大鼠脑中促肾上腺皮质激素样肽与阿片受体：构效关系研究
ACTH-like peptides and opiate receptors in the rat brain: structure-activity studies.
作者信息
Terenius L, Gispen W H, De Wied D
出版信息
Eur J Pharmacol. 1975 Sep-Oct;33(2):395-9. doi: 10.1016/0014-2999(75)90185-5.
The present study aims at further identifying the interaction of ACTH-like peptides and rat brain opiate receptors in vitro. The sequence ACTH4-10 is crucial with respect to affinity since it is the shortest sequence to inhibit the binding of [3H]-dihydromorphine and [3H]-naltrexone to these receptors. A second active site seems to be localized in the N-terminal part of ACTH11-24. This structure-activity relationship is compared to that observed for these peptides on the adrenal cortex and behavior.
本研究旨在进一步确定促肾上腺皮质激素样肽与大鼠脑阿片受体在体外的相互作用。就亲和力而言，促肾上腺皮质激素4 - 10序列至关重要，因为它是抑制[3H]-二氢吗啡和[3H]-纳曲酮与这些受体结合的最短序列。第二个活性位点似乎位于促肾上腺皮质激素11 - 24的N端部分。将这种构效关系与这些肽在肾上腺皮质和行为方面所观察到的构效关系进行比较。
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