的动物物种和人体中选择性抑制单胺氧化酶B,其安全范围是显著的。我们能够选择性地在体内阻断四种物种(小鼠、大鼠、猫、狗)脑中的MAO B活性,给予0.17- 0.31%LD 50。临床实践中常用的口服剂量范围为每日5-20 mg(0.05-0.2 mg/kg),比大鼠口服活性剂量低约十倍。
ABSTRACT — Deprenyl inhibits MAO‐B selectively in different animal species and in man. Its safety margin is remarkable. We were able to block MAO‐B activity in the brain selectively in vivo in four species (mouse, rat, cat, dog) with s.c. administration of 0.17–0.31% of LD50. The usual oral dose range in clinical practice, 5–20 mg daily (0.05–0.2 mg/kg), is about ten times lower than the orally active dose in the rat.
长期抗抑郁药治疗会降低螺哌啶醇标记的血清素受体结合。
DOI: 10.1126/science.6251550
发表时间: 1980
期刊: Science (New York, N.Y.)
影响因子: --
作者:
Peroutka,SJ;Snyder,SH
通讯作者: Snyder,SH
米安色林急性和慢性治疗后血清素受体敏感性。
DOI: --
发表时间: 1982
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Blackshear,MA;Sanders-Bush,E
通讯作者: Sanders-Bush,E
DOI: 10.1016/0006-2952(78)90226-5
发表时间: 1978-02
影响因子: 5.8
作者:
F. Sulser;J. Vetulani;P. Mobley
通讯作者: F. Sulser;J. Vetulani;P. Mobley