RS-51324的神经和心血管药理学,一种潜在的抗抑郁药

Marshall B Wallach , Brian J Alps , A.Peter Roszkowski , L.David Waterbury
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引用次数: 3

摘要

1.1. RS-51324 (DL-4(5)-(2,6二氯苯基)-2-甲氧羰基-氨基-4,5二氢咪唑)在动物中的神经和心血管作用已被探索。通过利血平拮抗作用和左旋多巴增强作用证实RS-51324具有抗抑郁作用。外周血管对5 -羟色胺的反应增强,但未发现中枢效应。心血管实验表明,RS-51324缺乏抗胆碱能作用,但具有轻微的抗组胺活性。RS-51324增强酪胺诱导的升压反应。RS-51324缺乏中枢作用的骨骼肌松弛剂活性。RS-51324的LD50大于2 gm/kg.9.9。RS-51324似乎是一种膜泵抑制化合物,可能具有抗抑郁活性。
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The neuro- and cardiovascular pharmacology of RS-51324, a potential antidepressant

  • 1.

    1. The neuro- and cardiovascular effects of RS-51324 (DL-4(5)-(2,6dichlorophenyl)-2-methoxycarbonyl-amino-4,5 dihydroimidazole) have been explored in animals.

  • 2.

    2. Antidepressant activities of RS-51324 were demonstrated by reserpine antagonism and L-DOPA potentiation.

  • 3.

    3. Norepinephrine uptake was inhibited but MAO activity was not inhibited by RS-51324.

  • 4.

    4. Peripheral vascular responses to serotonin were potentiated although central effects were not demonstrated.

  • 5.

    5. Cardiovascular experiments indicated that RS-51324 lacked anticholinergic effects but had mild antihistaminic activity.

  • 6.

    6. RS-51324 potentiated tyramine-induced pressor responses.

  • 7.

    7. RS-51324 lacks centrally acting skeletal muscle relaxant activity.

  • 8.

    8. The LD50 of RS-51324 was greater than 2 gm/kg.

  • 9.

    9. RS-51324 appears to be a membrane-pump inhibiting compound with probable antidepressant activity.

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