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亮氨酸脑啡肽非竞争性抑制[3H]纳洛酮与阿片μ-识别位点的结合:体外δ----μ结合位点相互作用的证据。

Leucine enkephalin noncompetitively inhibits the binding of [3H]naloxone to the opiate mu-recognition site: evidence for delta----mu binding site interactions in vitro.

作者信息

Rothman R B, Danks J A, Jacobson A E, Burke T R, Rice K C

出版信息

Neuropeptides. 1985 Jul;6(4):351-63. doi: 10.1016/0143-4179(85)90008-3.

DOI:10.1016/0143-4179(85)90008-3
PMID:2995865
Abstract

Using quantitative methods, this study examined the hypothesis that delta-ligands are noncompetitive inhibitors at a population of mu-binding sites. Evidence is presented that with the defined set of in vitro assay conditions utilized, [3H]naloxone labels two binding sites: the mu binding site and a second site tentatively identified as a kappa binding site, and that leucine enkephalin is a noncompetitive inhibitor at the mu recognition site.

摘要

本研究采用定量方法检验了δ-配体在一群μ-结合位点上为非竞争性抑制剂的假说。结果表明,在所使用的特定体外试验条件下,[3H]纳洛酮标记了两个结合位点:μ-结合位点和另一个暂定为κ-结合位点的位点,并且亮氨酸脑啡肽在μ-识别位点上为非竞争性抑制剂。

相似文献

1
Leucine enkephalin noncompetitively inhibits the binding of [3H]naloxone to the opiate mu-recognition site: evidence for delta----mu binding site interactions in vitro.亮氨酸脑啡肽非竞争性抑制[3H]纳洛酮与阿片μ-识别位点的结合:体外δ----μ结合位点相互作用的证据。
Neuropeptides. 1985 Jul;6(4):351-63. doi: 10.1016/0143-4179(85)90008-3.
2
Antagonist-induced opioid receptor up-regulation. II. Regionally specific modulation of mu, delta and kappa binding sites in rat brain revealed by quantitative autoradiography.拮抗剂诱导的阿片受体上调。II. 定量放射自显影揭示大鼠脑中μ、δ和κ结合位点的区域特异性调节。
J Pharmacol Exp Ther. 1988 Nov;247(2):729-36.
3
A quantitative study of [3H]D-Ala2-D-Leu5-enkephalin binding to rat brain membranes. Evidence that oxymorphone is a noncompetitive inhibitor of the lower affinity delta-binding site.[3H]D-丙氨酸2-D-亮氨酸5-脑啡肽与大鼠脑膜结合的定量研究。氧吗啡酮是低亲和力δ结合位点的非竞争性抑制剂的证据。
Mol Pharmacol. 1985 Mar;27(3):399-409.
4
Computer-assisted analysis of receptor-binding studies of [3H]-naloxone and [3H]-DADL: a reinterpretation of the Na+ effect.[3H]-纳洛酮和[3H]-DADL受体结合研究的计算机辅助分析:对钠离子效应的重新诠释
Life Sci. 1983;33 Suppl 1:163-6. doi: 10.1016/0024-3205(83)90469-1.
5
Naloxonazine effects on the interaction of enkephalin analogs with mu-1, mu and delta opioid binding sites in rat brain membranes.纳洛酮嗪对脑啡肽类似物与大鼠脑膜中μ-1、μ和δ阿片样物质结合位点相互作用的影响。
J Pharmacol Exp Ther. 1987 Jul;242(1):15-20.
6
Sodium regulation of agonist binding at opioid receptors. I. Effects of sodium replacement on binding at mu- and delta-type receptors in 7315c and NG108-15 cells and cell membranes.阿片受体激动剂结合的钠调节。I. 钠替代对7315c和NG108-15细胞及细胞膜中μ型和δ型受体结合的影响。
Mol Pharmacol. 1986 Aug;30(2):81-9.
7
Opiate receptor binding in the brain of rat during stress.应激期间大鼠大脑中的阿片受体结合
Pavlov J Biol Sci. 1988 Apr-Jun;23(2):54-6. doi: 10.1007/BF02995655.
8
Reversible and irreversible binding of beta-funaltrexamine to mu, delta and kappa opioid receptors in guinea pig brain membranes.β-芬太尼环丙基甲基酮在豚鼠脑膜中与μ、δ和κ阿片受体的可逆和不可逆结合。
J Pharmacol Exp Ther. 1986 Nov;239(2):351-7.
9
Effect of electroconvulsive treatment on cerebral opioid receptors in the rat: changes in delta but not mu receptors.电休克治疗对大鼠脑阿片受体的影响:δ受体而非μ受体发生变化。
Naunyn Schmiedebergs Arch Pharmacol. 1984 Nov;328(1):87-9. doi: 10.1007/BF00496112.
10
Interaction of leucine enkephalin with (3H)naloxone binding in rat brain: evidence for an opioid receptor complex.
Neurochem Res. 1983 Jul;8(7):913-31. doi: 10.1007/BF00964552.

引用本文的文献

1
Differential maturation of mu and delta opioid receptors in the chick embryonic brain.鸡胚脑中μ和δ阿片受体的差异成熟
Neurochem Res. 1987 Mar;12(3):279-88. doi: 10.1007/BF00972138.
2
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.