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荧光麻醉剂

Fluorescent Anesthetics.

作者信息

Emerson Daniel J, Dmochowski Ivan J

机构信息

University of Pennsylvania, Philadelphia, PA, United States.

University of Pennsylvania, Philadelphia, PA, United States.

出版信息

Methods Enzymol. 2018;603:93-101. doi: 10.1016/bs.mie.2018.02.006. Epub 2018 Apr 4.

DOI:10.1016/bs.mie.2018.02.006
PMID:29673536
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6636835/
Abstract

Methods for using exogenous fluorophore and general anesthetic 1-aminoanthracene (1-AMA) and its photoactive derivative 1-azidoanthracene (1-AZA) are provided. 1-AMA potentiates GABA chloride currents and immobilizes Xenopus laevis tadpoles. Cellular and tissue anesthetic distribution can be imaged for quantifying "on-pathway" and "off-pathway" targets. 1-AZA shares targets with 1-AMA and offers further optoanesthetic spatial and temporal control upon near-UV laser irradiation. Furthermore, 1-AZA adduction provides screening of possible relevant anesthetic protein targets and binding site characterization. We highlight several useful imaging and binding assays to demonstrate utility of 1-AMA and its derivative 1-AZA.

摘要

提供了使用外源性荧光团以及全身麻醉剂1-氨基蒽（1-AMA）及其光活性衍生物1-叠氮基蒽（1-AZA）的方法。1-AMA可增强γ-氨基丁酸氯离子电流并使非洲爪蟾蝌蚪固定不动。细胞和组织中的麻醉剂分布可以成像，以量化“通路内”和“通路外”靶点。1-AZA与1-AMA具有共同靶点，并在近紫外激光照射时提供进一步的光麻醉空间和时间控制。此外，1-AZA加合物可用于筛选可能相关的麻醉蛋白靶点并表征结合位点。我们重点介绍了几种有用的成像和结合测定方法，以证明1-AMA及其衍生物1-AZA的实用性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39b0/6636835/f39ca0317ce9/nihms-1022387-f0001.jpg

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本文引用的文献

1
Direct modulation of microtubule stability contributes to anthracene general anesthesia.直接调节微管稳定性有助于蒽类全身麻醉。
J Am Chem Soc. 2013 Apr 10;135(14):5389-98. doi: 10.1021/ja311171u. Epub 2013 Mar 29.
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A neurosteroid analogue photolabeling reagent labels the colchicine-binding site on tubulin: a mass spectrometric analysis.一种神经甾体类似物光标记试剂标记微管蛋白上的秋水仙素结合位点：质谱分析。
Electrophoresis. 2012 Feb;33(4):666-74. doi: 10.1002/elps.201100434.
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A novel fluorescent general anesthetic enables imaging of sites of action in vivo.
Anesthesiology. 2012 Jun;116(6):1363. doi: 10.1097/ALN.0b013e31824cb4b1.
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High-affinity fluorescent ligands for the 5-HT(3) receptor.高亲和力荧光配体用于 5-HT(3)受体。
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1151-5. doi: 10.1016/j.bmcl.2011.11.097. Epub 2011 Dec 1.
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Identification of a fluorescent general anesthetic, 1-aminoanthracene.一种荧光全身麻醉剂1-氨基蒽的鉴定。
Proc Natl Acad Sci U S A. 2009 Apr 21;106(16):6501-6. doi: 10.1073/pnas.0810590106. Epub 2009 Apr 3.
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ANS fluorescence: potential to augment the identification of the external binding sites of proteins.ANS荧光：增强蛋白质外部结合位点识别的潜力。
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General anesthetic potencies of a series of propofol analogs correlate with potency for potentiation of gamma-aminobutyric acid (GABA) current at the GABA(A) receptor but not with lipid solubility.一系列丙泊酚类似物的全身麻醉效能与γ-氨基丁酸（GABA）在GABA（A）受体处电流增强的效能相关，但与脂溶性无关。
J Pharmacol Exp Ther. 2001 Apr;297(1):338-51.
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Fluorescent protein spectra.荧光蛋白光谱。
J Cell Sci. 2001 Mar;114(Pt 5):837-8. doi: 10.1242/jcs.114.5.837.
9
Binding of quinacrine, a fluorescent local anesthetic probe, to mammalian axonal membranes. Evidence for a local anesthetic receptor site.荧光局部麻醉探针喹吖因与哺乳动物轴突膜的结合。局部麻醉受体位点的证据。
J Biol Chem. 1982 Aug 10;257(15):8964-71.
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Studies on the fluorescence of 1-anilino-8-naphthalenesulfonate by the membranes of the sarcoplasmic reticulum.关于肌质网膜对1-苯胺基-8-萘磺酸盐荧光的研究。
Eur J Biochem. 1973 May;35(1):114-21. doi: 10.1111/j.1432-1033.1973.tb02816.x.

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