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啮齿动物脊髓中的δ阿片受体结合位点。

Delta-opioid receptor binding sites in rodent spinal cord.

作者信息

Traynor J R, Hunter J C, Rodriguez R E, Hill R G, Hughes J

机构信息

Department of Chemistry, Loughborough University, Leics.

出版信息

Br J Pharmacol. 1990 Jun;100(2):319-23. doi: 10.1111/j.1476-5381.1990.tb15802.x.

DOI:10.1111/j.1476-5381.1990.tb15802.x
PMID:2165837
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1917433/
Abstract
  1. The delta-opioid receptor agonist [D-Pen2,D-Pen5]enkephalin showed an antinociceptive effect in the mouse tail-flick test, following intrathecal administration. This action was reversed by naloxone and by the selective delta-opioid receptor antagonist ICI 174864. 2. High affinity, saturable binding of [3H]-[D-Pen2,D-Pen5]enkephalin has been demonstrated in spinal cord homogenates from guinea-pig, hamster, rat and both adult and young (18-20 g) mice. The binding was shown by autoradiography to be concentrated in the superficial laminae of the dorsal horn. 3. Competition studies confirmed that the binding of [3H]-[D-Pen2,D-Pen5]enkephalin was to the delta-opioid site. However, anomalies were seen with displacement assays using mu-ligands, which may suggest some common high affinity site for delta- and mu-opioid receptor agonists in the spinal cord. 4. The results add further evidence for a role of the delta-opioid receptor in spinally-mediated antinociception.
摘要
  1. δ-阿片受体激动剂[D-青霉胺2，D-青霉胺5]脑啡肽经鞘内给药后，在小鼠甩尾试验中显示出抗伤害感受作用。这种作用可被纳洛酮和选择性δ-阿片受体拮抗剂ICI 174864逆转。2. 已证实在豚鼠、仓鼠、大鼠以及成年和幼年（18 - 20克）小鼠的脊髓匀浆中，[3H]-[D-青霉胺2，D-青霉胺5]脑啡肽具有高亲和力、可饱和结合。放射自显影显示结合集中在背角浅层。3. 竞争研究证实[3H]-[D-青霉胺2，D-青霉胺5]脑啡肽的结合是在δ-阿片位点。然而，在使用μ-配体的置换试验中出现了异常情况，这可能表明脊髓中δ-和μ-阿片受体激动剂存在一些共同的高亲和力位点。4. 这些结果为δ-阿片受体在脊髓介导的抗伤害感受中的作用提供了进一步的证据。
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/354f/1917433/8670abea5319/brjpharm00251-0131-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/354f/1917433/8670abea5319/brjpharm00251-0131-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/354f/1917433/8670abea5319/brjpharm00251-0131-a.jpg

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Delta-opioid receptor binding sites in rodent spinal cord.啮齿动物脊髓中的δ阿片受体结合位点。
Br J Pharmacol. 1990 Jun;100(2):319-23. doi: 10.1111/j.1476-5381.1990.tb15802.x.
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Opioid receptor ligands in the neonatal rat spinal cord: binding and in vitro depression of the nociceptive responses.新生大鼠脊髓中的阿片受体配体：结合与伤害性反应的体外抑制
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Biochemical characterization and regional quantification of mu, delta and kappa opioid binding sites in rat spinal cord.大鼠脊髓中μ、δ和κ阿片样物质结合位点的生化特性及区域定量分析。
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Opioid binding sites in the guinea pig and rat kidney: radioligand homogenate binding and autoradiography.豚鼠和大鼠肾脏中的阿片样物质结合位点：放射性配体匀浆结合及放射自显影
Mol Pharmacol. 1991 Jul;40(1):93-100.
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Delta opioid receptor enhancement of mu opioid receptor-induced antinociception in spinal cord.脊髓中δ阿片受体对μ阿片受体诱导的抗伤害感受的增强作用。
J Pharmacol Exp Ther. 1998 Jun;285(3):1181-6.
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Interaction between highly selective mu and delta opioids in vivo at the rat spinal cord.高选择性μ和δ阿片类药物在大鼠脊髓水平的体内相互作用。
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The use of [3H]-[D-Pen2,D-Pen5]enkephalin as a highly selective ligand for the delta-binding site.使用[3H]-[D-青霉胺2，D-青霉胺5]脑啡肽作为δ结合位点的高选择性配体。
Br J Pharmacol. 1985 Apr;84(4):927-32. doi: 10.1111/j.1476-5381.1985.tb17387.x.
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Heroin acts on different opioid receptors than morphine in Swiss Webster and ICR mice to produce antinociception.在瑞士韦伯斯特小鼠和ICR小鼠中，海洛因作用于与吗啡不同的阿片受体以产生抗伤害感受。
J Pharmacol Exp Ther. 1991 Feb;256(2):448-57.
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Distinct antinociceptive actions mediated by different opioid receptors in the region of lamina I and laminae III-V of the dorsal horn of the rat.大鼠背角I层和III - V层区域中不同阿片受体介导的不同抗伤害感受作用。
Br J Pharmacol. 1990 Oct;101(2):477-83. doi: 10.1111/j.1476-5381.1990.tb12733.x.
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Inhibition of mu and delta but not kappa opioid binding to membranes by Fab fragments from a monoclonal antibody directed against the opioid receptor.一种针对阿片受体的单克隆抗体的Fab片段对μ和δ阿片受体与膜的结合有抑制作用，但对κ阿片受体与膜的结合无抑制作用。
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本文引用的文献

1
Intrathecal morphine in mice: a new technique.小鼠鞘内注射吗啡：一项新技术。
Eur J Pharmacol. 1980 Oct 17;67(2-3):313-6. doi: 10.1016/0014-2999(80)90515-4.
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ICI 174864: a highly selective antagonist for the opioid delta-receptor.ICI 174864：一种阿片δ受体的高选择性拮抗剂。
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Interaction of selective mu and delta ligands with the kappa 2 subtype of opiate binding sites.
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（+）-草酸埃博霉素因烟碱激动剂活性产生的抗伤害感受和毒性作用。
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In vivo studies on spinal opiate receptor systems mediating antinociception. II. Pharmacological profiles suggesting a differential association of mu, delta and kappa receptors with visceral chemical and cutaneous thermal stimuli in the rat.介导抗伤害感受的脊髓阿片受体系统的体内研究。II. 药理学特征表明大鼠体内μ、δ和κ受体与内脏化学刺激和皮肤热刺激存在不同关联。
J Pharmacol Exp Ther. 1984 Jan;228(1):1-12.
5
Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.双青霉胺脑啡肽对δ阿片受体具有高度改善的特异性。
Proc Natl Acad Sci U S A. 1983 Oct;80(19):5871-4. doi: 10.1073/pnas.80.19.5871.
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In vivo studies on spinal opiate receptor systems mediating antinociception. I. Mu and delta receptor profiles in the primate.
J Pharmacol Exp Ther. 1983 Aug;226(2):303-16.
7
Opiate receptor binding sites in human spinal cord.人类脊髓中的阿片受体结合位点。
Brain Res. 1983 May 16;267(2):392-6. doi: 10.1016/0006-8993(83)90897-1.
8
Multiple opiate binding sites in the central nervous system of the rabbit. Large predominance of a mu subtype in the cerebellum and characterization of a kappa subtype in the thalamus.兔中枢神经系统中的多个阿片类结合位点。小脑内μ亚型占主导，丘脑内κ亚型的特征描述。
Mol Pharmacol. 1983 Jul;24(1):23-9.
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In vivo evaluation of the opiate delta receptor antagonist ICI 154, 129.
Life Sci. 1982;31(12-13):1263-6. doi: 10.1016/0024-3205(82)90357-5.
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In vivo evidence for multiple opiate receptors mediating analgesia in the rat spinal cord.大鼠脊髓中多种阿片受体介导镇痛作用的体内证据。
Brain Res. 1982 Sep 9;247(1):75-83. doi: 10.1016/0006-8993(82)91029-0.