Rats receiving oral doses of C14-carboxyl or 2,3( 125-I),5(126-I)-triiodobenzoic acid excreted 72-75 % of the radioactivity in urine and 24-28% in feces during the 4 days following drug administration... . Thin-layer chromatograms of ether extracts of urine (50-80% of the radioactivity was extracted) revealed the presence of: 2,5-diiodobenzoic acid, as the free acid and a conjugate, accounting for 66% of the extractable radioactivity (39.6% of dose); unchanged TIBA, 9.5% (5.7% of dose); 2-hydroxy-3,5-diiodobenzoic acid, 2.3% (1.4% of dose); and 3,5-diiodobenzoic acid, 0.7% (0.4% of dose). Thin-layer chromatograms of feces extracts revealed a metabolic pattern similar io urine.
The whole body retention, excretion, distribution, thyroid uptake, and metabolism of 2(131I),3,5-triiodobenzoic acid (TIBA) were studied in goats and a cow. A single oral dose of TIBA exhibited a two-component whole body radioactivity retention curve and was excreted primarily in the urine. TIBA plus nine metabolites, four of which were identified, were found in the urine. The major metabolite was 2,5-diiodobenzoic acid (2,5-DIBA). Trace amounts of 2,3-diiodobenzoic acid (2,3-DIBA), orthoiodobenzoic acid (OIBA), and iodide ion were found. TIBA was metabolized by deiodination. Iodide ion was concentrated in the thyroid and excreted by way of milk and urine.
The metabolites of 2,3,5-triiodobenzoic acid in cow's milk resulting from acute administration of the compound (1.197 g) were determined using electron capture gas-chromatograph procedures. The parent compound plus seven suspected metabolites were detected; of these, four were identified, and one quantitated. The primary metabolite was 2-OHI-3,5-diiodobenzoic acid. Occurring in trace amounts were mono-iodobenzoic acids, 2-0H-5 iodobenzoic acid, and 3,5-diiodobenzoic acid. The maximum concentration of 2,3,5-triiodobenzoic acid in raw milk was found in the 30-hr milk sample at the 0.79 mg/kilogram level and of 2-OH-3,5-diiodobenzoic acid in the 42-hr milk at the 0.27 mg/kilogram level.
/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/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
解毒与急救
/SRP:/ 高级治疗：对于无意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛，考虑给予β激动剂，如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注D5W /SRP: "保持开放"，最低流量/。如果出现低血容量的迹象，使用0.9%生理盐水（NS）或乳酸林格氏液。对于伴有低血容量迹象的低血压，谨慎给予液体。注意液体过载的迹象……。使用地西泮或劳拉西泮治疗癫痫……。使用丙美卡因氢氯化物协助眼部冲洗……。 /Poisons A and B/
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
The placental transfer of 2, 3, 5-triiodobenzoic acid and/or metabolites was studied using 14C-labeled 2, 3, 5-triiodobenzoic acid. Placental transfer of 2, 3, 5-triiodobenzoic acid and/or metabolites occurred in both cold-stressed and control rats. The maternal blood of cold-stressed and control rats contained significantly higher concentrations of 2, 3, 5-triiodobenzoic acid and/or metabolites than the blood of respective fetal rats. However, cold stress did not significantly alter either placental transfer or the level of 2, 3, 5-triiodobenzoic acid and/or metabolites in the maternal and fetal tissue. Cold stress had no apparent effect upon the plasma level of either 2, 3, 5-triiodobenzoic acid, 2, 5-diiodobenzoic acid, or 3, 5-diiodobenzoic acid in maternal or fetal animals. While nonpregnant rats acclimated to cold stress, pregnant rats did not, indicating cold stress and pregnancy may act synergistically.
Rats receiving oral doses of C14-carboxyl or 2,3( 125-I),5(125-I)-triiodobenzoic acid excreted 72-75% of the radioactivity in urine and 24-28% in feces during the 4 days following drug administration. Peak levels of carbon-14 were observed in brain, thyroid, liver, lungs, heart, spleen, kidneys, and carcass 4 or 8 hr after dosing and rapidly decreased thereafter. Levels of iodine-125 were significantly higher than carbon-14 levels in the brain and thyroid. Iodine-125 in thyroid increased with time. ...
[EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
申请人：GILEAD APOLLO LLC
公开号：WO2017075056A1
公开（公告）日：2017-05-04
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
本发明提供了三唑化合物，可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及其组合物和使用方法。
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
申请人：Dow AgroSciences LLC
公开号：US20180279612A1
公开（公告）日：2018-10-04
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
[EN] MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO<br/>[FR] MOLÉCULES PRÉSENTANT UNE UTILITÉ EN TANT QUE PESTICIDE, ET LEURS INTERMÉDIAIRES, COMPOSITIONS ET PROCÉDÉS
申请人：DOW AGROSCIENCES LLC
公开号：WO2017040194A1
公开（公告）日：2017-03-09
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions aga inst such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula ("Formula One").
MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO
申请人：Dow AgroSciences LLC
公开号：US20170210723A1
公开（公告）日：2017-07-27
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, compositions containing such molecules, and processes of using such molecules and compositions against such pests. These molecules and compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
