Klusha V, Georgiev V P, Petkov V D, Markovska V L, Svirskis S V, Mutzenietze R K, Anuans Z E
Acta Physiol Pharmacol Bulg. 1986;12(2):7-13.
Comparative studies were carried out of the central effects of the octapeptide angiotensin II (AT II) and of its fragments: C-terminal hexapeptide (AT 3-8), middle tetrapeptide (AT 3-6) and initial tripeptide (AT 1-3). The experiments were carried out with respect to the cerebral level of the biogenic amines DA, NA, 5-HT and their metabolites HVA and 5-HIAA in intact mice and in mice pretreated with haloperidol, as well as with respect to the animals' behaviour (haloperidol catalepsy, apomorphine stereotypy, unconditioned jumping reaction, hexobarbital sleep and the threshold of convulsive seizures induced by times intravenous infusion of pentylenetetrazol). The fragments studied were found to manifest activity in the tests used. In some respects this activity is very similar to the activity of AT II. There are also effects which differ from those of AT II, as well as effects which are entirely opposite in some respects, which makes it possible to examine some of these substance as its potential natural antagonists. All this shows that the biological activity of AT II in the brain undergoes a number of qualitative and quantitative changes when its molecule broken to produce peptides with shorter chains. In the effects observed AT II and its fragments interact predominantly with the DA-ergic transmission in the brain.
对八肽血管紧张素II（AT II）及其片段：C末端六肽（AT 3 - 8）、中间四肽（AT 3 - 6）和起始三肽（AT 1 - 3）的中枢效应进行了比较研究。实验针对完整小鼠和用氟哌啶醇预处理的小鼠中生物胺多巴胺（DA）、去甲肾上腺素（NA）、5 - 羟色胺（5 - HT）及其代谢产物高香草酸（HVA）和5 - 羟吲哚乙酸（5 - HIAA）的脑内水平进行，同时也针对动物的行为（氟哌啶醇致僵、阿扑吗啡刻板行为、无条件跳跃反应、己巴比妥睡眠以及静脉注射戊四氮诱导惊厥发作的阈值）进行。所研究的片段在所用测试中表现出活性。在某些方面，这种活性与AT II的活性非常相似。也有一些与AT II不同的效应，以及在某些方面完全相反的效应，这使得有可能将其中一些物质作为其潜在的天然拮抗剂进行研究。所有这些表明，当AT II的分子断裂产生较短链的肽时，其在脑内的生物活性会发生许多定性和定量的变化。在所观察到的效应中，AT II及其片段主要与脑内的多巴胺能传递相互作用。
