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二氢麦角碱(DHESN)对5-羟色胺能系统及行为的影响:DHESN是一种新型抗抑郁药吗?

Effect of dihydroergosine (DHESN) on the serotoninergic system and behaviour: is DHESN a new antidepressive agent?

作者信息

Pericić D, Manev H, Levanat S, Jernej B, Vujić D, Djordjević N

出版信息

Psychopharmacology (Berl). 1986;90(1):112-8. doi: 10.1007/BF00172881.

DOI:10.1007/BF00172881
PMID:2945220
Abstract

Acute (50.0 mg/kg) and repeated (0.1-10.0 mg/kg) administration of dihydroergosine (DHESN) to rats over 5 days lowered the concentration of 5-HIAA in the brain. DHESN given acutely increased the brain 5-HT in p-CPA-treated animals and diminished the probenecid-induced increase in brain 5-HIAA. In pargyline-treated rats DHESN enhanced the 5-HT/5-HIAA ratio. DHESN administered to rats repeatedly over 5 days decreased the level of 5-HT in blood platelets, and in vitro at concentrations of 10(-4) M and 10(-3) M inhibited the uptake of [14C]-5-HT in platelets. DHESN (10.0-100.0 mg/kg) potentiated the 5-HT syndrome produced in rats by pargyline and 5-HTP. This potentiation was blocked with cyproheptadine but not with haloperidol. DHESN (1.0 and 10.0 mg/kg) lowered the locomotor activity of rats and 10.0 mg/kg DHESN also reduced the duration of immobility in rats forced to swim in a restricted space. The results indicate that DHESN, like antidepressants, decreases the turnover of serotonin in the brain and potentiates the 5-HT-mediated behaviour. This might suggest that the drug should be further investigated for its potential antidepressive properties.

摘要

对大鼠急性(50.0毫克/千克)和重复(0.1 - 10.0毫克/千克)给药二氢麦角隐亭(DHESN)5天,可降低大脑中5 - 羟吲哚乙酸(5 - HIAA)的浓度。急性给予DHESN可增加对氯苯丙氨酸(p - CPA)处理动物大脑中的5 - 羟色胺(5 - HT),并减少丙磺舒诱导的大脑5 - HIAA增加。在帕吉林处理的大鼠中,DHESN提高了5 - HT/5 - HIAA比值。对大鼠重复给药5天的DHESN可降低血小板中5 - HT的水平,且在体外浓度为10^(-4) M和10^(-3) M时可抑制血小板对[14C] - 5 - HT的摄取。DHESN(10.0 - 100.0毫克/千克)增强了帕吉林和5 - 羟色氨酸(5 - HTP)在大鼠中产生的5 - HT综合征。这种增强作用被赛庚啶阻断,但未被氟哌啶醇阻断。DHESN(1.0和10.0毫克/千克)降低了大鼠的运动活性,10.0毫克/千克的DHESN还减少了被迫在有限空间游泳的大鼠的不动时间。结果表明,DHESN与抗抑郁药一样,可降低大脑中血清素的周转率并增强5 - HT介导的行为。这可能表明该药物应进一步研究其潜在的抗抑郁特性。

相似文献

1
Effect of dihydroergosine (DHESN) on the serotoninergic system and behaviour: is DHESN a new antidepressive agent?二氢麦角碱(DHESN)对5-羟色胺能系统及行为的影响:DHESN是一种新型抗抑郁药吗?
Psychopharmacology (Berl). 1986;90(1):112-8. doi: 10.1007/BF00172881.
2
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Do imipramine and dihydroergosine possess two components--one stimulating 5-HT1 and the other inhibiting 5-HT2 receptors?丙咪嗪和双氢麦角碱是否具有两种成分——一种刺激5-HT1受体,另一种抑制5-HT2受体?
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Effect of a selective 5-HT uptake inhibitor--Lu 10-171--on rat brain 5-HT turnover.一种选择性5-羟色胺摄取抑制剂——Lu 10-171——对大鼠脑5-羟色胺代谢的影响。
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The role of brain 5-hydroxytryptamine in the hyperactivity produced in rats by lithium and monoamine oxidase inhibition.脑5-羟色胺在锂和单胺氧化酶抑制所致大鼠多动中的作用。
Br J Pharmacol. 1974 Sep;52(1):19-26. doi: 10.1111/j.1476-5381.1974.tb09682.x.

引用本文的文献

1
Possible antidepressant dihydroergosine preferentially binds to 5-HT1B receptor sites in the rat hippocampus.可能具有抗抑郁作用的双氢麦角碱优先与大鼠海马体中的5-HT1B受体位点结合。
J Neural Transm Gen Sect. 1993;92(1):1-9. doi: 10.1007/BF01245157.
2
Is the forced swimming test a suitable model for revealing antidepressant activity?强迫游泳试验是揭示抗抑郁活性的合适模型吗?
Psychopharmacology (Berl). 1988;94(2):147-60. doi: 10.1007/BF00176837.
3
Dual species dependent effect of dihydroergosine on the convulsions induced by GABA antagonists.

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Dihydroergotoxine and the Seizure Threshold.双氢麦角毒碱与癫痫发作阈值
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Two distinct central serotonin receptors with different physiological functions.两种具有不同生理功能的独特中枢5-羟色胺受体。
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Inhibition of 5-hydroxytryptamine-mediated behaviour by the putative 5-HT2 antagonist pirenperone.假定的5-羟色胺2拮抗剂匹仑哌隆对5-羟色胺介导行为的抑制作用。
Neuropharmacology. 1983 May;22(5):573-8. doi: 10.1016/0028-3908(83)90147-8.
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Hemodynamic effects of two ergot derivatives in the conscious spontaneously hypertensive rat.
Pharmacology. 1984;29(4):215-23. doi: 10.1159/000138016.
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Effect of dihydroergotoxine on the susceptibility of rats to convulsions produced by different convulsant agents.双氢麦角毒碱对大鼠对不同惊厥剂所致惊厥易感性的影响。
Psychopharmacology (Berl). 1983;80(2):171-3. doi: 10.1007/BF00427963.
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Injections of dopaminergic, cholinergic, serotoninergic and GABAergic drugs into the nucleus accumbens: effects on locomotor activity in the rat.向伏隔核注射多巴胺能、胆碱能、5-羟色胺能和γ-氨基丁酸能药物:对大鼠运动活动的影响。
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Long-term treatment with zimelidine leads to a reduction in 5-hydroxytryptamine neurotransmission within the central nervous system of the mouse and rat.长期使用齐美利定治疗会导致小鼠和大鼠中枢神经系统内5-羟色胺神经传递减少。
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