The neuro- and cardiovascular pharmacology of RS-51324, a potential antidepressant

Progress in neuro-psychopharmacology Pub Date : 1981-01-01 DOI:10.1016/0364-7722(81)90098-9

Marshall B Wallach , Brian J Alps , A.Peter Roszkowski , L.David Waterbury

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引用次数: 3

Abstract

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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RS-51324的神经和心血管药理学，一种潜在的抗抑郁药

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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