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苯二氮䓬受体的光亲和标记损害识别位点,但不影响其效应机制。

Photoaffinity labelling of the benzodiazepine receptor compromises the recognition site but not its effector mechanism.

作者信息

Brown C L, Martin I L

出版信息

J Neurochem. 1984 Jul;43(1):272-3. doi: 10.1111/j.1471-4159.1984.tb06707.x.

DOI:10.1111/j.1471-4159.1984.tb06707.x
PMID:6327919
Abstract

When subjected to ultraviolet light flunitrazepam could be irreversibly attached to brain membrane preparations such that the affinity of the benzodiazepine receptor for certain ligands, such as diazepam, becomes markedly reduced. However, the apparent affinity for diazepam is increased by the addition of gamma-aminobutyric acid and sodium chloride, to the same extent in this membrane preparation as in membranes not so pretreated. This observation suggests that photoaffinity labelling of the benzodiazepine receptor with flunitrazepam modifies the recognition characteristics of the receptor but not its effector mechanism.

摘要

当受到紫外线照射时,氟硝西泮可不可逆地附着于脑膜制剂上,使得苯二氮䓬受体对某些配体(如地西泮)的亲和力显著降低。然而,在该脑膜制剂中,加入γ-氨基丁酸和氯化钠后,地西泮的表观亲和力增加,增加程度与未进行如此预处理的膜相同。这一观察结果表明,用氟硝西泮对苯二氮䓬受体进行光亲和标记会改变受体的识别特性,但不会改变其效应机制。

相似文献

1
Photoaffinity labelling of the benzodiazepine receptor compromises the recognition site but not its effector mechanism.苯二氮䓬受体的光亲和标记损害识别位点,但不影响其效应机制。
J Neurochem. 1984 Jul;43(1):272-3. doi: 10.1111/j.1471-4159.1984.tb06707.x.
2
Flunitrazepam photoaffinity labeling of the GABA(A) receptor reduces inhibition of [3H]Ro15-4513 binding by GABA.氟硝西泮对GABA(A)受体的光亲和标记降低了GABA对[3H]Ro15 - 4513结合的抑制作用。
Eur J Pharmacol. 1990 Jun 12;188(6):391-7. doi: 10.1016/0922-4106(90)90199-8.
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Photoaffinity labeling of benzodiazepine receptors in rat brain with flunitrazepam alters the affinity of benzodiazepine receptor agonist but not antagonist binding.
J Neurochem. 1983 Nov;41(5):1407-13. doi: 10.1111/j.1471-4159.1983.tb00839.x.
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Photoaffinity labelling of the benzodiazepine receptor cannot be used to predict ligand efficacy.
Neurosci Lett. 1983 Jan 31;35(1):37-40. doi: 10.1016/0304-3940(83)90523-2.
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Benzodiazepine receptor protein identified and visualized in brain tissue by a photoaffinity label.通过光亲和标记在脑组织中鉴定并可视化的苯二氮䓬受体蛋白。
Proc Natl Acad Sci U S A. 1980 Mar;77(3):1666-70. doi: 10.1073/pnas.77.3.1666.
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Photoaffinity labeling of different benzodiazepine receptors at physiological temperature.生理温度下不同苯二氮䓬受体的光亲和标记
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Effect of GABA and photoaffinity labelling on the affinity of drugs for benzodiazepine receptors in membranes of the cerebral cortex of five-day-old rats.
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gamma-Aminobutyric acid/benzodiazepine receptor protein carries binding sites for both ligands on both two major peptide subunits.
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Comparison of the kinetics of [3H]diazepam and [3H]flunitrazepam binding to cortical synaptosomal membranes.
J Neurochem. 1982 Dec;39(6):1716-25. doi: 10.1111/j.1471-4159.1982.tb08008.x.
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Distinction of benzodiazepine agonists from antagonists by photoaffinity labelling of benzodiazepine receptors in vitro.通过体外苯二氮䓬受体的光亲和标记区分苯二氮䓬激动剂与拮抗剂
Neurosci Lett. 1982 Jul 20;31(1):65-9. doi: 10.1016/0304-3940(82)90055-6.

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