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用[3H]酪氨酸-D-丙氨酸-甘氨酸-(甲基)苯丙氨酸-甘醇(DAMGO)的氯甲基酮衍生物进行阿片样物质受体标记II:3H-酪氨酸-D-丙氨酸-甘氨酸-(甲基)苯丙氨酸氯甲基酮对μ阿片样物质结合位点的共价标记

Opioid receptor labeling with the chloromethyl ketone derivative of [3H]Tyr-D-Ala-Gly-(Me)Phe-Gly-ol (DAMGO) II: Covalent labeling of mu opioid binding site by 3H-Tyr-D-Ala-Gly-(Me)Phe chloromethyl ketone.

作者信息

Oktem H A, Moitra J, Benyhe S, Toth G, Lajtha A, Borsodi A

机构信息

Institute of Biochemistry, Hungarian Academy of Sciences, Szeged.

出版信息

Life Sci. 1991;48(18):1763-8. doi: 10.1016/0024-3205(91)90214-v.

DOI:10.1016/0024-3205(91)90214-v
PMID:1850495
Abstract

Opioid receptors of rat brain membranes were prelabeled with 3H-Tyr-D-Ala2-(Phe4)-Gly-CH2Cl, a chloromethyl ketone derivative of enkephalin, and solubilized in 1% digitonin. Hydrodynamic parameters of the receptor detergent complex derived from gel filtration and sucrose density gradient ultracentrifugation were found to be 51 A and 8.7 S, respectively, and the size was estimated to be about 200 kDa. Sodium dodecyl sulfate gel electrophoresis followed by fluorography revealed specific alkylation of a major protein at 58 kDa.

摘要

大鼠脑膜的阿片受体先用脑啡肽的氯甲基酮衍生物3H-Tyr-D-Ala2-(Phe4)-Gly-CH2Cl进行预标记,然后溶解于1%的洋地黄皂苷中。通过凝胶过滤和蔗糖密度梯度超速离心得到的受体去污剂复合物的流体动力学参数分别为51 Å和8.7 S,估计其大小约为200 kDa。十二烷基硫酸钠凝胶电泳后进行荧光自显影,结果显示主要蛋白质在58 kDa处发生特异性烷基化。

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Opioid receptor labeling with the chloromethyl ketone derivative of [3H]Tyr-D-Ala-Gly-(Me)Phe-Gly-ol (DAMGO) II: Covalent labeling of mu opioid binding site by 3H-Tyr-D-Ala-Gly-(Me)Phe chloromethyl ketone.用[3H]酪氨酸-D-丙氨酸-甘氨酸-(甲基)苯丙氨酸-甘醇(DAMGO)的氯甲基酮衍生物进行阿片样物质受体标记II:3H-酪氨酸-D-丙氨酸-甘氨酸-(甲基)苯丙氨酸氯甲基酮对μ阿片样物质结合位点的共价标记
Life Sci. 1991;48(18):1763-8. doi: 10.1016/0024-3205(91)90214-v.
2
Opioid receptor labeling with the chloromethyl ketone derivative of (3)H-Tyr-D-Ala-Gly-(Me)Phe-Gly-ol (DAMGO) I: Binding properties of 3H-Tyr-D-Ala-Gly-(Me)Phe chloromethyl.
Life Sci. 1991;48(18):1757-62. doi: 10.1016/0024-3205(91)90213-u.
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Tyr-D-Ala-Gly-(Me)Phe-chloromethyl ketone: a mu specific affinity label for the opioid receptor.
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Synthesis of 3H-Tyr-D-Ala-Gly-N(Me)Phe chloromethyl ketone--an opioid affinity label.3H-酪氨酸-D-丙氨酸-甘氨酸-N(甲基)苯丙氨酸氯甲基酮的合成——一种阿片样物质亲和标记物。
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Covalent labeling of opioid receptors with 3H-D-Ala2-Leu5-enkephalin chloromethyl ketone. I. Binding characteristics in rat brain membranes.用³H-D-丙氨酸²-亮氨酸⁵-脑啡肽氯甲基酮对阿片受体进行共价标记。I. 大鼠脑膜中的结合特性
Life Sci. 1987 Jul 13;41(2):177-84. doi: 10.1016/0024-3205(87)90491-7.
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Covalent labeling of opioid receptors with 3H-D-Ala2-Leu5-enkephalin chloromethyl ketone. II. Binding characteristics in frog brain membranes.用³H - D - 丙氨酸² - 亮氨酸⁵ - 脑啡肽氯甲基酮对阿片受体进行共价标记。II. 蛙脑膜中的结合特性
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Design of opioid peptides for a potential delta-receptor affinity label function: comparison with the mu-specific Tyr-D-Ala-Gly-(Me)Phe-chloromethyl ketone.
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Identification of an opioid receptor subunit carrying the mu binding site.鉴定携带μ结合位点的阿片受体亚基。
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Irreversible labelling of rat brain opioid receptors by enkephalin chloromethyl ketones.脑啡肽氯甲基酮对大鼠脑阿片受体的不可逆标记
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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。
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