Organophosphorus compounds and oximes: a critical review.

Abstract:

:Organophosphorus (OP) pesticides and nerve agents still pose a threat to the population. Treatment of OP poisoning is an ongoing challenge and burden for medical services. Standard drug treatment consists of atropine and an oxime as reactivator of OP-inhibited acetylcholinesterase and is virtually unchanged since more than six decades. Established oximes, i.e. pralidoxime, obidoxime, TMB-4, HI-6 and MMB-4, are of insufficient effectiveness in some poisonings and often cover only a limited spectrum of the different nerve agents and pesticides. Moreover, the value of oximes in human OP pesticide poisoning is still disputed. Long-lasting research efforts resulted in the preparation of countless experimental oximes, and more recently non-oxime reactivators, intended to replace or supplement the established and licensed oximes. The progress of this development is slow and none of the novel compounds appears to be suitable for transfer into advanced development or into clinical use. This situation calls for a critical analysis of the value of oximes as mainstay of treatment as well as the potential and limitations of established and novel reactivators. Requirements for a straightforward identification of superior reactivators and their development to licensed drugs need to be addressed as well as options for interim solutions as a chance to improve the therapy of OP poisoning in a foreseeable time frame.

journal_name

Arch Toxicol

journal_title

Archives of toxicology

authors

Worek F,Thiermann H,Wille T

doi

10.1007/s00204-020-02797-0

subject

Has Abstract

pub_date

2020-07-01 00:00:00

pages

2275-2292

issue

7

eissn

0340-5761

issn

1432-0738

pii

10.1007/s00204-020-02797-0

journal_volume

94

pub_type

杂志文章,评审
  • Upregulation of hydroxysteroid sulfotransferase 2B1b promotes hepatic oval cell proliferation by modulating oxysterol-induced LXR activation in a mouse model of liver injury.

    abstract::Hydroxysteroid sulfotransferase 2B1b (SULT2B1b) sulfates cholesterol and oxysterols. Hepatic oval cells (HOCs), thought to be progenitor cells, can be triggered in chemically injured livers. The present study focused on the role of SULT2B1b in HOC proliferation after liver injury. Our experiments revealed that the exp...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-016-1693-z

    authors: Wang Z,Yang X,Chen L,Zhi X,Lu H,Ning Y,Yeong J,Chen S,Yin L,Wang X,Li X

    更新日期:2017-01-01 00:00:00

  • Inhibitory effect of berberine on tert-butyl hydroperoxide-induced oxidative damage in rat liver.

    abstract::Berberine, a main protoberberine component of Coptidis Rhizoma, was studied for the mechanism of its inhibitory effects on the tert-butyl hydroperoxide (t-BHP)-induced cytotoxicity and lipid peroxidation in rat liver. In the preliminary study, berberine expressed an antioxidant property by its capacity for quenching t...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-002-0351-9

    authors: Hwang JM,Wang CJ,Chou FP,Tseng TH,Hsieh YS,Lin WL,Chu CY

    更新日期:2002-11-01 00:00:00

  • Chemical and biological properties of toxic metals and use of chelating agents for the pharmacological treatment of metal poisoning.

    abstract::Exposure to toxic metals is a well-known problem in industrialized countries. Metals interfere with a number of physiological processes, including central nervous system (CNS), haematopoietic, hepatic and renal functions. In the evaluation of the toxicity of a particular metal it is crucial to consider many parameters...

    journal_title:Archives of toxicology

    pub_type: 杂志文章,评审

    doi:10.1007/s00204-010-0544-6

    authors: Sinicropi MS,Amantea D,Caruso A,Saturnino C

    更新日期:2010-07-01 00:00:00

  • Sexual dimorphism of cadmium-induced toxicity in rats: involvement of sex hormones.

    abstract::The toxic effect of cadmium varies with sex in experimental animals. Previous studies have demonstrated that pretreatment of male Fischer 344 (F344) rats with the female sex hormone progesterone markedly enhances the susceptibility to cadmium, suggesting a role for progesterone in the sexual dimorphism of cadmium toxi...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-012-0844-0

    authors: Shimada H,Hashiguchi T,Yasutake A,Waalkes MP,Imamura Y

    更新日期:2012-09-01 00:00:00

  • Selective poisoning of Ctnnb1-mutated hepatoma cells in mouse liver tumors by a single application of acetaminophen.

    abstract::Mouse liver tumors that harbor activating mutations in Ctnnb1, encoding β-catenin, express high levels of various cytochromes P450 (CYP), including CYP2E1 and CYP1A2. Acetaminophen (AAP) is metabolized in hepatocytes by these CYPs to the reactive intermediate N-acetyl-p-benzoquinone-imine, which is toxic to hepatocyte...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-013-1030-8

    authors: Singh Y,Braeuning A,Schmid A,Pichler BJ,Schwarz M

    更新日期:2013-08-01 00:00:00

  • GABAA receptor subtype selectivity of the proconvulsant rodenticide TETS.

    abstract::The rodenticide tetramethylenedisulfotetramine (TETS) is a potent convulsant (lethal dose in humans 7-10 mg) that is listed as a possible threat agent by the United States Department of Homeland Security. TETS has previously been studied in vivo for toxicity and in vitro in binding assays, with the latter demonstratin...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-017-2089-4

    authors: Pressly B,Nguyen HM,Wulff H

    更新日期:2018-02-01 00:00:00

  • Long-term simulation of lead concentrations in agricultural soils in relation to human adverse health effects.

    abstract::Lead (Pb) exposure of consumers and the environment has been reduced over the past decades. Despite all measures taken, immission of Pb onto agricultural soils still occurs, with fertilizer application, lead shot from hunting activities, and Pb from air deposition representing major sources. Little is known about the ...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-020-02762-x

    authors: Schupp T,Damm G,Foth H,Freyberger A,Gebel T,Gundert-Remy U,Hengstler JG,Mangerich A,Partosch F,Röhl C,Wollin KM

    更新日期:2020-07-01 00:00:00

  • A rapid gas-chromatographic method for the determination of drugs in clinical toxicology.

    abstract::A rapid gas-chromatographic method for the qualitative and quantitative measurement of various drugs in human plasma and other body fluids has been developed. The extraction procedure is done within 5 min, and gas-chromatographic measurement carried out on 2 diverse columns with detection by flame ionisation detectors...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00368231

    authors: Pentz R,Schütt A

    更新日期:1978-01-25 00:00:00

  • Infer the in vivo point of departure with ToxCast in vitro assay data using a robust learning approach.

    abstract::The development and application of high throughput in vitro assays is an important development for risk assessment in the twenty-first century. However, there are still significant challenges to incorporate in vitro assays into routine toxicity testing practices. In this paper, a robust learning approach was developed...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-018-2260-6

    authors: Wang D

    更新日期:2018-09-01 00:00:00

  • Dose and route dependency of metabolism and toxicity of chloroform in ethanol-treated rats.

    abstract::The effects of a single dose of ethanol on the metabolism and toxicity of chloroform administered to rats per os (p.o.), intraperitoneally (i.p.), or by inhalation (inh) at different doses were investigated. Rats that had been given either ethanol (2 g/kg) or vehicle (water) alone at 4 p.m. on the previous day were ch...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s002040050131

    authors: Wang PY,Kaneko T,Tsukada H,Sato A

    更新日期:1994-01-01 00:00:00

  • Birth weights of newborns and pregnancy outcomes of environmentally boron-exposed females in Turkey.

    abstract::Boric acid and sodium borates are currently classified as being toxic to reproduction under "Category 1B" with the hazard statement of "H360 FD" in the European CLP regulation. This has prompted studies on boron-mediated reprotoxic effects in male workers in boron mining areas and boric acid production plants. By cont...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-018-2238-4

    authors: Duydu Y,Başaran N,Üstündağ A,Aydın S,Yalçın CÖ,Anlar HG,Bacanlı M,Aydos K,Atabekoğlu CS,Golka K,Ickstadt K,Schwerdtle T,Werner M,Meyer S,Bolt HM

    更新日期:2018-08-01 00:00:00

  • Ethylmorphine concentrations in human samples in an overdose case.

    abstract::Capillary gas chromatography coupled to mass spectrometry was employed to quantify ethylmorphine in biological fluids and tissues in a death attributed to oral ethylmorphine ingestion. The femoral blood concentration of the drug was 488 ng/ml. Hair analysis revealed the individual's drug abuse pattern, particularly th...

    journal_title:Archives of toxicology

    pub_type: 信件

    doi:10.1007/s002040050057

    authors: Kintz P,Jamey C,Mangin P

    更新日期:1994-01-01 00:00:00

  • Determination of lorazepam in plasma by electron capture GLC.

    abstract::A method is described for the determination of lorazepam plasma levels involving extraction from the sample and analysis of the intact lorazepam by electron capture gas-liquid chromatography. Using mass spectrometry it is demonstrated, that lorazepam shows a thermal rearrangement under gas chromatographic conditions. ...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00293571

    authors: de Groot G,Maes RA,Lemmens HH

    更新日期:1976-06-08 00:00:00

  • Regulation of uterine AHR battery gene expression by 17β-Estradiol is predominantly mediated by estrogen receptor α.

    abstract::The aryl hydrocarbon receptor (AHR) is known to mediate the cellular response to numerous xenobiotics including dioxin. Surprisingly AHR knockout mice provide evidence for the involvement of the AHR signalling cascade in estrogen regulated physiological functions of the female reproductive system. Several studies alre...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-012-0870-y

    authors: Rataj F,Möller FJ,Jähne M,Zierau O,Diel P,Vollmer G,Kretzschmar G

    更新日期:2012-10-01 00:00:00

  • Investigation on the metabolic degradation of the side chain of furazolidone.

    abstract::The investigation was aimed at providing insight into the side chain metabolism of furazolidone in mice. The agents used in the experiments were furazolidone, 3-amino-2-oxazolidinone, oxazolidinone, nitrofurantoin, 3-aminohydantoin and hydantoin, administered intraperitoneally at five equimolar doses ranging from 0.17...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00661377

    authors: Hunder G,Schmid A,Mayring L

    更新日期:1987-12-01 00:00:00

  • Expressions of N-methyl-D-aspartate receptors NR2A and NR2B subunit proteins in normal and sulfite-oxidase deficient rat's hippocampus: effect of exogenous sulfite ingestion.

    abstract::Sulfites whether ingested or produced through the sulfur-containing amino acids metabolism of the animal are very active molecules and can cause cellular toxicity. Sulfite oxidase (SOX), a heme- and molybdenum containing mitochondrial enzyme, prevents mammalian cells from adverse effects of sulfite toxicity by metabol...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-006-0125-x

    authors: Oztürk OH,Küçükatay V,Yönden Z,Ağar A,Bağci H,Delibaş N

    更新日期:2006-10-01 00:00:00

  • The pyrrolizidine alkaloid senecionine induces CYP-dependent destruction of sinusoidal endothelial cells and cholestasis in mice.

    abstract::Pyrrolizidine alkaloids (PAs) are widely occurring phytotoxins which can induce severe liver damage in humans and other mammalian species by mechanisms that are not fully understood. Therefore, we investigated the development of PA hepatotoxicity in vivo, using an acutely toxic dose of the PA senecionine in mice, in c...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-019-02582-8

    authors: Hessel-Pras S,Braeuning A,Guenther G,Adawy A,Enge AM,Ebmeyer J,Henderson CJ,Hengstler JG,Lampen A,Reif R

    更新日期:2020-01-01 00:00:00

  • Human liver debrisoquine 4-hydroxylase: test for specificity toward various monooxygenase substrates and model of the active site.

    abstract::Polyclonal antibodies raised toward a debrisoquine 4-hydroxylating cytochrome P-450 species purified from rat liver (P-450UT-A) were used to determine which monooxygenase reactions are linked to debrisoquine hydroxylation in human liver. Anti P-450UT-A did not inhibit the oxidation of dimethylnitrosamine, morphine, di...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00296955

    authors: Wolff T,Distlerath LM,Worthington MT,Guengerich FP

    更新日期:1987-01-01 00:00:00

  • Nuclear aberrations in hair follicle cells of patients receiving cyclophosphamide. A possible in vivo assay for human exposure to genotoxic agents.

    abstract::The toxic effect of cyclophosphamide on the proliferative cell population of hair follicles plucked from the human scalp was examined by the in vivo nuclear aberration assay. Patients participating in an independent clinical trial received oral low dose cyclophosphamide, intravenous high dose cyclophosphamide or oral ...

    journal_title:Archives of toxicology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/BF01974396

    authors: Goldberg MT,Tackaberry LE,Hardy MH,Noseworthy JH

    更新日期:1990-01-01 00:00:00

  • Induction of peroxisomal beta-oxidation and P-450 4A-dependent activities by pivalic and trichloroacetic acid in rat liver and kidney.

    abstract::The influence of pivalic acid (PIV), a compound often used to make pro-drugs, and of the structurally related trichloroacetic acid (TCA), on several hepatic and renal enzymes was investigated in Sprague-Dawley rats, following a 4-day treatment period. The PIV and TCA treatments resulted in a similar and selective indu...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s002040050253

    authors: Zanelli U,Puccini P,Acerbi D,Ventura P,Gervasi PG

    更新日期:1996-01-01 00:00:00

  • Occupational exposure to some synthetic pyrethroids (permethrin and fenvalerate).

    abstract::In a two-step study on exposure control method for occupational handling of permethrin was developed. Air sampling on a filter can be used in case of exposure to permethrin in powder form. The detection limit is 0.001 mg/m3. If biological sampling is used, the acid metabolite moiety in the urine must be monitored. How...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00569234

    authors: Kolmodin-Hedman B,Swensson A,Akerblom M

    更新日期:1982-05-01 00:00:00

  • Involvement of the extracellular signal-regulated protein kinase pathway in phosphorylation of p53 protein and exerting cytotoxicity in human neuroblastoma cells (SH-SY5Y) exposed to acrylamide.

    abstract::Using human neuroblastoma SH-SY5Y cells, effects of acrylamide on p53 protein and intracellular signal transducting pathways were examined. Acrylamide increased p53, phosphorylated p53, and p53-associated protein murine double minute 2 (MDM2). The phosphorylation of p53 was specific for the Ser15 site. Among mitogen-a...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-005-0022-8

    authors: Okuno T,Matsuoka M,Sumizawa T,Igisu H

    更新日期:2006-03-01 00:00:00

  • Transfer and accumulation of cadmium, and the level of metallothionein in perfused human placentae.

    abstract::The purpose of the present study was to investigate the effect of perfusion with a medium containing 12 or 24 micrograms Cadmium (as CdCl2) per ml on this metal's accumulation, transfer rate and metallothionein (MT) level. The experiments were performed with an isolated lobule of a dually-perfused human term placenta....

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF01968966

    authors: Boadi WY,Yannai S,Urbach J,Brandes JM,Summer KH

    更新日期:1991-01-01 00:00:00

  • Cytotoxic effects of 3,4-methylenedioxy-N-alkylamphetamines, MDMA and its analogues, on isolated rat hepatocytes.

    abstract::The amphetamine-derived designer drugs have been illegally used worldwide as recreational drugs, some of which are known to be hepatotoxic in humans. To compare their cytotoxic effects, 3,4-methylenedioxy-N-methamphetamine (MDMA) and its related analogues, N-methyl-1-(3,4-methylenedioxyphenyl)-2-butanamine (MBDB), 3,4...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-008-0323-9

    authors: Nakagawa Y,Suzuki T,Tayama S,Ishii H,Ogata A

    更新日期:2009-01-01 00:00:00

  • Maintenance of drug metabolism and transport functions in human precision-cut liver slices during prolonged incubation for 5 days.

    abstract::Human precision-cut liver slices (hPCLS) are a valuable ex vivo model that can be used in acute toxicity studies. However, a rapid decline in metabolic enzyme activity limits their use in studies that require a prolonged xenobiotic exposure. The aim of the study was to extend the viability and function of hPCLS to 5 d...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-016-1865-x

    authors: Starokozhko V,Vatakuti S,Schievink B,Merema MT,Asplund A,Synnergren J,Aspegren A,Groothuis GMM

    更新日期:2017-05-01 00:00:00

  • Tissue distribution metabolism and excretion of 2,2',4,4',5-pentachlorodiphenyl ether in the rat.

    abstract::The tissue distribution, metabolism and excretion of 14C-2,2',4,4',5-pentachlorodiphenyl ether (PCDE) were studied in the rat. Radioactivity was distributed in all tissues examined, with the highest concentrations being found in the fat followed by the skin, liver, kidney and muscle. Most of the radioactivity found in...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00332484

    authors: Komsta E,Chu I,Villeneuve DC,Benoit FM,Murdoch D

    更新日期:1988-01-01 00:00:00

  • Are findings with isolated rat livers after short calcium free perfusion relevant for isolated cells?

    abstract::In the isolated liver transient perfusion without calcium results in cholestasis which was characterized by an increased efflux rate across the sinusoidal membrane and inhibition of the concentrative transport of bromosulfophthalein to the canalicular side of the cell. Cholestasis could not be reversed within the usua...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/BF00303180

    authors: Höke H,Krell H,Pfaff E

    更新日期:1980-03-01 00:00:00

  • No parallel relationship between nitric oxide production and wet dog shakes susceptible to nitric oxide synthase inhibitors following systemic administration of paraquat in rats.

    abstract::Shaking behavior, so-called wet dog shakes (WDS), in rats is characteristic behavior indicating morphine abstinence in morphine-dependence and central excitation in relation to seizures elicited by chemicals or electrical stimulation. We have found that paraquat (PQ), a nonselective herbicide, administered systemicall...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s002040000196

    authors: Hara S,Mukai T,Kurosaki K,Kuriiwa F,Yanase T,Kano S,Endo T

    更新日期:2001-02-01 00:00:00

  • Induction of Dectin-1 and asthma-associated signal transduction pathways in RAW 264.7 cells by a triple-helical (1, 3)-β-D glucan, curdlan.

    abstract::People living in damp buildings are typically exposed to spore and mycelial fragments of the fungi that grow on damp building materials. There is experimental evidence that this exposure to triple-helical (1, 3)-β-D glucan and low molecular weight toxins may be associated with non-atopic asthma observed in damp and mo...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-013-1042-4

    authors: Rand TG,Robbins C,Rajaraman D,Sun M,Miller JD

    更新日期:2013-10-01 00:00:00

  • The influence of chronic fluorosis on mitochondrial dynamics morphology and distribution in cortical neurons of the rat brain.

    abstract::The present study was designed to evaluate the effects of chronic fluorosis on the dynamics (including fusion and fission proteins), fragmentation, and distribution of mitochondria in the cortical neurons of the rat brain in an attempt to elucidate molecular mechanisms underlying the brain damage associated with exces...

    journal_title:Archives of toxicology

    pub_type: 杂志文章

    doi:10.1007/s00204-012-0942-z

    authors: Lou DD,Guan ZZ,Liu YJ,Liu YF,Zhang KL,Pan JG,Pei JJ

    更新日期:2013-03-01 00:00:00