CAS: 708-79-2; 1-Methyl-1H-Purine-2,6,8(3H,7H,9H)-Trione

上下游产品

CAS号6136-37-4 3,7-二氢-1-甲基-1H-... | CAS号57-13-6 尿素 | CAS号944-73-0 1,3-二甲基尿酸 | CAS号108074-34-6 1-methyl-4,5-di... | CAS号10034-85-2 氢碘酸 | CAS号7732-18-5 水 | CAS号854883-69-5 5-acetoxy-9-ace... | CAS号944-73-0 1,3-二甲基尿酸 | CAS号569-34-6 8-METHOXYCAFFEINE

📜1,3-二甲基尿酸置于rat Liver Microsome,还原型辅酶ii(Nadph)四钠盐体系中,用 Phosphate Buffer 作为反应溶剂,化学反应生成 1-U 1-甲基-2,6,8-三羟基嘌呤 1Mua
参考文献:Inhibition Kinetics Of Theophylline Metabolism By Mexiletine And Its Metabolites.
标题:Inhibition Kinetics Of Theophylline Metabolism By Mexiletine And Its Metabolites.
摘要:为了进一步确定茶碱(tp)和美西利汀(me)之间的药物相互作用模式,研究人员使用大鼠肝脏微粒体和 9000xg 上清液进行了体外动力学研究.动力学研究结果表明,在四种代谢途径中,将 Tp 代谢转化为 1,3-二甲基尿酸(1,3-Dmu)的 Km 值和 Vmax/km 比值分别为第二低和最高.因此,微粒体细胞色素 P-450 同工酶(p-450)的氧化代谢效率排序为 Tp 至 1,3-Dmu>Tp 至 1-甲基黄嘌呤(1-Mx)>Tp 至 3-Mx>1,3-Dmu 至 1-甲基尿酸,这表明代谢 Tp 的同工酶对 Tp 分子中 8 位的氧化亲和力高于 1 位和 3 位.lineweaver-Burk 图显示,Tp 向 3-Mx 和 1,3-Dmu 的转化受到 Me 及其代谢物的竞争性抑制,而 Tp 向 1-Mx 的转化途径则受到非竞争性抑制.从计算出的 Ki 值来看,脱氨基-对羟基 Me(daphme)可能是 Tp 代谢途径中最有效的抑制剂,其抑制作用的顺序大约是 Daphme>P-Hydroxy Me>Deamino-Hydroxymethyl Me>Me>Hydroxymethyl Me,但也有一些例外.tp 和 Me 之间的相互作用机制可能是由于肝脏中的代谢拮抗作用,Tp,Me 及其代谢物在 P-450 同工酶的介导下具有一些相同的代谢途径.
DOI:10.1248/bpb.18.75

专利信息

专利号:WO-9925699-A1
优先权日:1997-11-19
标 题:Salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids and 5,5'-arylidenebis(2-thiobarbituric) acids having an antibacterial, anti-chlamydial, antiviral and immuno-modulating activity
发明人：ASHKINAZI RIMMA ILIINICHNA
权利人:TETS VIKTOR VENIAMINOICH; ASHKINAZI RIMMA ILIINICHNA
摘要:The present invention relates to the production of new chemical substances having an anti-microbial, antiviral, immuno-modulating and anti-tumoral activity. This invention more precisely relates to the synthesis of new substances consisting of 5,5'-arylidenebis(2-thiobarbituric) acids and in salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids of general formula (I) where X is oxygen or sulphur. R1 is hydrogen, a nitro group or an alkoxy group, R2 is hydrogen, a nitro group, an alkoxy group or halogen and Cat+ is a proton or a pyridin- or 2-hydroxyethylammonium-cation. In the preferred embodiments of these substances, the following conditions are observed: X=O, Cat+ is pyridine, R1=H and R2=Cl (I); X=O, Cat+ is pyridine, R1=H and R2=NO2 (II); X=O, Cat+ is H3N+CH2CH2OH, R1=H and R2=NO2 (III); X=S, Cat+ is pyridine, R1=H and R2=Cl (IV); X=S, Cat+ is pyridine, R1=H and R2=OH (V); X=S, Cat+ is pyridine, R1=NO2 and R2=H (VI); X=S, Cat+ is pyridine and R1=R2=MeO (VII); X=O, Cat+ is pyridine, R1=H and R2=Br (VIII); X=O, Cat?+ is H+, R1¿=H and R2=Cl (IX); X=O, Cat?+ is H+, R1¿=H and R2=NO2 (X). This invention also relates to eight synthesis instances of these substances, to three tables representing the chemical and physical characteristics of the substances thus obtained and to the results of five series of experiments. These synthesis instances, tables and results demonstrate the biological properties of these substances on myco-bacteria, on herpes viruses and on Chlamydia trachomatis as well as their interferon-inducing activity and the absence of acute toxicity.

专利号:US-6355416-B1
优先权日:1997-02-14
标 题:Assay for the measurement of DNA synthesis rates
发明人：ABRAMSON FRED P
权利人:UNIV GEORGE WASHINGTON
摘要:Use of nonradioactive tracer technology used to measure DNA synthesis rates. DNA synthesis is determined by administering one or more stable isotope labelled precursors to one or more of DNA molecules and the amount of the stable isotope label in the DNA that is extracted from cells that are of interest is measured.

专利号:WO-2011114184-A1
优先权日:2010-03-15
标题 :Amides of heterocyclic compounds as trpa1 inhibitors
发明人：CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; WAGHMARE NAYAN TATERAO; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL
权利人:GLENMARK PHARMACEUTICALS SA; CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; WAGHMARE NAYAN TATERAO; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL
摘要:Amides of heterocyclic compounds as Transient Receptor Potential subfamily A (TRPA) modulators are provided In particular, compounds described herein are useful for treating or preventing diseases, conditions and/ or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1) Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. (I).

专利号:WO-9836095-A1
优先权日:1997-02-14
标 题 :An assay for the measurement of dna synthesis rates

专利号:CA-2281111-A1
优先权日:1997-02-14
标题 :An assay for the measurement of dna synthesis rates

专利号:AU-745236-B2
优先权日:1997-02-14
标 题 :An assay for the measurement of DNA synthesis rates