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。
The use of [3H]-[D-Pen2,D-Pen5]enkephalin as a highly selective ligand for the delta-binding site.
作者信息
Cotton R, Kosterlitz H W, Paterson S J, Rance M J, Traynor J R
出版信息
Br J Pharmacol. 1985 Apr;84(4):927-32. doi: 10.1111/j.1476-5381.1985.tb17387.x.
Abstract
The characteristics of the binding of [3H]-[D-Pen2,D-Pen5]enkephalin were determined in homogenates of guinea-pig and rat brain. In the guinea-pig, the maximum binding capacity for [3H]-[D-Pen2,D-Pen5]enkephalin was 4.19 pmol g-1 and the KD 1.61 nM. In the rat, the corresponding values were 2.47 pmol g-1 and 5.42 nM. In both species, the maximum binding capacity and the affinity were not altered when mu-binding was suppressed with [D-Ala2,MePhe4,Gly-ol5]enkephalin. The mu-agonists, [D-Ala2,MePhe4,Gly-ol5]enkephalin and morphine, displaced a small portion of the binding of [3H]-[D-Pen2,D-Pen5]enkephalin with high affinities.
摘要
在豚鼠和大鼠脑匀浆中测定了[3H]-[D-青霉胺2，D-青霉胺5]脑啡肽的结合特性。在豚鼠中，[3H]-[D-青霉胺2，D-青霉胺5]脑啡肽的最大结合容量为4.19 pmol g-1，解离常数（KD）为1.61 nM。在大鼠中，相应的值分别为2.47 pmol g-1和5.42 nM。在这两个物种中，当用[D-丙氨酸2，甲硫氨酸苯丙氨酸4，甘醇5]脑啡肽抑制μ结合时，最大结合容量和亲和力均未改变。μ激动剂[D-丙氨酸2，甲硫氨酸苯丙氨酸4，甘醇5]脑啡肽和吗啡以高亲和力取代了一小部分[3H]-[D-青霉胺2，D-青霉胺5]脑啡肽的结合。
相似文献
1
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.
2
Characterization of [3H][2-D-penicillamine, 5-D-penicillamine]-enkephalin binding to delta opiate receptors in the rat brain and neuroblastoma--glioma hybrid cell line (NG 108-15).[3H][2-D-青霉胺，5-D-青霉胺]脑啡肽与大鼠脑及神经母细胞瘤-胶质瘤杂交细胞系（NG 108-15）中δ阿片受体结合的特性研究
Proc Natl Acad Sci U S A. 1985 Apr;82(8):2543-7. doi: 10.1073/pnas.82.8.2543.
3
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.
4
5
Binding of [3H][D-Ala2, MePhe4, Gly-ol5] enkephalin, [3H][D-Pen2, D-Pen5]enkephalin, and [3H]U-69,593 to airway and pulmonary tissues of normal and sensitized rats.[3H][D-丙氨酸2，甲基苯丙氨酸4，甘氨醇5]脑啡肽、[3H][D-青霉胺2，D-青霉胺5]脑啡肽以及[3H]U-69,593与正常和致敏大鼠气道及肺组织的结合。
Peptides. 1997;18(10):1603-8. doi: 10.1016/s0196-9781(97)00247-7.
6
7
Quantitative analysis of multiple kappa-opioid receptors by selective and nonselective ligand binding in guinea pig spinal cord: resolution of high and low affinity states of the kappa 2 receptors by a computerized model-fitting technique.通过选择性和非选择性配体结合对豚鼠脊髓中多种κ-阿片受体进行定量分析：利用计算机模型拟合技术解析κ2受体的高亲和力和低亲和力状态。
Mol Pharmacol. 1990 May;37(5):694-703.
8
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
Br J Pharmacol. 1990 Mar;99(3):503-8. doi: 10.1111/j.1476-5381.1990.tb12958.x.
9
Role of steric interactions in the delta opioid receptor selectivity of [D-Pen2, D-Pen5]enkephalin.空间相互作用在[D-青霉胺2，D-青霉胺5]脑啡肽的δ阿片受体选择性中的作用
Int J Pept Protein Res. 1988 Jul;32(1):1-8. doi: 10.1111/j.1399-3011.1988.tb00919.x.
10
Selectivity of ligand binding to opioid receptors in brain membranes from the rat, monkey and guinea pig.
Eur J Pharmacol. 1988 Apr 13;148(3):343-51. doi: 10.1016/0014-2999(88)90112-4.
引用本文的文献
1
Presynaptic opioid receptors on noradrenergic and serotonergic neurons in the human as compared to the rat neocortex.与大鼠新皮层相比，人类去甲肾上腺素能和5-羟色胺能神经元上的突触前阿片受体。
Br J Pharmacol. 2006 Jul;148(6):795-806. doi: 10.1038/sj.bjp.0706782. Epub 2006 Jun 5.
2
Opioid inhibition of hippocampal interneurons via modulation of potassium and hyperpolarization-activated cation (Ih) currents.阿片类药物通过调节钾离子和超极化激活阳离子（Ih）电流对海马中间神经元产生抑制作用。
J Neurosci. 1998 Sep 15;18(18):7084-98. doi: 10.1523/JNEUROSCI.18-18-07084.1998.
3
Characterization of opioid receptors in the cat carotid body involved in chemosensory depression in vivo.猫颈动脉体中参与体内化学感受性抑制的阿片受体的特征
Br J Pharmacol. 1986 Aug;88(4):889-98. doi: 10.1111/j.1476-5381.1986.tb16263.x.
4
Beta-endorphin-(1-27) is a naturally occurring antagonist of the reinforcing effects of opioids.β-内啡肽-（1-27）是一种天然存在的阿片类药物强化作用拮抗剂。
Naunyn Schmiedebergs Arch Pharmacol. 1988 Oct;338(4):392-6. doi: 10.1007/BF00172115.
5
Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins.在与GTP结合蛋白偶联的δ阿片受体上具有负性内在活性的拮抗剂。
Proc Natl Acad Sci U S A. 1989 Oct;86(19):7321-5. doi: 10.1073/pnas.86.19.7321.
6
Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding sites.强啡肽：一类对δ阿片样物质结合位点具有高亲和力和选择性的天然存在的肽。
Proc Natl Acad Sci U S A. 1989 Jul;86(13):5188-92. doi: 10.1073/pnas.86.13.5188.
7
[D-Pen2, D-Pen5]enkephalin, the standard delta opioid agonist, induces morphine-like behaviors in mice.
Psychopharmacology (Berl). 1990;102(3):425-6. doi: 10.1007/BF02244117.
8
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.
9
Different profile of electrocortical power spectrum changes after micro-infusion into the locus coeruleus of selective agonists at various opioid receptor subtypes in rats.大鼠蓝斑微量注射不同阿片受体亚型选择性激动剂后，皮质电图功率谱变化的不同特征。
Br J Pharmacol. 1990 Nov;101(3):655-61. doi: 10.1111/j.1476-5381.1990.tb14136.x.
10
Glial growth is regulated by agonists selective for multiple opioid receptor types in vitro.在体外，胶质细胞生长受多种阿片受体类型的选择性激动剂调控。
J Neurosci Res. 1991 Aug;29(4):538-48. doi: 10.1002/jnr.490290415.
本文引用的文献
1
Comparison of the binding characteristics of tritiated opiates and opioid peptides.氚标记阿片类药物与阿片肽结合特性的比较。
Br J Pharmacol. 1980 Nov;70(3):481-90. doi: 10.1111/j.1476-5381.1980.tb08727.x.
2
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.
3
Spectrum of the mu, delta- and kappa-binding sites in homogenates of rat brain.大鼠脑匀浆中μ、δ和κ结合位点的光谱
Br J Pharmacol. 1982 Nov;77(3):461-9. doi: 10.1111/j.1476-5381.1982.tb09319.x.
4
The binding spectrum of narcotic analgesic drugs with different agonist and antagonist properties.具有不同激动剂和拮抗剂特性的麻醉性镇痛药的结合光谱。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Jun;319(3):197-205. doi: 10.1007/BF00495865.
5
Selectivities of opioid peptide analogues as agonists and antagonists at the delta-receptor.阿片肽类似物作为δ受体激动剂和拮抗剂的选择性。
Br J Pharmacol. 1984 Sep;83(1):271-9. doi: 10.1111/j.1476-5381.1984.tb10143.x.
6
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.抑制常数（K1）与导致酶促反应50%抑制率（I50）的抑制剂浓度之间的关系。
Biochem Pharmacol. 1973 Dec 1;22(23):3099-108. doi: 10.1016/0006-2952(73)90196-2.
Zotero 插件