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[3H]环福辛,一种适用于正电子发射断层扫描的配体,可标记μ和κ阿片受体。

[3H]cyclofoxy, a ligand suitable for positron emission tomography, labels mu and kappa opioid receptors.

作者信息

McLean S, Rice K C, Lessor R, Rothman R B

机构信息

Laboratory of Neurophysiology, NIMH, Bethesda, MD 20892.

出版信息

Neuropeptides. 1987 Oct;10(3):235-9. doi: 10.1016/0143-4179(87)90073-4.

DOI:10.1016/0143-4179(87)90073-4
PMID:2825063
Abstract

The autoradiographic distribution of [3H]cyclofoxy (6-deoxy-6 beta-fluoronaltrexone) after in vivo administration or in vitro incubation suggests that it labels mu and kappa opioid receptors. In the rat, the pattern of [3H]cyclofoxy binding is similar to the distribution of mu receptors, however labeling is also present in the neural lobe of the pituitary, the central nucleus of the amygdala and the hypothalamus, areas where kappa receptors outnumber mu receptors. In the guinea pig, [3H]cyclofoxy binding sites are dense in the deep layers of the cortex, an area enriched in kappa receptors. These results are consistent with [3H]cyclofoxy binding to mu and kappa receptors.

摘要

体内给药或体外孵育后,[3H]环福可昔(6-脱氧-6β-氟纳曲酮)的放射自显影分布表明它标记了μ和κ阿片受体。在大鼠中,[3H]环福可昔结合模式与μ受体分布相似,然而在垂体神经叶、杏仁核中央核和下丘脑(这些区域κ受体数量超过μ受体)也有标记。在豚鼠中,[3H]环福可昔结合位点在皮质深层密集,该区域富含κ受体。这些结果与[3H]环福可昔与μ和κ受体结合一致。

相似文献

1
[3H]cyclofoxy, a ligand suitable for positron emission tomography, labels mu and kappa opioid receptors.[3H]环福辛,一种适用于正电子发射断层扫描的配体,可标记μ和κ阿片受体。
Neuropeptides. 1987 Oct;10(3):235-9. doi: 10.1016/0143-4179(87)90073-4.
2
An examination of the opiate receptor subtypes labeled by [3H]cycloFOXY: an opiate antagonist suitable for positron emission tomography.对由[3H]环FOXY标记的阿片受体亚型的研究:一种适用于正电子发射断层扫描的阿片拮抗剂。
Biol Psychiatry. 1988 Mar 1;23(5):435-58. doi: 10.1016/0006-3223(88)90016-9.
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A brief study of the selectivity of norbinaltorphimine, (-)-cyclofoxy, and (+)-cyclofoxy among opioid receptor subtypes in vitro.诺宾烷托啡诺、(-)-环福可昔、(+)-环福可昔在体外对阿片受体亚型选择性的简要研究。
Neuropeptides. 1988 Oct;12(3):181-7. doi: 10.1016/0143-4179(88)90052-2.
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The pattern of [3H]cyclofoxy retention in rat brain after in vivo injection corresponds to the in vitro opiate receptor distribution.体内注射后大鼠脑中[3H]环福司的保留模式与体外阿片受体分布一致。
Brain Res. 1987 Feb 3;402(2):275-86. doi: 10.1016/0006-8993(87)90034-5.
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Interaction of beta-funaltrexamine with [3H]cycloFOXY binding in rat brain: further evidence that beta-FNA alkylates the opioid receptor complex.β-芬太尼酰去甲丙胺与大鼠脑内[³H]环FOXY结合的相互作用:β-FNA使阿片受体复合物烷基化的进一步证据。
Synapse. 1991 Jun;8(2):86-99. doi: 10.1002/syn.890080203.
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Chronic morphine upregulates a mu-opiate binding site labeled by [3H]cycloFOXY: a novel opiate antagonist suitable for positron emission tomography.慢性吗啡上调由[3H]环FOXY标记的μ-阿片受体结合位点:一种适用于正电子发射断层扫描的新型阿片拮抗剂。
Eur J Pharmacol. 1987 Oct 6;142(1):73-81. doi: 10.1016/0014-2999(87)90655-8.
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Apparent down-regulation of rat brain mu- and kappa-opioid binding sites labelled with [3H]cycloFOXY following chronic administration of the potent 5-hydroxytryptamine reuptake blocker, clomipramine.在长期给予强效5-羟色胺再摄取阻滞剂氯米帕明后,用[3H]环福昔(cycloFOXY)标记的大鼠脑μ-和κ-阿片样物质结合位点出现明显下调。
J Pharm Pharmacol. 1989 Dec;41(12):865-7. doi: 10.1111/j.2042-7158.1989.tb06390.x.
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Anatomical distribution of mu, delta, and kappa opioid- and nociceptin/orphanin FQ-stimulated [35S]guanylyl-5'-O-(gamma-thio)-triphosphate binding in guinea pig brain.豚鼠脑中μ、δ和κ阿片受体以及孤啡肽/孤啡肽FQ刺激的[35S]鸟苷-5'-O-(γ-硫代)-三磷酸结合的解剖分布
J Comp Neurol. 1997 Oct 6;386(4):562-72. doi: 10.1002/(sici)1096-9861(19971006)386:4<562::aid-cne4>3.0.co;2-0.
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Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic.纳布啡:一种激动剂/拮抗剂镇痛药在中枢神经系统中的放射自显影阿片受体结合图谱。
J Pharmacol Exp Ther. 1988 Jan;244(1):391-402.
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Opioid receptor imaging with positron emission tomography and [(18)F]cyclofoxy in long-term, methadone-treated former heroin addicts.使用正电子发射断层扫描和[(18)F]环磷酰氧对长期接受美沙酮治疗的 former heroin addicts 进行阿片受体成像 。 注:“former heroin addicts”直译为“以前的海洛因成瘾者”,结合语境这里应该是指“曾经的海洛因成瘾者” 。
J Pharmacol Exp Ther. 2000 Dec;295(3):1070-6.

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