... In feces intact (14)C-cymoxanil (< 1%) and IN W3595 was detected, but the majority of radioactivity was (14)C-glycine (about 9 - 13%). Based on the data, the metabolic pathway involves hydrolysis of cymoxanil to IN W3595, which is then degraded to glycine, which in turn is incorporated into natural constituents or further metabolized.
... IN-U3204 (1-ethyl-5,6-di-2,4(1H,3H) pyridinedione) was detected in pooled 0-48 hr urine samples, both sexes, from animals treated with 120 mg/kg DPX-3217 and in pooled 0-24 hr samples, both sexes, from animals treated with 2.5 mg/kg in an ongoing low dose biliary fistula study. The latter group was included to ensure that the presence of IN-U3204 was not an artifact of storage; IN-U3204 was detected in both groups, though at apparently low levels.
/2-(14)C-DPX-T3217/ was administered /to rats/ in corn oil to/ single dose groups: 2.5 & 120 mg/kg, 0.5 & 2 mL/animal (~10 & ~20 uCi/animal, groups D & E, respectively) and a multiple dose group: daily administration at 2.5 mg/kg for 14 days followed by labeled dose at 2.5 mg/kg (group F). /In a/ 5/sex/dose regimen, the primary metabolites detected by HPLC and TLC in excreta were IN-W3595 (2-cyano-2-methoxyimino acetic acid) and polar components (glycine and other amino acid conjugates); In group D males, 24 hr: 58% of /administered dose (AD)/ in urine (8.6% as IN-W3595, 46.5% as polars), 21.9% in feces (14% extractable, <1% IN-W3595, 13.1% polars). In /group D/ females, 64.2% of AD /appeared/ in urine (16.1% IN-W3595, 45.2% polars), 16.3% in feces (10.1% extractable, <1% IN-W3595, 8.7% polars). In group E males, 70.3% of AD /appeared/ in urine (26.3% IN-W3595, 40.3% polars), 16.1% in feces (11.3% extractable, <1% IN-W3595, 8.6% polars). /In group E/ females, 73% of AD in urine (33% IN-W3595, 36.7% polars), 17.1% in feces (11.5% extractable, <1% IN-W3595, 8.5% polars). In group F males, 66.2% of AD /appeared/ in urine (6.5% IN-W3595, 55% polars), 14.5% in feces (9% extractable, <1% IN-W3595, 8.9% polars). In group F females, 63.1% of AD /appeared/ in urine (11.1% IN-W3595, 46.6% polars), 19.4% in feces (12.3% extractable, <1% IN-W3595, 12.2% polars). /IN-W3595 metabolite/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：不太可能对人类致癌
Cancer Classification: Not Likely to be Carcinogenic to Humans
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
皮肤致敏剂 - 一种可以诱导皮肤产生过敏反应的制剂。
Skin Sensitizer - An agent that can induce an allergic reaction in the skin.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
LCLo（大鼠）= 4,980 毫克/立方米/4小时
LCLo (rat) = 4,980 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/
Cymoxanil is rapidly absorbed and maximum concentrations in the blood and plasma is reached within 4 hours after dosing. Rapid and almost complete elimination of the administered radioactive dose was observed in urine and feces within 48 hours. Excretion is primarily by urine (64 - 75%), fecal (16 - 24%) and expired air (< 5%) of the administered dose. There is no significant difference in residue profiles or elimination rates between sexes, dose levels, or single or multiple dosing. No evidence of bioaccumulation was detected. DPX-T3217 is metabolized extensively and only trace level of the administered (14)C-cymoxanil was detected in the urine and feces. ...
Five SD rats/sex with cannulated bile ducts were dosed orally with 2.5 mg/kg of (14)C-Cymoxanil (radiochemical purity = 98%; 14.09 uCi/mg) as a corn oil suspension. Urine, feces, and bile were collected over a 48 h period, after which the animals were terminated and whole blood, liver, kidneys, and residual carcass were collected for measurement of radiolabel. ...More than 85% of the test compound was eliminated in urine ( approximately 65%), feces (approximately 14%), and bile (approximately 7%) within 48 hr in both sexes, with most elimination occurring with the first 24 hr; polar amino acid conjugates comprised the major class of metabolites found in both urine (approximately 45-50%) and bile (approximately 4-6%); Metabolite A (unknown) and IN-W3595 /(2-cyano-2-methoxyimino acetic acid)/ were found at much lower concentrations (< 10%) in urine. IN-W3595 was found at higher concentrations in the urine of females (7.7%) as compared to males (2.8%); Metabolite A was not found in bile.
/To study the absorption, distribution, metabolism, and excretion of 2-(14)C-DPX-T3217 in rats, doses of/ 2.5 & 120 mg/kg in corn oil /at/ 0.5 & 2 mL/animal, /were administered. Radioactivity amounted to/ ~10 & ~20 uCi/animal, respectively. /High dose/ set by expectation of slight toxicity. /With/ single gavage administration: 3/sex/dose - blood pharmacokinetics, 5/sex/dose - elimination/distribution, 8/sex/dose - tissue distribution; multiple administration (cold dosing at 2.5 mg/kg for 14 days followed by labeled dose): 5/sex; no significant differences between groups in blood/plasma and tissue residue profiles. Max. blood concentrations were attained by 4 hr; with the possible exception of a somewhat decreased relative fecal excretion at the high dose (both sexes) and at the multiple low dose (males only). No significant differences in excretion time or route were seen when comparing sexes, doses, or single vs. multiple dosing regimens. Including all dose groups, 57-65% of the administered dose (AD) recovered in urine & 5-17% in feces by 24 hr, 63-75% in urine & 16-24% in feces by 96 hr; at 96 hr <1% of AD remained in tissues (highest levels found in kidney, liver, & skin).
(14)C-Cymoxanil was applied to either the root system or to the foliage of tomato plants and its uptake, translocation and degradation was followed using autoradiography, combustion and thin-layer chromatographic analyses of water or methanolic extracts. Cymoxanil was taken up by the root system within 1 hr and translocated to cotyledons, stem and leaves within 16 hr. The compound was degraded, mostly to glycine, within 16-44 h, in the root and all parts of the shoot. When applied to the surface of leaf 2 of five-leaf plants, enhanced uptake, translocation and degradation (mainly to glycine) of (14)C-cymoxanil was observed in plants treated with a mixture of oxadixyl and (14)C-cymoxanil, compared with plants treated with (14)C-cymoxanil alone. Root application data confirm that cymoxanil is a systemic compound with a short persistence in tomato plants. Foliage application data suggest that the well-documented synergistic interaction between cymoxanil, oxadixyl and mancozeb in controlling plant diseases caused by Peronosporales does not result from a delayed degradation of cymoxanil in the presence of the other fungicides; the mechanism of synergism has not yet been elucidated.
腈类化合物在医药、农用化学品、染料和功能材料等不同领域的应用激增，需要开发快速有效的检测和识别方法。在这项研究中，我们引入了一种采用新型19 F 标记探针的化学传感策略，有助于快速、准确地分析多种含腈分析物。该方法利用19 F 标记探针与分析物之间的可逆相互作用来产生类似色谱图的输出，确保精确识别复杂基质中的各种药物和农药。此外，该动态系统提供了一个多功能平台来研究空间19 F- 19 F 相互作用，展示了其在机械研究中未来应用的潜力。
The metabolism of cymoxanil [1-(2-cyano-2-methoxyiminoacetyl)-3-ethyl urea] by a very sensitive strain of Botrytis cinerea toward this fungicide was studied by using [2-(14)C]-cymoxanil. Labeled cymoxanil was added either in a culture of this strain or in its enzymatic extract. The main metabolites, detected in biological samples, were isolated and identified by mass and NMR spectrometry. Their identification allowed us to show that this strain quickly metabolized cymoxanil according to at least three enzymatic pathways: (i) cyclization leading, after hydrolysis, to ethyl parabanic acid, (ii) reduction giving demethoxylated cymoxanil, and (iii) hydrolysis and reduction followed by acetylation leading to N-acetylcyanoglycine. In a cell-free extract of the same strain, only the first and the second enzymatic reactions, quoted above, occurred. Biological tests showed that, among all the metabolites, only N-acetylcyanoglycine is fungitoxic toward this sensitive strain.
The surge in applications of nitrile compounds across diverse fields, such as pharmaceuticals, agrochemicals, dyes, and functional materials, necessitates the development of rapid and efficient detection and identificationmethods. In this study, we introduce a chemosensing strategy employing a novel 19F-labeled probe, facilitating swift and accurate analysis of a broad spectrum of nitrile-containing
腈类化合物在医药、农用化学品、染料和功能材料等不同领域的应用激增，需要开发快速有效的检测和识别方法。在这项研究中，我们引入了一种采用新型19 F 标记探针的化学传感策略，有助于快速、准确地分析多种含腈分析物。该方法利用19 F 标记探针与分析物之间的可逆相互作用来产生类似色谱图的输出，确保精确识别复杂基质中的各种药物和农药。此外，该动态系统提供了一个多功能平台来研究空间19 F- 19 F 相互作用，展示了其在机械研究中未来应用的潜力。
