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Development of a sensitive chemiluminescent neuraminidase assay for the determination of influenza virus susceptibility to zanamivir

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ANALYTICAL BIOCHEMISTRY 2000年第2期280卷 291-300页

作者： Buxton, RC Edwards, B Juo, RR Voyta, JC Tisdale, M Bethell, RC Glaxo Wellcome Res & Dev Ltd Med Res Ctr Stevenage SG1 2NY Herts England Tropix Inc Bedford MA 01730 USA

Determination of the sensitivity of influenza viruses to neuraminidase (NA) inhibitors is presently based on assays of NA function because, unlike available cell culture methods, the results of such assays are predictive of susceptibility in vivo. At present the most widely used substrate in assays of NA function is the fluorogenic reagent 2'-O-(4-methylumbelliferyl)-N-acetylneuraminic acid (MUN). A rapid assay with improved sensitivity is required because a proportion of clinical isolates has insufficient NA to be detectable in the current fluorogenic assay, and because some mutations associated with resistance to NA inhibitors reduce the activity of the enzyme. A chemiluminescence-based assay of NA activity has been developed that uses a 1,2-dioxetane derivative of sialic acid (NA-STAR) as the substrate. When compared with the fluorogenic assay, use of the NA-STAR substrate results in a 67-fold reduction in the limit of detection of the NA assay, from 200 pM (11 fmol) NA to 3 pM (0.16 fmol) NA. A panel of isolates from phase 2 clinical studies of zanamivir, which were undetectable in the fluorogenic assay, was tested for activity using the NA-STAR substrate. Of these 12 isolates with undetectable NA activity, 10 (83%) were found to have detectable NA activity using the NA-STAR substrate. A comparison of sensitivity to zanamivir of a panel of influenza A and B viruses using the two NA assay methods has been performed. IC50 values for zanamivir using the NA-STAR were in the range 1.0-7.5 nM and those for the fluorogenic assay in the range 1.0-5.7 nM (n = 6). The NA-STAR assay is a highly sensitive, rapid assay of influenza virus NA activity that is applicable to monitoring the susceptibility of influenza virus clinical isolates to NA inhibitors. (C) 2000 Academic Press.

关键词：金刚烷/类似物和衍生物抗病毒药/药理学化学发光测定法酶抑制剂/药理学胍类微生物敏感性试验/方法神经氨酸酶/分析神经氨酸酶/拮抗剂和抑制剂神经氨酸酶/代谢正黏病毒科/药物作用吡喃类敏感性与特异性唾液酸类/药理学光谱法荧光/方法糖酸类扎那米韦

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Cellular uptake of adamantyl conjugated peptide nucleic acids

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BIOCONJUGATE CHEMISTRY 1999年第6期10卷 965-972页

作者： Ljungstrom, T Knudsen, H Nielsen, PE Univ Copenhagen Panum Inst Ctr Biomol Recognit Dept Med Biochem & GenetBiochem Lab B DK-2200 Copenhagen N Denmark

Peptide nucleic acids (PNA) (15-mers) conjugated to adamantyl acetic acid and labeled with fluorescein have been prepared, and their (liposome mediated) uptake in human cells in culture (HeLa, IMR-90 and MDA-MB-453) has been studied by confocal fluorescence microscopy. It is found that adamantyl-PNAs show greatly improved (endosomal) cellular uptake, but that this uptake is dependent on the cell line. Cellular uptake of such lipophilic PNAs is further mediated by cationic liposomes, and in some cases, the intracellular localization is diffuse cytoplasmic or nuclear, again cell-type dependent. The results show that this simple PNA modification can indeed greatly improve cellular uptake, but the effect appears strongly cell-type as well as PNA-sequence dependent.

关键词：金刚烷/类似物和衍生物金刚烷/化学乳腺肿瘤细胞系药物载体荧光染料 HeLa细胞脂质体显微镜检查共焦显微镜检查荧光肽核酸类/投药和剂量肽核酸类/化学肽核酸类/代谢磷脂酰乙醇胺类季胺类化合物肿瘤细胞培养的人类

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ANTIVIRAL AGENTS .11. NUCLEOPHILIC SUBSTITUTIONS AND ADDITIONS WITH 2-AMINOADAMANTANE

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ARCHIV DER PHARMAZIE 1976年第11期309卷 919-925页

作者： KREUTZBERGER, A SCHRODERS, HH FREE UNIV BERLIN INST PHARM D-1000 BERLIN 33 GERMANY UNIV MUNSTER INST PHARM CHEM D-4400 MUNSTER GERMANY

Derivatives of 2-aminoadamantane (1) were prepared and compared with derivatives of 1-aminoadamantane for antiviral activity. Reaction of 1 with isothiocyanates yields the N''-substituted N-(2-adamantyl) thiou... 详细信息

关键词：金刚烷/类似物和衍生物金刚烷/化学合成抗病毒药/化学合成桥基化合物/化学合成

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ANTIVIRAL AGENTS .6. VARIATION OF SUBSTITUENTS IN SERIES OF N'-SUBSTITUTED N-[ADAMANTYL-(1)]-THIOUREAS

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ARCHIV DER PHARMAZIE 1975年第10期308卷 748-754页

作者： KREUTZBERGER, A SCHRODERS, HH FREIE UNIV BERLIN INST PHARMKONIGIN LUISE STR 2-41 BERLINFED REP GER WESTFAL WILHELMS UNIV INST PHARM CHEMMUNSTERFED REP GER

Aus der Umsetzung des 1‐Amino‐adamantans ( 1 ) mit Isothiocyanaten 2 gehen die N‐[Adamantyl‐(1)]‐thioharnstoffe 3 hervor. Die Verbindungen 3a, b, c und d weisen auffallende antivirale Wirksamkeit auf. Thiosemicarbazonbildung zu 6 erfolgt bei der Einwirkung von Aldehyden, wie Anisaldehyd ( 5 ), auf 4‐[Adamantyl‐(1)]‐thiosemicarbazid ( 4 ). Variation of Substituents in the Series of N′‐Substituted N‐[Adamantyl‐(1)]‐thioureas . N‐[Adamantyl‐(1)]‐thioureas 3 arise from the interaction of 1‐amino‐adamantane ( 1 ) with isothiocyanates 2 . Compounds 3a, b, c , and d exhibit marked antiviral activity. Thiosemicarbazone ( 6 ) formation occurs upon the action of aldehydes, like anisaldehyde ( 5 ), on 4‐[adamantyl‐(1)]‐thiosemicarbazide ( 4 ).

关键词：金刚烷/类似物和衍生物金刚烷/化学合成抗病毒药/化学合成桥基化合物/化学合成硫脲/类似物和衍生物硫脲/化学合成

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AEROSOL THERAPY OF INFLUENZA INFECTIONS OF MICE AND PRIMATES WITH RIMANTADINE, RIBAVIRIN, AND RELATED COMPOUNDS

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ANNALS OF THE NEW YORK ACADEMY OF SCIENCES 1977年第MAR4期284卷 264-271页

作者： STEPHEN, EL WALKER, JS DOMINIK, JW YOUNG, HW BERENDT, RF USA MED RES INST INFECT DISDIV ANIM ASSESSMENTFREDERICKMD 21701

Ribavirin administered as small-article aerosols had significant therapeutic effect in the treatment of viral respiratory infections induced by influenza virus. The preliminary experiment using ribavirin to treat influenza infection in the squirrel monkey is encouraging. We expect to extend these experiments by initiating therapy at a later time to investigate the potential value of ribavirin in a clinical situation. Several derivatives of ribavirin are effective antiviral compounds. The tri-O-acetyl derivative appears to offer a potential advantage over ribavirin, although this cannot be stated with certainty since the data were obtained from separate experiments. Radiolabeling has been used as a means of measuring tissue concentration and clearance rates of various drugs. It is hoped that the use of labeled ribavirin and the tri-O-acetyl derivative will assist us in determining whether a depot of antiviral drug is created in pulmonary tissues after administration as a small-particle aerosol. These experiments are now in progress.

关键词：金刚烷/投药和剂量金刚烷/类似物和衍生物金刚烷/治疗应用气雾剂抗病毒药/投药和剂量抗病毒药/治疗应用直鼻猴亚目正黏病毒科感染/药物疗法利巴韦林/投药和剂量利巴韦林/类似物和衍生物利巴韦林/治疗应用核糖核苷类/治疗应用松鼠猴属动物女(雌)性小鼠

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Neurotensin stimulates Cl^- secretion in human colonic mucosa in vitro:: Role of adenosine

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GASTROENTEROLOGY 2000年第2期119卷 348-357页

作者： Riegler, M Castagliuolo, I Wang, C Wlk, M Sogukoglu, T Wenzl, E Matthews, JB Pothoulakis, C Beth Israel Deaconess Med Ctr Div Gastroenterol Boston MA 02215 USA Beth Israel Deaconess Med Ctr Dept Surg Boston MA 02215 USA Univ Vienna Vienna Gen Hosp Surg Clin Vienna Austria

Background & Aims: Previous studies indicated that the peptide neurotensin (NT) stimulates Cl- secretion in animal small intestinal mucosa in vitro, In this study, we investigated whether NT causes Cl- secretion in human colonic mucosa and examined the mechanism of this response, Methods: Human mucosal preparations mounted in Ussing chambers were exposed to NT. Drugs for pharmacologic characterization of NT-induced responses were applied 30 minutes before NT. Results: Serosal, but not luminal, administration of NT (10(-8) to 10(-6) mol/L) induced a rapid, monophasic, concentration- and chloride-dependent, bumetanide-sensitive short-circuit current (Isc) increase that was inhibited by the specific nonpeptide NT receptor antagonists SR 48692 and SR 142948A, the neuronal blocker tetrodotoxin, and the prostaglandin synthesis inhibitor indomethacin, The mast cell stabilizer lodoxamide and the histamine 1 and 2 receptor antagonists pyrilamine and ranitidine, respectively, did not significantly alter NT-induced Ise increase. In contrast, the adenosine receptor 1 and 2 antagonists inhibited this secretory response, whereas the adenosine uptake inhibitors S-(4-nitrobenzyl)-6-thioguanosine and S-(4-nitrobenzyl)-6-thioinosine and the adenosine deaminase inhibitor deoxycoformycin potentiated NT-induced Ise increase. Serosal adenosine induced a rapid, monophasic, concentration- and chloride-dependent, bumetanide-sensitive rsc increase, Conclusions: NT stimulates chloride secretion in human colon by a pathway(s) involving mucosal nerves, adenosine, and prostaglandins.

关键词：金刚烷/类似物和衍生物金刚烷/药理学腺苷/代谢腺苷/药理学腺苷脱氨酶抑制剂亲和力标记物/药理学消炎药非甾类/药理学细胞培养的氯化物/代谢结肠/细胞学结肠/神经支配电生理学肠神经系统/化学肠神经系统/药物作用肠神经系统/生理学酶抑制剂/药理学鸟苷/类似物和衍生物鸟苷/药理学组胺/代谢咪唑类/药理学吲哚美辛/药理学肠黏膜/酶学肠黏膜/神经支配肠黏膜/代谢肥大细胞/代谢膜电位/药物作用膜电位/生理学神经降压肽/药理学喷司他丁/药理学吡唑类/药理学喹啉类/药理学受体神经降压肽/分析受体神经降压肽/拮抗剂和抑制剂受体神经降压肽/生理学河豚毒素/药理学硫代肌苷/类似物和衍生物硫代肌苷/药理学硫代核苷类/药理学人类

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Cytotoxic polyprenylated benzoylphloroglucinol derivatives with an unusual adamantyl skeleton from Hypericum sampsonii (Guttiferae)

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ORGANIC LETTERS 1999年第6期1卷 879-882页

作者： Lu, LH Sim, KY Natl Univ Singapore Dept Chem Singapore 119260 Singapore

[GRAPHICS] The structures of sampsoniones I and J, isolated from the aerial parts of the Chinese medicinal plant Hypericum sampsonii, have been elucidated by detailed spectral analysis. They are complex adamantyl derivatives, and sampsonione I is the first polyprenylated benzoylphloroglucinol derivative with the unique caged tetracyclo[7.3.1.1(3,11).0(3,8)]tetradecane-2,12,14-trione skeleton. Cytotoxic sampsonione I has also been obtained by the biomimetic transformation of sampsonione J.

关键词：金刚烷/类似物和衍生物金刚烷/化学金丝桃属/化学磁共振波谱学质谱分析法分子模拟分子结构植物药用

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The trapping block of NMDA receptor channels in acutely isolated rat hippocampal neurones

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JOURNAL OF PHYSIOLOGY-LONDON 2000年第3期526卷 493-506页

作者： Sobolevsky, AI Yelshansky, MV Russian Acad Med Sci Inst Gen Pathol & Pathol Physiol Moscow 125315 Russia

1. N-methyl-D-aspartate (NMDA) receptor responses were recorded from acutely isolated rat hippocampal neurones using the whole-cell patch-clamp, technique. A rapid perfusion system was used to study the voltage-dependent block of NMDA channels by Mg2+, amantadine (AM) and N-2-(adamantyl)-hexamethylenimine (A-7). 2. Mg2+, AM and A-7-induced stationary blockade of NMDA channels increased with the blocker concentration but did not depend on the agonist (aspartate;Asp) concentration. Blockade by AM and A-7, but not Mg2+, was weakly use dependent. 3. 'Hooked' tail currents were observed after coapplication of Asp and Mg2+, AM or A-7. The hooked tail current kinetics, amplitude and carried charge indicated that Mg2+, AM and A-7 did not prevent closure and desensitization of NMDA channels nor agonist dissociation. 4. Tail currents following Asp application in the absence and continuous presence of Mg2+, AM or A-7 had similar kinetics. 5. Application of multiple stationary and kinetic criteria to the Mg2+, AM and A-7 blockade led us to conclude that their effects on NMDA channels can be described in terms of a 'trapping' model, which is fully symmetrical with respect to the blocking transition. 6. In general, the apparent blocking/recovery kinetics predicted by the fully symmetrical trapping model differ significantly from the microscopic kinetics and depend on the rate of binding and unbinding of the blocker, the NMDA channel open probability and the rate of solution exchange.

关键词：金刚烷/类似物和衍生物金刚烷/药理学金刚烷胺/代谢金刚烷胺/药理学抗震颤麻痹药/药理学天冬氨酸/代谢天冬氨酸/药理学细胞分离多巴胺药/药理学剂量效应关系药物海马/细胞学海马/药物作用海马/代谢离子通道/药物作用离子通道/代谢镁/代谢镁/药理学膜电位/药物作用神经元/细胞学神经元/药物作用神经元/代谢膜片钳术灌流大鼠 Wistar 受体 N-甲基-D-天冬氨酸/激动剂受体 N-甲基-D-天冬氨酸/拮抗剂和抑制剂受体 N-甲基-D-天冬氨酸/代谢动物大鼠

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N-[1-(2-phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT₂ receptor antagonists

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 2000年第21期10卷 2457-2461页

作者： Fujio, M Kuroita, T Sakai, Y Nakagawa, H Matsumoto, Y Welfide Corp Drug Discovery Labs Exploratory Res 1 Iruma Saitama 3580026 Japan Welfide Corp Drug Discovery Labs Exploratory Res 2 Hirakata Osaka 5731153 Japan Welfide Corp Drug Dev Labs Dept Pharmacol Yoshitomi Fukuoka 8718550 Japan

A series of 1-adamantanecarboxamides was synthesized and examined for their potency as a selective 5-HT2 receptor antagonist. We found (S)-N-{1 -[2-(4-fluorophenyl)ethyl]pyrrolidin-3-yl}-1-adamantanecarboxamide hydrochloride hydrate (10-(S), Y-39241) to have a high affinity and selectivity for 5-HT2 receptors, and this potent anti-platelet effect of Y-39241 was confirmed both in vitro and in vivo. (C) 2000 Elsevier Science Ltd. All rights reserved.

关键词： 8-羟-2-(二-n-丙胺)四氢萘/代谢金刚烷/类似物和衍生物金刚烷/化学合成金刚烷/化学金刚烷/代谢金刚烷/药理学脑化学酮色林/代谢分子结构血小板聚集抑制剂/化学合成血小板聚集抑制剂/化学血小板聚集抑制剂/代谢血小板聚集抑制剂/药理学吡咯烷类/化学合成吡咯烷类/化学吡咯烷类/代谢吡咯烷类/药理学大鼠 Wistar 受体血清素/代谢受体血清素 5-HT1 血清素拮抗药/化学合成血清素拮抗药/化学血清素拮抗药/代谢血清素拮抗药/药理学动物男(雄)性兔大鼠

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Specific inhibitors of influenza virus replication as potential chemoprophylactic agents

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Journal of Antimicrobial Chemotherapy 1975年第1期1卷 7-23页

作者： Oxford, J.S. Division of Virology National Institute for Medical Research London N.W.7 England Mill Hill United Kingdom

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