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单甲氧基苯丙胺中枢5-羟色胺能效应的药理学证据。

Pharmacological evidence for the central serotonergic effects of monomethoxyamphetamines.

作者信息

Menon M K, Tseng L F, Loh H H

出版信息

J Pharmacol Exp Ther. 1976 May;197(2):272-9.

PMID:946817
Abstract

The effects of three monomethoxyamphetamines, dl-para-methoxyamphetamine (dl-PMA), dl-meta-methoxyamphetamine (dl-MMA) and dl-ortho-methyoxyamphetamine (dl-OMA), and d-amphetamine (d-A) on the myoclonic twitch activity (MTA) of PMA, MMA and d-A were found to increase the MTA but OMA was ineffective. The increased MTA induced by d-A was not influenced by the blockade of 5-hydroxytryptamine (5-HT) receptor by methysergide or inhibition of 5-HT synthesis by para chlorophenylalamine (PCPA) but was reduced by haloperidol which blocked the dopamine receptor. On the other hand, the increased MTA produced by PMA was not influenced by haloperidol but was reduced by methysergide and PCPA. The increased MTA induced by MMA was not effectively blocked by either PCPA or haloperidol but was blocked by the combination of both PCPA and haloperidol. The results indicate that whereas the increased MTA produced by d-A is not dependent on the availability of 5-HT, PMA exerts by a release of 5-HT and that the MMA effect is due to a release of both 5-HT and dopamine. High doses of PMA and MMA increased the locomotor activity arevious biochemical findings that PMA releases 5-HT in brain tissue and suggests that PMA exerts its pharmacological effects by releasing 5-HT.

摘要

研究发现,三种单甲氧基苯丙胺,即消旋对甲氧基苯丙胺(dl-PMA)、消旋间甲氧基苯丙胺(dl-MMA)和消旋邻甲氧基苯丙胺(dl-OMA)以及右旋苯丙胺(d-A)对肌阵挛抽搐活动(MTA)的影响中,PMA、MMA和d-A可增加MTA,但OMA无效。d-A诱导的MTA增加不受麦角新碱对5-羟色胺(5-HT)受体的阻断或对氯苯丙氨酸(PCPA)对5-HT合成的抑制的影响,但可被阻断多巴胺受体的氟哌啶醇降低。另一方面,PMA产生的MTA增加不受氟哌啶醇影响,但可被麦角新碱和PCPA降低。MMA诱导的MTA增加既不能被PCPA也不能被氟哌啶醇有效阻断,但可被PCPA和氟哌啶醇联合阻断。结果表明,d-A产生的MTA增加不依赖于5-HT的可用性,PMA通过释放5-HT发挥作用,而MMA的作用是由于5-HT和多巴胺的释放。高剂量的PMA和MMA增加了运动活性,先前的生化研究结果表明PMA在脑组织中释放5-HT,并提示PMA通过释放5-HT发挥其药理作用。

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