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配体结合数据的多维分析:在阿片受体中的应用。

Multidimensional analysis of ligand binding data: application to opioid receptors.

作者信息

Rothman R B, Barrett R W, Vaught J L

出版信息

Neuropeptides. 1983 Jul;3(5):367-77. doi: 10.1016/0143-4179(83)90025-2.

DOI:10.1016/0143-4179(83)90025-2
PMID:6312362
Abstract

The existence of distinct mu and delta opioid receptors is now well accepted. Most investigators favor the hypothesis that these receptors are physically distinct and that the enkephalins are only 2-10 fold selective for the delta receptor. Rothman and Westfall (Mol. Pharmacol. 21:548-557) recently challenged this hypothesis, proposing that at least some population of mu and delta receptors coexist in an opioid receptor complex and that the enkephalins are at least 100 fold selective for the delta receptor. In this paper we describe a generally applicable method we have used to design and analyze ligand binding experiments which distinguish between the two different models.

摘要

现在,不同的μ和δ阿片受体的存在已被广泛接受。大多数研究人员支持这样的假说,即这些受体在物理上是不同的,并且脑啡肽对δ受体的选择性仅为2至10倍。罗斯曼和韦斯特福尔(《分子药理学》21:548 - 557)最近对这一假说提出了质疑,他们提出至少有一些μ和δ受体群体共存于一个阿片受体复合物中,并且脑啡肽对δ受体的选择性至少为100倍。在本文中,我们描述了一种普遍适用的方法,我们用它来设计和分析区分这两种不同模型的配体结合实验。

相似文献

1
Multidimensional analysis of ligand binding data: application to opioid receptors.配体结合数据的多维分析:在阿片受体中的应用。
Neuropeptides. 1983 Jul;3(5):367-77. doi: 10.1016/0143-4179(83)90025-2.
2
Comparative pharmacological properties and functional coupling of mu and delta opioid receptor sites in human neuroblastoma SH-SY5Y cells.人神经母细胞瘤SH-SY5Y细胞中μ和δ阿片受体位点的比较药理学特性及功能偶联
Mol Pharmacol. 1987 Jul;32(1):109-18.
3
Binding in vivo of selective mu and delta opioid receptor agonists: opioid receptor occupancy by endogenous enkephalins.
Eur J Pharmacol. 1989 Nov 21;171(2-3):167-78. doi: 10.1016/0014-2999(89)90105-2.
4
Opioid binding to rat and guinea-pig neural membranes in the presence of physiological cations at 37 degrees C.在37摄氏度生理阳离子存在的情况下,阿片类药物与大鼠和豚鼠神经膜的结合。
J Pharmacol Exp Ther. 1985 Jun;233(3):722-8.
5
Distribution of mu, delta, and kappa opioid receptor binding sites in the brain of the one-day-old domestic chick (Gallus domesticus): an in vitro quantitative autoradiographic study.一日龄家鸡(原鸡)大脑中μ、δ和κ阿片受体结合位点的分布:一项体外定量放射自显影研究。
J Comp Neurol. 1990 Dec 15;302(3):543-51. doi: 10.1002/cne.903020310.
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Neuroanatomical patterns of the mu, delta, and kappa opioid receptors of rat brain as determined by quantitative in vitro autoradiography.通过定量体外放射自显影法测定大鼠脑内μ、δ和κ阿片受体的神经解剖学模式。
Proc Natl Acad Sci U S A. 1987 Jun;84(12):4308-12. doi: 10.1073/pnas.84.12.4308.
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DAMGO, a mu-opioid receptor selective ligand, distinguishes between mu-and kappa-opioid receptors at a different region from that for the distinction between mu- and delta-opioid receptors.DAMGO是一种μ阿片受体选择性配体,它在与区分μ阿片受体和δ阿片受体不同的区域区分μ阿片受体和κ阿片受体。
FEBS Lett. 1995 May 1;364(1):23-7. doi: 10.1016/0014-5793(95)00340-f.
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Rational design and biological properties of highly specific mu and delta opioid peptides.
Adv Biochem Psychopharmacol. 1982;33:321-31.
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Opiate binding in the rat spinal cord: evidence for mu and delta sites.大鼠脊髓中的阿片类物质结合:μ和δ位点的证据。
Neuropeptides. 1984 Dec;5(1-3):81-4. doi: 10.1016/0143-4179(84)90032-5.
10
Differential effects of cyanogen bromide on ligand binding by mu, delta and kappa opioid receptors.
Life Sci. 1990;47(24):2225-30. doi: 10.1016/0024-3205(90)90153-i.

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1
Experimental design and estimation of parameters in complex radioligand binding systems.复杂放射性配体结合系统中的实验设计与参数估计
J Pharmacokinet Biopharm. 1996 Dec;24(6):589-609. doi: 10.1007/BF02353482.