Taurine can be metabolized by diverse organisms to form different types of metabolites derived from the original form of taurine. In the human, the pathways that form the metabolism of taurine are divided in the formation of 5-glutamyl-taurine by the action of the enzyme gamma-glutamyltransferase 6 or the formation of taurocholate by the action of the bile acid-CoA:amino acid N-acyltransferase.
There are two sources of taurine in the body: dietary and endogenous. In mammals, taurine is synthesised in many tissues; the main sites are liver, brain and pancreas, predominantly in alpha-islets. Taurine is synthesised from cysteine and methionine in a few steps, one of which requires pyridoxal-5-phosphate (vitamin B6) as coenzyme of cysteine sulphinate decarboxylase. In species other than mammals, the biosynthesis of taurine has been poorly studied. The extent of synthesis varies widely between species. An adult rat consuming standard laboratory food produces about 80 % of its total body taurine and obtains the remainder from the diet. However, if required, rats can obtain all body taurine from biosynthesis, since rats fed taurine-free diets for extended periods do not exhibit any decrease in tissue taurine concentrations. Cats have low levels of activity of cysteine sulphinate decarboxylase, the rate-limiting enzyme for taurine biosynthesis, and are, therefore, dependent on a dietary source to maintain their body pool of this amino acid. Thus, taurine is an essential nutrient in cats.
来源:Hazardous Substances Data Bank (HSDB)
代谢
牛磺胆酸盐是牛磺酸和胆酸通过酶胆酰辅酶A N-酰基转移酶作用形成的主要结合物。
Taurocholate, the bile salt conjugate of taurine and cholic acid, is the principal conjugate formed via the action of the enzyme choloyl-CoA N-acyltransferase.
In all vertebrates except mammals, taurine is the sole amino acid conjugated to form bile salts. Among the mammals, carnivores also tend to be conjugators of taurine only, whereas other species tend to conjugate both taurine and glycine. High concentrations of taurine are present in retina, liver, pancreas, central nervous system and white blood cells. The largest pools of taurine are found in skeletal and cardiac muscles, where it regulates intracellular Ca2+ concentration...
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
它阻止了大鼠中乙醇引起的高血压的发展。
It prevented the development of ethanol-induced hypertension in rats.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
在动物研究中，牛磺酸被发现可以改善博来霉素的肺部副作用（肺纤维化）。
In animal studies, taurine was found to ameliorate the pulmonary side effects (pulmonary fibrosis) of bleomycin.
...Three fatalities occurred after "energy" drinks had been consumed in combination with alcohol, whereby the forensic examinations including autopsy yielded negative results concerning medicaments and drugs, values between 0.59 and 0.87 parts per thousand of ethanol in blood samples, but no clear causes of death.
...Severe adverse effects arose after consumption of an "energy" drink in combination with physical efforts: A 31-year old regularly trained man consumed 750 mL of an "energy" drink while taking part in a 3,000 m competition. He developed a poor general condition with a rhabdomyolysis and acute kidney failure with tubular necrosis diagnosed one week after the competition.
/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/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
吸收
对牛磺酸的口服给药进行了研究，报告了AUC、Cmax和tmax的剂量依赖性值，其中1-30 mg/kg剂量的范围分别为89-3452 mcg min/L、2-15.7 mcg min/ml和15分钟。在健康个体中的进一步研究给出的AUC、Cmax和tmax范围分别为116-284.5 mg h/L、59-112.6 mg/L和1-2.5小时。
Oral administration of taurine was studied and it reported dose-dependent values of AUC, Cmax and tmax wherein a dose of 1-30 mg/kg ranged from 89-3452 mcg min/L, 2-15.7 mcg min/ml and 15 min respectively. Further studies in healthy individuals gave an AUC, Cmax and tmax in the range of 116-284.5 mg h/L, 59-112.6 mg/L and 1-2.5 h.
Taurine flows and gets distributed in veins and arteries and reports have observed the presence of a significant released of taurine in portally drained viscera, thus suggesting that the main elimination route of taurine is by the gut. This elimination route may be explained by the enterohepatic cycle of taurine.
The distribution of taurine was studied under the two-compartment model and each one of the compartments gave a range for the volume of distribution of 299-353 ml/kg in compartment 1 and 4608-8374 ml/kg in compartment 2 in mice. Further studies in healthy indivudals gave a volume of distribution that ranged from 19.8 to 40.7 L.
The clearance rate of orally administered taurine was reported to be dose-dependent wherein a dose of 1 mg/kg it presents a clearance rate of 11.7 ml min/kg, 10 mg/kg generates a clearance rate of 18.7 ml min/kg and a dose of 30 mg/kg reports a clearance rate of 9.4 ml min/kg. Further studies in healthy individuals generate a clearance rate that ranged from 14 to 34.4 L/h.
来源:DrugBank
吸收、分配和排泄
牛磺酸通常不会完全被肾脏重新吸收，摄入的牛磺酸有一部分会通过尿液排出。
Taurine is not usually completely reabsorbed from the kidneys, and some fraction of an ingested dose of taurine is excreted in the urine.
One-electron oxidation and reduction of glycosaminoglycan chloramides: A kinetic study
摘要：
Hypochlorous acid and its acid-base counterpart, hypochlorite ions, produced under inflammatory conditions, may produce chloramides of glycosaminoglycans, these being significant components of the extracellular matrix (ECM). This may occur through the binding of myeloperoxidase directly to the glycosaminoglycans. The N-Cl group in the chloramides is a potential selective target for both reducing and oxidizing radicals, leading possibly to more efficient and damaging fragmentation of these biopolymers relative to the parent glycosaminoglycans. In this study, the fast reaction techniques of pulse radiolysis and nanosecond laser flash photolysis have been used to generate both oxidizing and reducing radicals to react with the chloramides of hyaluronan (HAG) and heparin (HepCl). The strong reducing formate radicals and hydrated electrons were found to react rapidly with both HACl and HepCl with rate constants of 1-1.7 x 10(8) and 0.7-12 x 10(8) M-1 s(-1) for formate radicals and 2.2 x 10(9) and 7.2 x 10(8) M-1 s(-1) for hydrated electrons, respectively. The spectral characteristics of the products of these reactions were identical and were consistent with initial attack at the N-Cl groups, followed by elimination of chloride ions to produce nitrogen-centered radicals, which rearrange subsequently and rapidly to produce C-2 radicals on the glucosamine moiety, supporting an earlier EPR study by M.D. Rees et al. (J. Am. Chem. Soc. 125: 13719-13733; 2003). The oxidizing hydroxyl radicals also reacted rapidly with HACl and HepCl with rate constants of 2.2 x 10(8) and 1.6 x 10(8) M-1 s(-1), with no evidence from these data for any degree of selective attack on the N-Cl group relative to the N-H groups and other sites of attack. The carbonate anion radicals were much slower with HACl and HepCl than hydroxyl radicals (1.0 x 10(5) and 8.0 x 10(4) M-1 s(-1), respectively) but significantly faster than with the parent molecules (3.5 x 10(4) and 5.0 x 10(4) M-1 s(-1), respectively). These findings suggest that these potential in vivo radicals may react in a site-specific manner with the N-Cl group in the glycosaminoglycan chloramides of the ECM, possibly to produce more efficient fragmentation. This is the first study therefore to conclusively demonstrate that reducing radicals react rapidly with glycosaminoglycan chloramides in a site-specific attack at the N-Cl group, probably to produce a 100% efficient biopolymer fragmentation process. Although less reactive, carbonate radicals, which may be produced in vivo via reactions of peroxynitrite with serum levels of carbon dioxide, also appear to react in a highly site-specific manner at the N-Cl group. It is not yet known if such site-specific attacks by this important in vivo species lead to a more efficient fragmentation of the biopolymers than would be expected for attack by the stronger oxidizing species, the hydroxyl radical. It is clear, however, that the N-Cl group formed under inflammatory conditions in the extracellular matrix does present a more likely target for both reactive oxygen species and reducing species than the N-H groups in the parent glycosaminoglycans. (C) 2013 Elsevier Inc. All rights reserved.
Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors.
[EN] TRIAZINES SUITABLE FOR USE IN FABRIC TREATMENT COMPOSITIONS<br/>[FR] TRIAZINES POUVANT ETRE UTILISEES DANS DES COMPOSITIONS DE TRAITEMENT DE TISSUS
申请人：UNILEVER PLC
公开号：WO2005123699A1
公开（公告）日：2005-12-29
A water-soluble, triazine-based, non-dye, cellulose cross-linking agent that has a highly flexible linking group between at least two, mono-reactive cross-linking moieties and further hydrophilic or non-hydrophilic substituents, being preferrably represented by the general formula (I): (R1)(X1)T-L1-B-T(X2)(R2) wherein: R1 et R2 are cellulose-unreactive substituent groups on the s-triazine (T) and may be the same or different, X1 and X2 are leaving groups on the s-triazine which are lost on reaction with cellulose and may be the same or different, L1 et L2 are linking groups, an may be the same or different or absent, B is the bridging group comprising or consisting of at least one aliphatic polyoalkylene chain.
[EN] TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY<br/>[FR] DÉRIVÉS DE TRIAZOLE ET D'IMIDAZOLE DESTINÉS À ÊTRE UTILISÉS EN TANT QU'AGONISTES DE TGR5 DANS LE TRAITEMENT DU DIABÈTE ET DE L'OBÉSITÉ
申请人：EXELIXIS INC
公开号：WO2010093845A1
公开（公告）日：2010-08-19
The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.
Potential antiatherosclerotic agents. 3. Substituted benzoic and nonbenzoic acid analogs of cetaben
作者：J. Donald Albright、Vern G. DeVries、Mila T. Du、Elwood E. Largis、Thomas G. Miner、Marvin F. Reich、Robert G. Shepherd
DOI：10.1021/jm00364a010
日期：1983.10
acid group of cetaben is replaced by carboxylate ester, carboxamide, or a variety of other substituent groups is described. Also reported are the syntheses of analogues in which the phenyl ring of cetaben is either modified by the presence of additional substituents or replaced entirely by another moiety. Structure-activity relationships of these compounds both as hypolipidemic agents and as inhibitors
