CD Rats, /male and female,/ were administered single oral doses of dimethylhydantoin-14C (DMH-14C) at either 100 (high dose) or 20 mg/kg (low dose). ... The parent DMH-14C was the only major radioactive component found in urine by thin layer chromatographic analysis. One minor metabolite was detected, which amounted to 2.5% of the urinary 14C. ...
A case of allergic contact dermititis secondary to photographic print coating liquid is described ... . Patch test reactions to the mixture were positive, but negative to the individual components which included dimethylhydantoin formaldehyde resin, the logical allergen. ... In this patient, the combination of components was necessary to yield a sensitivity reaction. ... Dermatitis secondary to this product has not been previously reported.
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/
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/
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/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
人类毒性摘录
中枢神经系统抑制剂
/SIGNS AND SYMPTOMS/ Central nervous system depressant
CD Rats, /male and female,/ were administered single oral doses of dimethylhydantoin-14C (DMH-14C) at either 100 (high dose) or 20 mg/kg (low dose). The disposition of the 14C was followed for a seven-day period. ... Urine and feces were collected and measured for the amount of 14C at the following periods: 0 - 8 hours, 8 - 16 hours, 15 - 24 hours, 24 - 32 hours, 32 - 48 hours, then 24 hour collections on Study Days 2 through 5. All animals were killed on Study Day 6. The following tissues were removed and immediately frozen: heart, liver, kidneys, spleen, abdominal fat, right leg muscle, leg bone, gonads and brain tissue. These tissues were measured for amount of 14C. The interior of the cage was washed with methanol and 14C was measured in the wash liquid. ... The average recovery of 14C from the rats was 95%. The compound was absorbed rapidly and was eliminated primarily in the urine with only minor metabolic conversion. ... The average amount eliminated in the urine was 91% of the dose. The elimination also was rapid, as 88% was eliminated in the first 24 hours after dosing. ... In the case of rats receiving the high dose, low levels of 14C were detected in kidney and bone tissues; however all measurements were not significant. ...
Development of New Hydroxamate Matrix Metalloproteinase Inhibitors Derived from Functionalized 4-Aminoprolines
作者：Michael G. Natchus、Roger G. Bookland、Biswanath De、Neil G. Almstead、Stanislaw Pikul、Michael J. Janusz、Sandra A. Heitmeyer、Erin B. Hookfin、Lily C. Hsieh、Martin E. Dowty、Charles R. Dietsch、Vikram S. Patel、Susan M. Garver、Fei Gu、Matthew E. Pokross、Glen E. Mieling、Timothy R. Baker、David J. Foltz、Sean X. Peng、David M. Bornes、Michael J. Strojnowski、Yetunde O. Taiwo
DOI：10.1021/jm000246e
日期：2000.12.1
activity with sub-nanomolar potency for some enzymes. Modifications of the P1' portion of the molecule played a key role in affecting both potency and selectivity within the MMP family. Longer-chain aliphatic substituents in this region of the molecule tended to increase potency for MMP-3 and decrease potency for MMP-1, as exemplified by compounds 48-50, while aromatic substituents, as in compound 52, generated
An environmentally friendly palladium‐catalyzed Suzuki–Miyauracoupling reaction of twisted amides with potassium aryl trifluoroborates has been developed, generating ketones under pure water phase, room temperature, and ligand‐free condition.
[EN] CORTISTATIN ANALOGUES AND SYNTHESES AND USES THEREOF<br/>[FR] ANALOGUES DE CORTISTATINE ET SYNTHÈSES ET UTILISATIONS ASSOCIÉES
申请人：HARVARD COLLEGE
公开号：WO2015100420A1
公开（公告）日：2015-07-02
Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the β-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1 -alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.
Catalytic Halogen Bond Activation in the Benzylic C–H Bond Iodination with Iodohydantoins
作者：Sascha H. Combe、Abolfazl Hosseini、Lijuan Song、Heike Hausmann、Peter R. Schreiner
DOI：10.1021/acs.orglett.7b03034
日期：2017.11.17
This letter presents the side-chain iodination of electron-deficient benzylic hydrocarbons at rt using N-hydroxyphthalimide (NHPI) as radical initiator and 1,3-diiodo-5,5-dimethylhydantoin and 3-iodo-1,5,5-trimethylhydantoin (3-ITMH) as iodine source. Addition of a carboxylic acid increased the reactivity due to complex formation with and activation of 3-ITMH by proton transfer and halogen bond formation
Reverse hydroxamate inhibitors of matrix metalloproteinases
申请人：Abbott Laboratories
公开号：US06294573B1
公开（公告）日：2001-09-25
Compounds having the formula
are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.
