Rabbit sera brought about removal of sulfur and hydrolysis to p-nitrophenol. ...After incubation of EPN with nadph2, oxygen and microsomes of rat, housefly, or rabbit liver, corresponding phenol was found in each case. Oxon analog was also produced. Some conversion of oxon to corresponding phenol was also observed.
.../Para-nitrophenol/ is formed either by way of esteratic cleavage of the /EPN/ oxon or directly from .../EPN/ by mono-oxygenase-catalyzed dearylation prompted by initial oxidative attack at p=s.
Metabolism of single 1 mg (2.7 uci/kg) oral dose of (14)C EPN in 1 wk old chicks produced o-ethyl phenylphosphonic acid, phenylphosphonic acid, and o-ethyl phenylphosphonothioic acid.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
A4；不能归类为人类致癌物。
A4; Not classifiable as a human carcinogen.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
暴露途径
该物质可以通过吸入其气溶胶、通过皮肤接触以及摄入进入人体。
The substance can be absorbed into the body by inhalation of its aerosol, through the skin and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
EPN is readily absorbed following either oral or dermal exposure. In rats, following a single oral dose of 1.5 mg/kg EPN, about 61-68% of the dose was excreted in urine and 7-21% of the dose was excreted in the feces. Metabolism was essentially complete because urinary excretion of metabolites totaled 60-68% of the total dose, the corresponding fecal values were 6.7-17.2%. ...In rats given 0.72 or 0.072 mg/kg EPN three times at 24 hr intervals, 14 and 26% of the dose was excreted as p-nitrophenol in urine. EPN was not detectable in blood at any time after the final dose but was detectable in adipose tissue (0.06 ppm) only on day 3.
Radioactivity of single dermal dose, 20.0 mg/kg of (14)C-EPN admin to adult male cats disappeared exponentially at rate constant of 0.46/day, corresponding to half-life of 1.5 days. Most of radioactivity was excreted in urine (29.9%); only 3.2% in feces. None was detected in expired CO2. Only traces of EPN were detected in urine and feces. EPN was major substance identified 0.5 day after admin in brain, spinal cord, sciatic nerve, adipose tissue, plasma, muscle, liver and kidney. Most radioactivity in liver and kidney after 4 days was identified as metabolites. Half-life of EPN elimination from plasma was 9.1 days. Relative residence of EPN relative to plasma was longest in sciatic nerve and shortest in kidney.
When a rat was preconditioned for 21 days on a diet that contained 450 ppm EPN, only traces of the dose remained in body tissues after 72 hr. Thus, EPN was practically completely metabolized and eliminated in rats. Two EPN conditioned hens that received 2.5 mg/kg EPN for 21 days and two unconditioned hens excreted 94-100% of a single oral, nonneurotoxic 4 mg/kg dose with in 72 hr of admin. No significant difference was apparent in the dose excreted from conditioned or unconditioned chickens. Small amounts of EPN remained in body tissues; only trace amounts were found in the brain and spinal cord. By contrast, a single oral neurotoxic dose of 50 mg/kg EPN was slowly metabolized and excreted by chickens. Only 65% of the dose was eliminated during the 72 hr test. Excreta extract contained the same five metabolites found in the rat. Thus, the 50 mg/kg dose may have exceeded the metabolic capacity of the liver to detoxify EPN.
In cats, EPN was readily absorbed when a single dose of 20 mg/kg was dermally applied as reflected by disappearance of EPN from the application site. Most of the absorbed dose was excreted in urine (29.9%); 3.2% was recovered in the feces. In cats given daily dermal doses of 0.5 mg/kg EPN for 10 days, 62% fo the total dose was given daily dermal doses of 0.5 mg/kg EPN for 10 days, 62% of the total dose was eliminated in the urine. Thus, the metabolism and toxicokinetics of EPN in the cat are intermediate between those in the rat and in the chicken. Similarly to the rat, EPN is excreted as polar metabolite, mostly in the urine. As int he chicken, however, EPN is persistent in cat tissues, especially in nervous tissues. The finding that the cat is ten times less sensitive than the chicken to subchronic dermal exposure to EPN may be explained by the relatively rapid metabolism and elimination of EPN in the cat.
...Elimination of the phosphorus-containing residue may be via the urine or feces. Some bound residues remain in exposed animals. Binding seems to be to proteins, principally, and the turnover appears to be related to the half-life of these proteins. There are limited data showing that incorporation of residues into DNA occurs only in trace amounts and not by direct alkylation, such as might be believed to be associated with genetic damage. /Organophosphorus Pesticides/
Oxidation of organophosphorus pesticides for the sensitive detection by a cholinesterase-based biosensor
摘要：
A potentiometric flow injection-type biosensor developed in our laboratory was used for the determination of organophosphorus pesticides (OPs). The principle of the biosensor is that the degree of inhibition of a sensor enzyme by an OP is dependent on the concentration of the pesticide. The sensor system consisted of a reactor with acetylcholinesterase (AChE) immobilized on a controlled pore glass and a detector with a tubular H+-selective membrane electrode. In order to examine the possibility of enhancing the sensitivity of the sensor by converting OPs to oxidized forms (stronger inhibitors), a comparison of the degree of enzyme inhibition by OPs at 10(-6) M before and after their oxidation was made. All of the ten pesticides tested exhibited greater inhibitory power toward the sensor enzyme following oxidation. All of the oxidized pesticides at 10(-6) M inhibited the sensor enzyme to a considerable degree, demonstrating the utility of the developed method for the class-specific determination of OPs. A calibration curve for diazinon, over the concentration range of 10(-11)-10(-4) M, was obtained. The lower detection limit was 2 x 10(-10) M. Treatment of the inhibited enzyme with pyridine-2-aldoxime restored the enzyme to near full activity, allowing repeated use of the sensor. (C) 2002 Published by Elsevier Science Ltd.
HYDRAZONYL GROUP-CONTAINING CONDENSED HETEROCYCLIC COMPOUND OR SALT THEREOF, AGRICULTURAL AND HORTICULTURAL INSECTICIDE COMPRISING THE COMPOUND, AND METHOD FOR USING THE INSECTICIDE
申请人：Nihon Nohyaku Co., Ltd.
公开号：US20190177319A1
公开（公告）日：2019-06-13
An object of the present invention is to develop and provide a novel agricultural and horticultural insecticide in view of the still immense damage caused by insect pests etc. and the emergence of insect pests resistant to existing insecticides in crop production in the fields of agriculture, horticulture and the like.
Provided is a hydrazonyl group-containing condensed heterocyclic compound or a salt thereof, preferably a condensed heterocyclic compound represented by the general formula (1):
wherein R
1
represents, for example, an alkyl group, R
2
represents, for example, a hydrogen atom, R
3
and R
4
each represent, for example, an alkyl group, a haloalkyl group or an acyl group, A
1
represents, for example, a nitrogen atom, A
2
represents, for example, N-Me or an oxygen atom, A
3
represents, for example, a carbon atom or a nitrogen atom, A
4
represents, for example, C—H, m represents, for example, 2, and n represents, for example, 1}, or a salt thereof; an agricultural and horticultural insecticide comprising the compound or a salt thereof as an active ingredient; and a method for using the insecticide.
PYRIDONE COMPOUNDS AND AGRICULTURAL AND HORTICULTURAL FUNGICIDES CONTAINING THE SAME AS ACTIVE INGREDIENTS
申请人：MITSUI CHEMICALS AGRO, INC.
公开号：US20200172486A1
公开（公告）日：2020-06-04
Provided are a pyridone compound represented by Formula (1):
wherein
R1 represents a C1-C6 alkyl group which may be substituted, etc.,
R2 represents a halogen atom, a cyano group, etc.,
R3 and R4 are independent to each other, and each represents a hydrogen atom, a C1-C6 alkyl group which may be substituted, etc., or in combination with the nitrogen atom to which they are bonded form a pyrrolidinyl group, a piperidinyl group, etc., which may be substituted,
Y represents a phenyl group which may be substituted, etc.,
X represents an oxygen atom or a sulfur atom,
and an agricultural and horticultural fungicide containing the same as an active ingredient.
[EN] TETRAZOLINONE COMPOUNDS AND ITS USE AS PEST CONTROL AGENTS<br/>[FR] COMPOSÉS TÉTRAZOLINONE ET LEUR UTILISATION EN TANT QU'AGENTS DE LUTTE CONTRE LES NUISIBLES
申请人：SUMITOMO CHEMICAL CO
公开号：WO2018097318A1
公开（公告）日：2018-05-31
The present invention provides a tetrazolinone represented by formula (I) and a pest control agent comprising the same, and their use thereof. Formula (I) [wherein, W1 represents an oxygen atom or a sulfur atom; W2 represents a hydrogen atom, or a C1-C6 chain hydrocarbon group; R15 and R16 represent a halogen atom and the like; u is 0, 1, 2 or 3; the combination of E, G, X1, Y1 and Z1 represents any one of the combinations of the following a and the like: a: a combination wherein E represents #-C(X1)(Y1)-O-N=C(Z1)-, #-C(X1)(Y1)-S-N=C(Z1)-, #-C(X1)(Y1)-O-N=C(Z1)-O-CH2-, #-C(X1)(Y1)-O-N=C(Z1)-S-CH2-, #-C(X1)(Y1)-S-N=C(Z1)-O-CH2-, #-C(X1)(Y1)-S-N=C(Z1)-S-CH2-, #-C(Z1)=N-N=C(Z2)-, #-C(X1)=C(Y1)-C(Z1)=N-O-CH2- or #-C(X1)=C(Y1)-C(Z1)=N-S-CH2-; G represents a C1-C6 chain hydrocarbon group, a (C1-C6 alkoxy)C1-C6 alkyl group, a (C1-C6 alkylthio)C1-C6 alkyl group the C1-C6 chain hydrocarbon group, the (C1-C6 alkoxy)C1-C6 alkyl group, and the (C1-C6 alkylthio)C1-C6 alkyl group may have one or more substituents selected from Group S} or R1-T1-, X1 and Y1, which are identical to or different from each other, independently represents substituents selected from Group T, and Z1 represents a substituent selected from Group V.]
OXIME GROUP-CONTAINING CONDENSED HETEROCYCLIC COMPOUND OR SALT THEREOF, AGRICULTURAL AND HORTICULTURAL INSECTICIDE COMPRISING THE COMPOUND, AND METHOD FOR USING THE INSECTICIDE
申请人：NIHON NOHYAKU CO., LTD.
公开号：US20210371424A1
公开（公告）日：2021-12-02
Provided are an oxime group-containing condensed heterocyclic compound or a salt thereof, preferably a condensed heterocyclic compound represented by general formula (1):
(wherein the symbols are defined in the specification); an agricultural and horticultural insecticide comprising the compound or a salt thereof as an active ingredient; and a method for using the insecticide.
A method of controlling plant diseases, especially fungi, using oxime carbamates and analogs thereof and novel compounds within the class.
Reason: Rule 8.1.i PCT.
