Cyanide is rapidly alsorbed through oral, inhalation, and dermal routes and distributed throughout the body. Cyanide is mainly metabolized into thiocyanate by either rhodanese or 3-mercaptopyruvate sulfur transferase. Cyanide metabolites are excreted in the urine. (L96)
Cyanide is an inhibitor of cytochrome c oxidase in the fourth complex of the electron transport chain (found in the membrane of the mitochondria of eukaryotic cells). It complexes with the ferric iron atom in this enzyme. The binding of cyanide to this cytochrome prevents transport of electrons from cytochrome c oxidase to oxygen. As a result, the electron transport chain is disrupted and the cell can no longer aerobically produce ATP for energy. Tissues that mainly depend on aerobic respiration, such as the central nervous system and the heart, are particularly affected. Cyanide is also known produce some of its toxic effects by binding to catalase, glutathione peroxidase, methemoglobin, hydroxocobalamin, phosphatase, tyrosinase, ascorbic acid oxidase, xanthine oxidase, succinic dehydrogenase, and Cu/Zn superoxide dismutase. Cyanide binds to the ferric ion of methemoglobin to form inactive cyanmethemoglobin. (L97)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌物分类
对人类不具有致癌性（未被国际癌症研究机构IARC列名）。
No indication of carcinogenicity to humans (not listed by IARC).
Exposure to high levels of cyanide for a short time harms the brain and heart and can even cause coma, seizures, apnea, cardiac arrest and death. Chronic inhalation of cyanide causes breathing difficulties, chest pain, vomiting, blood changes, headaches, and enlargement of the thyroid gland. Skin contact with cyanide salts can irritate and produce sores. (L96, L97)
Cyanide poisoning is identified by rapid, deep breathing and shortness of breath, general weakness, giddiness, headaches, vertigo, confusion, convulsions/seizures and eventually loss of consciousness. (L96, L97)
After oral administration of the anthelmintic, (14)C-bitoscanate to dogs, renal elimination ... and fall-off of blood concentrations ... of (14)C- were biphasic. Similar results were obtained in man except that urinary excretion was more delayed, and more (14)C- was excreted renally. Much of the (14)C- had been excreted within 5 days from both species, but excretion of the remainder was protracted. Thus after 3 weeks, the dog had excreted 80% in the feces, and 12% in the urine, and after 5 weeks, man had excreted respectively 55 and 28% by these routes; 3% still circulated in the blood. Fetuses contained 3% of the dose, 16 hr after admin of (14)C-bitoscanate to a pregnant dog. The data indicated that part of the (14)C binding to the tissues was only slowly excreted, possibly because (14)C-bitoscanate was irreversibly bound to biological macromolecules through its isothiocyanate groups. ... final rates of excretion of (14)C reflected rates of metabolism and excretion of the endogenous macromolecules to which bitoscanate was bound.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
Bitoscanate部分从胃肠吸收，然后慢慢排泄...
Bitoscanate is partly absorbed from the gastro-intestinal tract and slowly excreted ...
2-Thioxo-1,3-thiazepan-4-ones, a novel class of cyclic dithiourethanes with a 7-membered ring system
作者：Wolfgang Hanefeld、Harald Schütz
DOI：10.1002/jhet.5570360509
日期：1999.9
Reaction of isothiocyanates 1 with γ-thiobutyrolactone (2) in alkaline medium yielded 4-thiocarbamoylthiobutyric acids 3 after acidification, which could be cyclized to the 2-thioxo-1,3-thiazepan-4-ones 6. Additional reactions were observed with the formation of 6t from p-phenylenediisothiocyanate (1s) and with the formation of 6w from benzyl isothiocyanate (1t). 3-Acetylamino-γ-thiobutyrolactone (7)
The exocyclic functionalisation of bis(thiosemicarbazonate) complexes of zinc and copper: the synthesis of monomeric and dimeric species
作者：Martin Christlieb、Harriet S. R. Struthers、Paul D. Bonnitcha、Andrew R. Cowley、Jonathan R. Dilworth
DOI：10.1039/b705087a
日期：——
exocylic imine groups bearing a range of substituents. The zinc complexes can be quantitatively and rapidly transmetallated to the corresponding copper complexes and this route or direct reaction with the free ligand can be used to radiolabel the monomericspecies with (64)Cu. In vivo and in vitro studies of one of the (64)Cu imine complexes shows substantial hypoxic selectivity and high tumour uptake in
SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
申请人：BlinkBio, Inc.
公开号：US20170202970A1
公开（公告）日：2017-07-20
Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.
ANTHELMINTIC COMPOUNDS AND COMPOSITIONS AND METHOD OF USING THEREOF
申请人：Meng Charles Q.
公开号：US20140142114A1
公开（公告）日：2014-05-22
The present invention relates to novel anthelmintic compounds of formula (I) below:
wherein
Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X
1
, X
2
, X
3
, X
4
, X
5
, X
6
, X
7
and X
8
are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy1, Cy2, R1, R2, R3, R4, Ra and Rb is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
