Metabolic profiles for different species (rat, human, mouse, rabbit) did not have any significant differences in metabolites, but the degree of absorption, especially in cutaneous applications, varied from species to species.
Characterization of metabolites of lauramine oxide resulted in the positive identification of only one metabolite, N-dimethyl-4-aminobutyric acid N-oxide. Several pathways exist for metabolism of lauramine oxide: omega,beta-oxidation of alkyl chains (the most common pathway for surfactant metabolism), hydroxylation of alkyl chains, and reduction of the amine oxide group.
Urinary metabolites in rats, rabbits and humans suggested metabolism via omega, beta-oxidation of the aliphatic chain, amine oxide reduction and aliphatic, mid-chain hydroxylation. N,N-dimethyl-4-aminobutyric acid and its N-oxide accounted for 28, 28 and 23% in man, rats and rabbits, respectively.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
Dermatotoxin - 皮肤烧伤。
Dermatotoxin - Skin burns.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
大鼠LC50 = 5.3克/毫升/4小时（0.3%月桂胺氧化物气溶胶）
LC50 (rat) = 5.3 g/mL/4h (aerosol of 0.3% lauramine oxide;
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
/LABORATORY ANIMALS: Acute Exposure/ The ocular irritation potential of formulations containing 0.3% active lauramine oxide was evaluated by instilling 10 uL into the conjunctival sac of New Zealand White rabbits. The eyes of some rabbits were rinsed with distilled water. Irritation was scored according to the method of Draize (maximum possible score: 110). Slight irritation of the conjunctivae was observed in all unrinsed eyes and in two of three rinsed eyes at the 24-hr grading period. The maximum average score was 2.0 for the animals with unrinsed eyes, and 1.3 for those whose eyes were rinsed. All eyes were clear after 48 hr.
/LABORATORY ANIMALS: Acute Exposure/ The primary dermal irritation potential of three formulations, each containing 30% lauramine oxide, was evaluated using New Zealand white rabbits. Three male and three female rabbits had 0.5 mL of each formulation applied under occlusive patches to separate sites on their clipped backs for 24 hr. The sites were rinsed after patch removal and were scored for erythema, eschar, and edema at the time of removal and 48 hr later. The primary dermal indices (maximum possible score: 8) were 7.0, 7.2, and 7.6. Moderate to severe erythema and edema, two cases of necrosis, and one case of necrosis and fissuring with bleeding were observed at the 24-hr grading period. At the 72-hr reading, ... severe erythema and edema, eschar, fissuring with bleeding, and necrosis and/or thickened skin /did occur/.
/LABORATORY ANIMALS: Acute Exposure/ Liquid droplet aerosol /formulation containing 0.3% active lauramine oxide/ at concentrations of 0.2, 1.0, and 5.2 mg/L were tested on three groups of four male Swiss-Webster mice. Only the heads of the mice were exposed to the aerosol. The average respiratory rate was monitored using plethysmography 5 min before, 10 min during, and 10 min after each exposure, and the percentage change in respiratory rate was calculated. A decrease in respiratory rate was considered a response to upper airway irritation. A transient decrease was observed in the respiratory rate of the 1.0 mg/L exposed group, but this was not considered significant because no signs of irritation were seen at greater exposure concentrations. The groups treated with 1.0 mg/L and 5.2 mg/L had a 6% decrease in their average respiratory rates. However, these decreases were not attributed to upper airway irritation because the respiratory rates were even lower during the postexposure recovery period. No decrease in respiratory rate was observed in the 0.2 mg/L exposed mice.
(1-Dodecyl-14C)lauramine oxide (10 mg with 100 uCi of 14C) was applied to the skin of two humans to study cutaneous absorption and metabolism of lauramine oxide. Ninety-two percent of the applied radioactivity was recovered from the skin of the test subjects 8 hr after dosing, and 0.1 and 0.23% of the radioactivity was recovered from the excretion products of the test subjects. The stratum corneum contained <0.2% of the applied dose.
Oral administration of a solution containing 50 mg (1-dodecyl-14C)lauramine oxide (100 uCi of 14C) to two humans resulted in excretion patterns of radioactivity similar to that of the other species studied. Fifty percent and 37% of the radioactivity was found in the urine within 24 hr of dosing, and expired 14C02 contained between 18 and 22% of the radioactivity administered.
Four Sprague-Dawley rats were given intraperitoneal injections of 22 mg (methyl-14C)lauramine oxide kg (specific activity 1.3 mCi/g). Sixty-seven percent of the total radioactivity was eliminated in the urine, 8% was expired as I4CO2, and 6% was eliminated in the feces within 24 hr. The distribution of radioactivity was essentially the same as that seen in rats given oral doses of lauramine oxide. The conclusion was that "... microbial metabolism by gastrointestinal flora does not play a major role in the absorption and excretion of [lauramine oxide] in rats."
Aqueous (methyl-14C)lauramine oxide (10 mg containing 1.3 mCi/g) was applied to the skin of four Sprague-Dawley rats to test metabolism and absorption of the compound. Over 72 hr, 14.2% of the total radioactivity was found in the urine, 2.5% in the CO2, and 1.8% in the feces. Radioactivity was detected in the liver, kidneys, testes, blood, and expired CO2.
开发替代的良性反应条件以进行多组分反应是提高有机合成可持续性的一种有趣且理想的策略。在本文中，我们报道了一种新版本的 A 3 -偶联 MCR，用于在酸性 DES 作为反应介质、介电加热和四氮杂大环存在下，以醛、炔烃和胺为原料制备不同取代的炔丙胺。银络合物作催化剂。就醛伙伴而言，反应范围很广。富电子苯乙炔是更具反应性的炔烃伙伴，而胺的性质是更严重的限制，因为仅允许使用仲环状胺。
[EN] 3-[(HYDRAZONO)METHYL]-N-(TETRAZOL-5-YL)-BENZAMIDE AND 3-[(HYDRAZONO)METHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE DERIVATIVES AS HERBICIDES<br/>[FR] DÉRIVÉS DE 3-[(HYDRAZONO))MÉTHYL]-N-(TÉTRAZOL-5-YL)-BENZAMIDE ET DE 3-[(HYDRAZONO)MÉTHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE UTILISÉS EN TANT QU'HERBICIDES
申请人：SYNGENTA CROP PROTECTION AG
公开号：WO2021013969A1
公开（公告）日：2021-01-28
The present invention related to compounds of Formula (I): or an agronomically acceptable salt thereof, wherein Q, R2, R3, R4, R5 and R6 are as described herein. The invention further relates to compositions comprising said compounds, to methods of controlling weeds using said compositions, and to the use of compounds of Formula (I) as a herbicide.
[EN] INSECTICIDAL TRIAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZINONE INSECTICIDES
申请人：SYNGENTA PARTICIPATIONS AG
公开号：WO2013079350A1
公开（公告）日：2013-06-06
Compounds of the formula (I) or (I'), wherein the substituents are as defined in claim 1, are useful as pesticides.
式(I)或(I')的化合物，其中取代基如权利要求1所定义的那样，可用作杀虫剂。
[EN] A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS<br/>[FR] CONJUGUÉ D'UN AGENT CYTOTOXIQUE À UNE MOLÉCULE DE LIAISON CELLULAIRE AVEC DES LIEURS RAMIFIÉS
申请人：HANGZHOU DAC BIOTECH CO LTD
公开号：WO2020257998A1
公开（公告）日：2020-12-30
Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.
[EN] CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES<br/>[FR] DÉRIVÉ DE DIMÈRE DE PYRROLOBENZODIAZÉPINE RÉTICULÉ (PBD) ET SES CONJUGUÉS
申请人：HANGZHOU DAC BIOTECH CO LTD
公开号：WO2020006722A1
公开（公告）日：2020-01-09
A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.
Imaging compounds, methods of making imaging compounds, methods of imaging, therapeutic compounds, methods of making therapeutic compounds, and methods of therapy
申请人：Chen Xiaoyuan
公开号：US20080267882A1
公开（公告）日：2008-10-30
Embodiments of the present disclosure provide for RGD compounds that include a multimeric RGD (arginine-glycine-aspartic acid (Arg-Gly-Asp)) peptide, methods of making the RGD compound, pharmaceutical compositions including RGD compound, methods of using the RGD compositions or the pharmaceutical compositions including RGD compositions, methods of diagnosing and/or targeting angiogenesis related disease and related biological events, kits for diagnosing and/or targeting angiogenesis related disease and related biological events, and the like. In addition, the present disclosure includes compositions used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging) of the RGD compounds in vivo.
