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用[125I-酪氨酸1,D-脯氨酸10]强啡肽A-(1-11)对脊髓上κ-阿片受体进行放射自显影定位

Autoradiographic localization of supraspinal kappa-opioid receptors with [125I-Tyr1, D-Pro10]dynorphin A-(1-11).

作者信息

Jomary C, Gairin J E, Cros J, Meunier J C

机构信息

Laboratoire de Pharmacologie et de Toxicologie Fondamentales, Centre National de la Recherche Scientifique, Toulouse, France.

出版信息

Proc Natl Acad Sci U S A. 1988 Jan;85(2):627-31. doi: 10.1073/pnas.85.2.627.

DOI:10.1073/pnas.85.2.627
PMID:2893376
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC279604/
Abstract

[125I-Tyr1, D-Pro10]dynorphin A-(1-11) (125I-DP-DYN), an opioid peptide analogue that has previously been shown to be kappa selective, displays specific, saturable, and high-affinity (Kd = 0.3 nM) binding in slide-mounted sections from nerve tissue. We have used 125I-DPDYN to autoradiographically visualize supraspinal kappa-opioid receptor sites in rats, guinea pigs, and rabbits. The autoradiographic dispositions of 125I-DPDYN in sections from cerebellum are clearly different in guinea pig and rabbit, suggesting that kappa receptors have different functions in this organ of the two species. Autoradiograms from 125I-DPDYN-labeled brain sections also reveal major species differences, in particular in thalamus, which is densely labeled in rabbit and considerably less so in rat and guinea pig. The data show that 125I-DPDYN is a useful probe to visualize kappa-opioid receptor sites in nerve tissue sections directly and rapidly.

摘要

[125I-酪氨酰1,D-脯氨酰10]强啡肽A-(1-11)(125I-DP-DYN)是一种阿片肽类似物,先前已被证明具有κ选择性,在神经组织的载玻片标本中显示出特异性、可饱和性和高亲和力(Kd = 0.3 nM)结合。我们已使用125I-DP-DYN通过放射自显影法在大鼠、豚鼠和兔子中可视化脊髓上κ阿片受体位点。125I-DP-DYN在豚鼠和兔子小脑切片中的放射自显影分布明显不同,这表明κ受体在这两个物种的该器官中具有不同功能。125I-DP-DYN标记的脑切片的放射自显影片也显示出主要的物种差异,特别是在丘脑中,兔子中丘脑被密集标记,而在大鼠和豚鼠中则标记程度低得多。数据表明,125I-DP-DYN是一种直接且快速地可视化神经组织切片中κ阿片受体位点的有用探针。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a94c/279604/b8cabe52825a/pnas00254-0339-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a94c/279604/a92ee08b870c/pnas00254-0338-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a94c/279604/b8cabe52825a/pnas00254-0339-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a94c/279604/a92ee08b870c/pnas00254-0338-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a94c/279604/b8cabe52825a/pnas00254-0339-a.jpg

相似文献

1
Autoradiographic localization of supraspinal kappa-opioid receptors with [125I-Tyr1, D-Pro10]dynorphin A-(1-11).用[125I-酪氨酸1,D-脯氨酸10]强啡肽A-(1-11)对脊髓上κ-阿片受体进行放射自显影定位
Proc Natl Acad Sci U S A. 1988 Jan;85(2):627-31. doi: 10.1073/pnas.85.2.627.
2
125I-DPDYN, monoiodo [D-Pro10]- dynorphin (1-11), is an effective and useful tool for the study of kappa opioid receptors.125I-DPDYN,单碘代[D-脯氨酸10]-强啡肽(1-11),是研究κ阿片受体的一种有效且有用的工具。
NIDA Res Monogr. 1986;75:232-5.
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125I-DPDYN, monoiodo[D-Pro10]dynorphin(1-11): a highly radioactive and selective probe for the study of kappa opioid receptors.125I - DPDYN,单碘代[D - 脯氨酸10]强啡肽(1 - 11):一种用于研究κ阿片受体的高放射性且选择性的探针。
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N,N-diallyl-tyrosyl substitution confers antagonist properties on the kappa-selective opioid peptide [D-Pro10]dynorphin A(1-11).N,N-二烯丙基-酪氨酰取代赋予κ-选择性阿片肽[D-脯氨酸10]强啡肽A(1-11)拮抗特性。
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[125I]dynorphin(1-8) produces a similar pattern of kappa-opioid receptor labelling to [3H]dynorphin(1-8) and [3H]etorphine in guinea pig brain: a quantitative autoradiographic study.[125I]强啡肽(1 - 8)在豚鼠脑中产生的κ-阿片受体标记模式与[3H]强啡肽(1 - 8)和[3H]埃托啡相似:一项定量放射自显影研究。
Neurosci Lett. 1988 Apr 12;86(3):272-8. doi: 10.1016/0304-3940(88)90495-8.
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Dynorphin A-(1-13)-Tyr14-Leu15-Phe16-Asn17-Gly18-Pro19 : a potent and selective kappa opioid peptide.强啡肽A-(1-13)-酪氨酰14-亮氨酰15-苯丙氨酰16-天冬酰胺17-甘氨酰18-脯氨酰19:一种强效且选择性的κ阿片肽。
Eur J Pharmacol. 1991 Apr 17;196(2):161-7. doi: 10.1016/0014-2999(91)90423-n.
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Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.强啡肽A(1-11)-NH2第3位残基修饰对κ受体选择性和效价的影响。
J Med Chem. 1996 Jun 21;39(13):2456-60. doi: 10.1021/jm950655o.
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[D-Pro10]-dynorphin(1-11) is a kappa-selective opioid analgesic in mice.[D-脯氨酸10]-强啡肽(1-11)是小鼠中的一种κ选择性阿片类镇痛药。
J Pharmacol Exp Ther. 1988 Jun;245(3):995-1001.
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[D-Pro10]Dynorphin-(1-11) is a highly potent and selective ligand for kappa opioid receptors.
Eur J Pharmacol. 1984 Nov 13;106(2):457-8. doi: 10.1016/0014-2999(84)90741-6.
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Synthesis and biological activity of dynorphin-(1-13) and analogs substituted in positions 8 and 10.强啡肽-(1-13)及其8位和10位取代类似物的合成与生物活性
Int J Pept Protein Res. 1986 Mar;27(3):300-5. doi: 10.1111/j.1399-3011.1986.tb01824.x.

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Kappa opiate binding sites in the substantia nigra and bulbus olfactorius of the guinea pig as shown by in vitro autoradiography.豚鼠黑质和嗅球中κ阿片受体结合位点的体外放射自显影研究。
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Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr: a new highly potent and fully specific agonist for opiate delta-receptors.δ脑啡肽,酪氨酰-D-苏氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸:一种新型高效且完全特异性的阿片δ受体激动剂。
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Novel opiate binding sites selective for benzomorphan drugs.对苯并吗啡烷类药物具有选择性的新型阿片样物质结合位点。
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[D-Pro10]Dynorphin-(1-11) is a highly potent and selective ligand for kappa opioid receptors.
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