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[使用放射受体法对新型阿片样肽的分析]

[Analysis of new opiate-like peptides using a radioreceptor method].

作者信息

Shestak K I, Sergeeva M G, Zaĭtsev S V, Kharchenko E P, Varfolomeev S D, Kalikhevich V N, Ardemasova Z A

出版信息

Ukr Biokhim Zh (1978). 1990 Mar-Apr;62(2):23-9.

PMID:1973313
Abstract

A screening of new synthetic opioid-like peptides has been carried out by the radioreceptor assay using selective labeled ligands to mu-, delta- and gamma-opioid receptors of the rat brain membranes. With this aim peptides from sequences of the following proteins were used: kapporphin-Tyr-Ser-Phe-Gly-Gly and its analogues-Tyr-Ser-Phe-Gly-Gly-NH2, Tyr-D-Ser-Phe-Gly-Gly, Tyr-D-Ser-Phe-Gly-Gly-NH2, myelorphin-Phe-Gly-Tyr-Gly-Gly, interenkephalin B-Arg-Arg-Gln-Phe-Lys and chimeric peptide IEPhBin 1-Tyr-Gly-Gly-Phe-Leu-Arg-Pro-Tyr-Ile-Leu consisting of leu-enkephalin and pentaneurotensin. It has been found that myelorphin has a prevalent affinity to mu-receptor, while the kapporphin analogues both to mu- and delta-receptors. The presence of pentaneurotensin in chimeric peptide does not affect the specificity of binding to opioid receptors, but decreases affinity to mu- and delta-receptors approximately by an order as compared to leu-enkephalin. Kapprorphin and interenkephalin B displace neither of the selective labeled opioid ligands under study.

摘要

利用放射性受体分析法,使用针对大鼠脑膜μ、δ和γ阿片受体的选择性标记配体,对新的合成阿片样肽进行了筛选。为此,使用了来自以下蛋白质序列的肽:强啡肽-酪氨酰-丝氨酰-苯丙氨酰-甘氨酰-甘氨酸及其类似物-酪氨酰-丝氨酰-苯丙氨酰-甘氨酰-甘氨酸-氨基、酪氨酰-D-丝氨酰-苯丙氨酰-甘氨酰-甘氨酸、酪氨酰-D-丝氨酰-苯丙氨酰-甘氨酰-甘氨酸-氨基、髓啡肽-苯丙氨酰-甘氨酰-酪氨酰-甘氨酰-甘氨酸、脑啡肽B-精氨酰-精氨酰-谷氨酰胺-苯丙氨酰-赖氨酸以及由亮氨酸脑啡肽和五肽神经降压素组成的嵌合肽IEPhBin 1-酪氨酰-甘氨酰-甘氨酸-苯丙氨酰-亮氨酰-精氨酰-脯氨酰-酪氨酰-异亮氨酰-亮氨酸。已发现髓啡肽对μ受体具有普遍亲和力,而强啡肽类似物对μ和δ受体均有亲和力。嵌合肽中五肽神经降压素的存在不影响与阿片受体结合的特异性,但与亮氨酸脑啡肽相比,对μ和δ受体的亲和力大约降低了一个数量级。强啡肽和脑啡肽B均未取代所研究的选择性标记阿片配体。

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