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[P物质分子N端在应激相关行为及血压紊乱中的作用]

[The role of the N-terminal of the substance P molecule in its action in stress-related behavioral and blood pressure disorders].

作者信息

Roske I, Oehme P, Hecht K, Nieber K, Hilse H, Wachtel E

出版信息

Pharmazie. 1986 Nov;41(11):799-805.

PMID:2436239
Abstract

Substance P and the N-terminal sequences SP1-9, SP1-7, SP1-4 and SP1-2 were investigated in their action on stress related alterations in blood pressure behaviour, stress related disturbances in conditioned reflex learning behaviour, alterations in the endogenous opioid system and on the blood pressure behaviour of spontaneously hypertensive rats. In addition the occurrence of vegetative effects such as acute hypertension and histamine release from mast cells were investigated. The results of this work show that N- and C-terminal sequences of the Substance P molecule differ in their actions. Whereas the vegetative effects decrease if the SP molecule is shortened from the C to the N-terminus the "antistress effect" of the Substance P molecule remains unchanged. Whereas the N-terminal tetrapeptide SP1-4 can be considered "essential" for the "antistress effect", the C-terminal pentapeptide of SP is considered to be the "essential sequence" for the vegetative effects. These results will open new possibilities for the synthesis of selectively acting SP-agonists.

摘要

研究了P物质及其N端序列SP1-9、SP1-7、SP1-4和SP1-2对血压行为中应激相关改变、条件反射学习行为中应激相关干扰、内源性阿片系统改变以及对自发性高血压大鼠血压行为的作用。此外,还研究了诸如急性高血压和肥大细胞组胺释放等自主神经效应的发生情况。这项工作的结果表明,P物质分子的N端和C端序列作用不同。当SP分子从C端到N端缩短时,自主神经效应减弱,而P物质分子的“抗应激效应”保持不变。虽然N端四肽SP1-4可被认为是“抗应激效应”的“必需”成分,但SP的C端五肽被认为是自主神经效应的“必需序列”。这些结果将为合成具有选择性作用的SP激动剂开辟新的可能性。

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