Potent tetrapeptide enkephalins.

Potent tetrapeptide enkephalins.
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有效的四肽脑啡肽。

DOI:
10.1016/0024-3205(81)90384-2
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发表时间:
1981
期刊:
影响因子:
6.1
通讯作者:
Stewart,JM
Stewart,JM
中科院分区:
医学2区
文献类型:
--
作者:
Chipkin,RE;Morris,DH;English,MG;Rosamond,JD;Stammer,CH;York,EJ;Stewart,JM

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Small peptides with opiate-like activity have generally had structures closely resembling that of the opioid pentapeptide enkephalin: Tyr-Gly-Gly-Phe-Met-COOH. Single deletions of any one of the amino acids has been demonstrated to reduce opiate activity drastically. In this work we show that the potency losses resulting from the removal of glycine3can be fully attenuated by substitution of D-alanine in position two and derivatization of the acid to the amide. This tetrapeptide (Tyr-DAla-Phe-Met-NH2) has narcotic activity similar to the parent pentapeptide in the guinea pig ileum and mouse tail-flick tests. This enhanced potency, relative to the unaltered tetrapeptide, is theorized to arise from increased resistance to enzymatic destruction. the data presented show that a five amino acid sequence is not mandatory for the expression of opiate activity in enkephalin analogs.
DOI: 10.1038/258577a0
发表时间: 1975-01-01
期刊: NATURE
影响因子: 64.8
作者:
HUGHES, J;SMITH, TW;MORRIS, HR
通讯作者: MORRIS, HR
一些新的甲硫氨酸脑啡肽类似物具有类似吗啡的活性。
DOI: --
发表时间: 1979
期刊: Life Science
影响因子: --
作者:
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DOI: --
发表时间: 1977
期刊: Biochemical and Biophysical Research Communications - BBRC
影响因子: --
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脑啡肽样四肽 H-Tyr-D-Ala-Gly-Phe-NH2 具有有效的镇痛活性。
DOI: --
发表时间: 1978
期刊: Life Science
影响因子: --
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W. McGregor;L. Stein;J. Belluzzi
通讯作者: J. Belluzzi
DOI: --
发表时间: --
期刊:
影响因子: --
作者:
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通讯作者: A. Miekeley