Palladium may be absorbed through oral, dermal, and inhalation exposure. Once in the body it distributes to the kidney, liver, spleen, lymph nodes, adrenal gland, lung and bone. Palladium's ability to form complexes allows it the bind to amino acids, proteins, DNA, and other macromolecules. Palladium and its metabolites are excreted in the urine and faeces. (A21)
IDENTIFICATION: Palladium chloride is a rust colored powder soluble in water, hydrochloric acid, alcohol and acetone. This compound used in plating baths. It is used in photography, toning solutions, electroplating parts of clocks and watches, detecting carbon monoxide leaks in burried gas pipes, manufacture of indelible ink. Palladium chloride is available in purity grades 99% to 99.999%. HUMAN EXPOSURE: A few studies indicate individuals showed a positive skin reaction to palladium chloride patches. ANIMAL/PLANT STUDIES/AQUATIC ORGANISMS: Palladium chloride was poorly absorbed from the digestive tract in adult and suckling rats. Absorption and retention in adult rats was higher following intratracheal or iv exposure. Transfer of small amounts of palladium to offspring via placenta and milk was noted with a single iv doses of this compound. Rats injected with (103)C-palladium chloride mean retention time changed little for the kidney, spleen, muscle, pancreas, thymus, brain. They decreased slightly in liver and markedly in lung, adrenal glandf and blood. Mice given palladium chloride in drinking water from weaning until natural death showed suppression of body weight, a longer life span only in males, an increase in amyloidosis of several inner organs and doubling of malignant tumors. The compound induced eye irritation in rabbits. It also caused erythema in intact and abraded skin. Palladium chloride is a potent skin sensitizer. Reduced testicle weight was noted in mice that recieved sc doses. Mice given palladium chloride in drinking water until natural death developed lymphomas, leukemias and adenocarcinoma of the lung. Eye irritation noted in the eye of a rabbit treated with palladium chloride. This compound inhibited DNA/RNA biosynthesis in vitro with mouse fibroblasts. Palladium chloride is highly toxic to a fresh water worm Tubifex tubifex. It is also highly toxic to fish and grasses.[
Due to their ability to form strong complexes with both inorganic and organic ligands, palladium ions can disturb cellular equilibria, replace other essential ions, and interact with functional groups of macromolecules, such as proteins or DNA. Palladium complexes binding to DNA and RNA leads to strand breakage. Palladium ions are able to inhibit most major cellular functions, including DNA and RNA synthesis. Palladium compounds have been shown to bind to and inhibit various enzymes, including creatine kinase and prolyl hydroxylase. (L798)
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).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
健康影响
与钯接触可能会导致钯敏感和过敏。动物研究显示，钯可能会对肝脏和肾脏造成损害。
Contact with palladium may cause palladium sensitivity and allergy. Animal studies have shown that palladium may damage the liver and kidney. (L798)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
症状
皮肤接触钯可能会导致接触性皮炎、红斑和水肿。
Skin contact with palladium may cause contact dermatitis, erythema, and oedema. (L798)
来源:Toxin and Toxin Target Database (T3DB)
吸收、分配和排泄
氯化钯不易通过皮下注射被吸收...
Palladium chloride is not readily absorbed from sc injection ... .
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
钯从胃肠道（GI）的吸收是微不足道的。给Charles River CD-1雄性大鼠单次胃内剂量的103Pd同位素后，该同位素会迅速从它们体内通过粪便排出。总保留率低于0.5%。24小时后，仅在肝脏和肾脏中发现了微量的氯化钯；104天后在任何分析的组织或器官中都没有发现氯化钯。静脉注射氯化钯后，观察到显著更高的吸收和保留。在肾脏、脾脏、肝脏、肾上腺、肺和骨骼中发现了103PdCl2同位素最高浓度。在接受了25微克PdCl2和0.2毫升生理盐水的Charles River CD-1雄性大鼠中，3天后动物器官中的保留量为初始剂量的0.4%，吸收量小于初始剂量的0.5%。经气管内给药后，在肺中观察到103Pd的最高浓度，其次是肾脏、脾脏、骨骼和肝脏。
The absorption of palladium from the GI tract is insignificant. A single intragastrical dose of 103Pd isotope given to male Charles River CD-1 rats was rapidly excreted from their organism with feces. The total retention was lower than 0.5%. After 24 hr, insignificant quantities of palladium chloride were found only in liver and kidneys; after 104 days no palladium chloride was found in any analyzed tissue or organ. A considerably higher absorption and retention were observed after iv administration of palladium chloride. The highest concentration of 103PdCl2 isotope was found in kidneys, spleen, liver, adrenals, lungs, and bones. ...In male Charles River CD-1 rats receiving 25 ug PdCl2 in 0.2 mL saline, the retention in the animals' organs after 3 days was 0.4% of the initial charge and the absorption was <0.5% of the initial dose. ...After intratracheal administration, the highest concentrations of 103Pd were observed in lungs, followed by kidneys, spleen, bones, and liver.
The presence of 103Pd isotope was also examined in the internal organs of female rats receiving PdCl2 iv on 16th day of gestation. The concentration of 103Pd was assessed in various organs of the dams and in fetuses 24 hr after the administration. The low concentration of 103Pd isotope in fetal bodies indicates that Pd does not easily penetrate the placenta.
Dietary administration to rats of high levels of the slightly water-soluble palladium salts /including/ palladium(II) chloride... (about 3000 mg palladium/kg feed for 4 weeks; corresponding to about 700 mg/kg bw/day) resulted in palladium tissue concentrations (in mg/kg wet weight) as follows: kidney (35, respectively) >liver (2) >spleen (0.7) >testis (0.24) >blood (<0.04) >brain (<0.01). ...The total consumption during the 4-wk diet period amounted to about 2000 mg palladium/rat (i.e., 2020 mg palladium/rat from palladium(II) chloride; mean body weights of the rats when started on the diets: 100-110 g).
Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
4-Allyl azetidinone intermediate for .beta.-lactam antibacterial agents
申请人：Beecham Group Limited
公开号：US04401595A1
公开（公告）日：1983-08-30
Compounds are provided of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group and A.sub.1 is a hydrogen atom or a methyl group. These compounds possess antibacterial activity. The preparation of these compounds is described.
Imidazolyl compounds as inhibitors of farnesyl-protein tranferase
申请人：Zeneca Limited
公开号：US06414145B1
公开（公告）日：2002-07-02
The present invention relates to inhibitors of ras farnesylation of Formula (I), wherein T is of Formula (1) or (2) or (3); A is aryl or heteroaryl; B is aryl or heteroaryl; X and Y represent hydrogen, or both X and Y can represent a single bond (so as to form a double bond); R1 represents a group of Formula (II) or (III), the group of Formula (II) or Formula (III) (having L or D configuration at the chiral alpha carbon in the corresponding free amino acid); R2 represents hydrogen, aryl or heteroaryl; Z represents a direct bond, methylene, ethylene, vinylene, oxy, —CH2—O— or —O—CH2—; and R3—R4, p and r are as defined in the specification or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy
Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against bacteria, including gram positive organisms, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
Process for the preparation of octyl p-methoxy cinnamate
申请人：Bromine Compounds Ltd.
公开号：US05728865A1
公开（公告）日：1998-03-17
A process for the preparation of octyl p-methoxy cinnamate is provided. The procedure generally concerns reacting p-bromo anisole with acrylic acid; and esterifying the resulting product with 2-ethyl hexanol. Preferred reactants and conditions are provided.
