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大鼠吸入2,3-[¹⁴C]二氯丙烯后的处置与代谢

Disposition and metabolism of 2,3-[14C]dichloropropene in rats after inhalation.

作者信息

Bond J A, Medinsky M A, Dutcher J S, Henderson R F, Cheng Y S, Mewhinney J A, Birnbaum L S

出版信息

Toxicol Appl Pharmacol. 1985 Mar 30;78(1):47-54. doi: 10.1016/0041-008x(85)90303-5.

Abstract

2,3-Dichloropropene (2,3-DCP) is a constituent of some commercially available preplant soil fumigants for the control of plant parasitic nematodes. Human exposure potential exists during manufacture of the chemicals or during bulk handling activities. The purpose of this investigation was to determine the disposition and metabolism of 2,3-[14C]DCP in rats after inhalation. Male Fischer-344 rats were exposed nose-only to a vapor concentration of 250 nmol 2,3-[14C]DCP/liter air (7.5 ppm; 25 degrees C, 620 Torr) for 6 hr. Blood samples were taken during exposure, and urine, feces, expired air, and tissues were collected for up to 65 hr after exposure. Urinary excretion was the major route of elimination of 14C (55% of estimated absorbed 2,3-DCP). Half-time for elimination of 14C in urine was 9.8 +/- 0.05 hr (means +/- SE). Half-time for elimination of 14C feces (17% of absorbed 2,3-DCP) was 12.9 +/- 0.14 hr (means +/- SE). Approximately 1 and 3% of the estimated absorbed 2,3-[14C]DCP were exhaled as either 2,3-[14C]DCP or 14CO2, respectively. Concentrations of 14C in blood increased during 240 min of exposure, after which no further increases in blood concentration of 14C were seen. 14C was widely distributed in tissues analyzed after a 6-hr exposure of rats to 2,3-[14C]DCP. Urinary bladder (150 nmol/g), nasal turbinates (125 nmol/g), kidneys (84 nmol/g), small intestine (61 nmol/g), and liver (35 nmol/g) were tissues with the highest concentrations of 14C immediately after exposure. Over 90% of the 14C in tissues analyzed was 2,3-DCP metabolites. Half-times for elimination of 14C from tissues examined ranged from 3 to 11 hr. The data from this study indicate that after inhalation 2,3-DCP is metabolized in tissues and readily excreted.

摘要

2,3 - 二氯丙烯(2,3 - DCP)是一些市售前种植土壤熏蒸剂的成分,用于防治植物寄生线虫。在化学品制造过程或散装处理活动中存在人类接触的可能性。本研究的目的是确定大鼠吸入2,3 - [¹⁴C]DCP后的处置和代谢情况。雄性Fischer - 344大鼠仅通过鼻腔暴露于浓度为250 nmol 2,3 - [¹⁴C]DCP/升空气(7.5 ppm;25℃,620 Torr)的蒸气中6小时。在暴露期间采集血样,并在暴露后长达65小时收集尿液、粪便、呼出气体和组织。尿排泄是¹⁴C消除的主要途径(占估计吸收的2,3 - DCP的55%)。尿中¹⁴C消除的半衰期为9.8±0.05小时(平均值±标准误)。粪便中¹⁴C消除的半衰期(占吸收的2,3 - DCP的17%)为12.9±0.14小时(平均值±标准误)。估计吸收的2,3 - [¹⁴C]DCP中分别约有1%和3%以2,3 - [¹⁴C]DCP或¹⁴CO₂的形式呼出。在大鼠暴露于2,3 - [¹⁴C]DCP 6小时的过程中血液中¹⁴C浓度升高,之后血液中¹⁴C浓度未见进一步升高。大鼠暴露于2,3 - [¹⁴C]DCP 6小时后,¹⁴C广泛分布于所分析的组织中。暴露后立即¹⁴C浓度最高的组织是膀胱(150 nmol/g)、鼻甲(125 nmol/g)、肾脏(84 nmol/g)、小肠(61 nmol/g)和肝脏(35 nmol/g)。所分析组织中超过90%的¹⁴C是2,3 - DCP代谢物。所检查组织中¹⁴C消除的半衰期为3至11小时。本研究的数据表明,吸入后2,3 - DCP在组织中代谢并易于排泄。

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