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所选类皮啡肽的阿片受体结合特征

Opioid receptor binding profile of selected dermorphin-like peptides.

作者信息

Rossi A C, de Castiglione R, Perseo G

出版信息

Peptides. 1986 Sep-Oct;7(5):755-9. doi: 10.1016/0196-9781(86)90091-4.

DOI:10.1016/0196-9781(86)90091-4
PMID:2879276
Abstract

The receptor binding profile of a selected group of dermorphin-like peptides was determined and correlated with the results of the guinea pig ileum (GPI) and mouse vas deferens (MVD) bioassays and with the currently used antinociception tests in the rat. For the peptides with the characteristic dermorphin D-Ala2-Phe3-Gly4 sequence, a linear negative correlation was found between the reciprocal of sodium shift and relative affinity for the mu-type opioid receptor. For the same peptides, a positive correlation was evidenced between relative potency on GPI and MVD and relative affinity for mu- and delta-type receptors, respectively.

摘要

测定了一组选定的类皮啡肽的受体结合谱,并将其与豚鼠回肠(GPI)和小鼠输精管(MVD)生物测定结果以及目前在大鼠中使用的抗伤害感受试验结果进行了关联。对于具有特征性皮啡肽D-Ala2-Phe3-Gly4序列的肽,发现钠移位倒数与对μ型阿片受体的相对亲和力之间呈线性负相关。对于相同的肽,分别证明了在GPI和MVD上的相对效价与对μ型和δ型受体的相对亲和力之间呈正相关。

相似文献

1
Opioid receptor binding profile of selected dermorphin-like peptides.所选类皮啡肽的阿片受体结合特征
Peptides. 1986 Sep-Oct;7(5):755-9. doi: 10.1016/0196-9781(86)90091-4.
2
Dimeric dermorphin analogues as mu-receptor probes on rat brain membranes. Correlation between central mu-receptor potency and suppression of gastric acid secretion.二聚体皮肤吗啡类似物作为大鼠脑膜上的μ受体探针。中枢μ受体效能与胃酸分泌抑制之间的相关性。
J Biol Chem. 1989 Jan 5;264(1):354-62.
3
Dermorphin-related peptides from the skin of Phyllomedusa bicolor and their amidated analogs activate two mu opioid receptor subtypes that modulate antinociception and catalepsy in the rat.来自双色叶泡蛙皮肤的与皮吗啡相关的肽及其酰胺化类似物激活两种μ阿片受体亚型,这些亚型可调节大鼠的抗伤害感受和僵住症。
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Structure-activity relationships of dermorphin analogues containing N-substituted amino acids in the 2-position of the peptide sequence.在肽序列2位含有N-取代氨基酸的德莫啡类似物的构效关系。
Int J Pept Protein Res. 1995 Jul;46(1):47-55. doi: 10.1111/j.1399-3011.1995.tb00580.x.
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Dermorphin interaction with peripheral opioid receptors.强啡肽与外周阿片受体的相互作用。
Neuropeptides. 1984 Dec;5(1-3):157-60. doi: 10.1016/0143-4179(84)90051-9.
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Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.吲哚苯部分被取代的纳曲吲哚类似物的合成、阿片受体结合及生物活性测定。
J Med Chem. 1998 Jul 16;41(15):2872-81. doi: 10.1021/jm980083i.
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Characterisation and visualisation of [3H]dermorphin binding to mu opioid receptors in the rat brain. Combined high selectivity and affinity in a natural peptide agonist for the morphine (mu) receptor.[3H]德莫啡肽与大鼠脑内μ阿片受体结合的表征与可视化。一种天然肽激动剂对吗啡(μ)受体具有高选择性和亲和力。
Eur J Biochem. 1990 May 20;189(3):625-35. doi: 10.1111/j.1432-1033.1990.tb15531.x.
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Dermenkephalin (Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2): a potent and fully specific agonist for the delta opioid receptor.皮肤脑啡肽(酪氨酰-D-蛋氨酰-苯丙氨酰-组氨酰-亮氨酰-蛋氨酰-天冬氨酰胺):一种强效且高度特异性的δ阿片受体激动剂。
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Antinociceptive potencies of beta-casomorphin analogs as compared to their affinities towards mu and delta opiate receptor sites in brain and periphery.
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Dermorphin interaction with rat brain opioid receptors: involvement of hydrophobic sites in the binding domain.强啡肽与大鼠脑阿片受体的相互作用:结合域中疏水位点的作用。
Mol Pharmacol. 1990 Jun;37(6):886-92.

引用本文的文献

1
Nature-Derived Peptides: A Growing Niche for GPCR Ligand Discovery.天然衍生肽:G 蛋白偶联受体配体发现的新兴领域。
Trends Pharmacol Sci. 2019 May;40(5):309-326. doi: 10.1016/j.tips.2019.03.004. Epub 2019 Apr 5.
2
Activity of mu- and delta-opioid agonists in vas deferens from mice deficient in MOR gene.μ-和δ-阿片样物质激动剂在MOR基因缺陷小鼠输精管中的活性。
Br J Pharmacol. 2001 Apr;132(7):1485-92. doi: 10.1038/sj.bjp.0703966.
3
Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding sites.
强啡肽:一类对δ阿片样物质结合位点具有高亲和力和选择性的天然存在的肽。
Proc Natl Acad Sci U S A. 1989 Jul;86(13):5188-92. doi: 10.1073/pnas.86.13.5188.
4
Opioid activity of dermenkephalin analogues in the guinea-pig myenteric plexus and the hamster vas deferens.皮肤脑啡肽类似物在豚鼠肠肌丛和仓鼠输精管中的阿片样活性。
Br J Pharmacol. 1991 Oct;104(2):428-32. doi: 10.1111/j.1476-5381.1991.tb12446.x.