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吗啡肽(NH4-酪氨酰-脯氨酰-苯丙氨酰-脯氨酰胺):一种强效且特异性的吗啡(μ)受体激动剂。

Morphiceptin (NH4-tyr-pro-phe-pro-COHN2): a potent and specific agonist for morphine (mu) receptors.

作者信息

Chang K J, Lillian A, Hazum E, Cuatrecasas P, Chang J K

出版信息

Science. 1981 Apr 3;212(4490):75-7. doi: 10.1126/science.6259732.

DOI:10.1126/science.6259732
PMID:6259732
Abstract

The synthetic peptide NH2-Tyr-Pro-Phe-Pro-CONH2 (morphiceptin), which is the amide of a fragment of the milk protein beta-casein, has morphinelike activities and is highly specific for morphine (mu) receptors but not for enkephalin (delta) receptors. It is as active as morphine in the guinea pig ileum but much less active in the mouse and rat vas deferens. The discovery of this specific morphine receptor ligand substantiates the hypothesis of multiple opiate receptors. The ligand, which may be of physiological significance since a very similar, or identical, activity can be detected in enzymatic digests of beta-casein, may prove useful for further investigation of the functions of opiate receptor subtypes.

摘要

合成肽NH2-Tyr-Pro-Phe-Pro-CONH2(吗啡七肽)是乳蛋白β-酪蛋白片段的酰胺,具有吗啡样活性,对吗啡(μ)受体具有高度特异性,而对脑啡肽(δ)受体不具有特异性。它在豚鼠回肠中的活性与吗啡相当,但在小鼠和大鼠输精管中的活性要低得多。这种特异性吗啡受体配体的发现证实了多种阿片受体的假说。该配体可能具有生理意义,因为在β-酪蛋白的酶消化物中可检测到非常相似或相同的活性,它可能对进一步研究阿片受体亚型的功能有用。

相似文献

1
Morphiceptin (NH4-tyr-pro-phe-pro-COHN2): a potent and specific agonist for morphine (mu) receptors.吗啡肽(NH4-酪氨酰-脯氨酰-苯丙氨酰-脯氨酰胺):一种强效且特异性的吗啡(μ)受体激动剂。
Science. 1981 Apr 3;212(4490):75-7. doi: 10.1126/science.6259732.
2
Potent morphiceptin analogs: structure activity relationships and morphine-like activities.强效吗啡肽类似物:构效关系及类吗啡活性
J Pharmacol Exp Ther. 1983 Nov;227(2):403-8.
3
Guanyl nucleotide interactions with opiate receptors in guinea pig brain and ileum.鸟苷酸与豚鼠脑和回肠中阿片受体的相互作用。
Brain Res. 1980 Mar 31;186(2):486-91. doi: 10.1016/0006-8993(80)90996-8.
4
Opioid activity of pro-enkephalin-derived peptides in mouse vas deferens and guinea pig ileum.前脑啡肽衍生肽在小鼠输精管和豚鼠回肠中的阿片样活性。
Neurosci Lett. 1985 Nov 11;61(3):267-71. doi: 10.1016/0304-3940(85)90475-6.
5
Opioid receptor selectivity of beta-endorphin in vitro and in vivo: mu, delta and epsilon receptors.β-内啡肽在体外和体内对阿片受体的选择性:μ、δ和ε受体
J Pharmacol Exp Ther. 1988 Sep;246(3):1018-25.
6
Receptors for opioid peptides in the guinea-pig ileum.豚鼠回肠中阿片肽受体
J Pharmacol Exp Ther. 1985 Nov;235(2):389-92.
7
Structure-activity relationships of enkephalin analogs at opiate and enkephalin receptors: correlation with analgesia.脑啡肽类似物在阿片受体和脑啡肽受体上的构效关系:与镇痛作用的相关性
Eur J Pharmacol. 1980 Apr 11;63(1):35-46. doi: 10.1016/0014-2999(80)90114-4.
8
Interaction of morphine-epoxide with multiple opiate receptors.吗啡环氧化物与多种阿片受体的相互作用。
J Pharmacobiodyn. 1984 Apr;7(4):221-6. doi: 10.1248/bpb1978.7.221.
9
Tobacco mosaic virus-enkephalin conjugates: potentiation of opioid activity.烟草花叶病毒-脑啡肽缀合物:阿片样物质活性的增强
Peptides. 1981 Spring;2(1):89-92. doi: 10.1016/s0196-9781(81)80016-2.
10
Specific protection of the binding sites of D-Ala2-D-Leu5-enkephalin (delta-receptors) and dihydromorphine (mu-receptors).对D-丙氨酸2-D-亮氨酸5-脑啡肽(δ受体)和二氢吗啡(μ受体)结合位点的特异性保护。
Proc R Soc Lond B Biol Sci. 1979 Aug 31;205(1160):425-32. doi: 10.1098/rspb.1979.0076.

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