CAS: 1131-64-2; Debrisoquin

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CAS号91-21-4 1,2,3,4-四氢异喹啉 | CAS号1184-90-3 氨基(亚氨基)甲磺酸 | CAS号59333-79-8 (±)4-羟基去氢异喹

📜2-Hydroxyamidino-1,2,3,4-Tetrahydroisoquinoline置于cytochrome B5,Mitochondrial Amidoxime Reducing Component 1,Nadh Cytochrome B5 Reductase,还原型辅酶ⅰ体系中,化学反应生成异喹胍
参考文献:The Fourth Molybdenum Containing Enzyme Marc: Cloning And Involvement In The Activation Of N-Hydroxylated Prodrugs
标题:The Fourth Molybdenum Containing Enzyme Marc: Cloning And Involvement In The Activation Of N-Hydroxylated Prodrugs
摘要:The Recently Discovered Mammalian Molybdoprotein Marc1 Is Capable Of Reducing N-Hydroxylated Compounds. Upon Reconstitution With Cytochrome B(5) And B5 Reductase,Benzamidoxime,Pentamidine,And Diminazene Amidoximes,N-Hydroxymelagatran,Guanoxabenz,And N-Hydroxydebrisoquine Are Efficiently Reduced. These Substances Are Amidoxime/n-Hydroxyguanidine Prodrugs,Leading To Improved Bioavailability Compared To The Active Amidines/guanidines. Thus,The Recombinant Enzyme Allows Prediction About In Vivo Reduction Of N-Hydroxylated Prodrugs. Furthermore,The Prodrug Principle Is Not Dependent On Cytochrome P450 Enzymes.
Doi:10.1021/jm8010417

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-9662347-B2
优先权日:2010-05-11
标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
发明人：LEE BONG HEE; BYUN KYUNG HEE
权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.

专利号:US-RE41998-E
优先权日:1990-02-26
标题 :Compositions and methods of treatment of sympathetically maintained pain
发明人：CAMPBELL JAMES N
权利人:ARCLON THERAPEUTICS INC
摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

专利号:US-5447947-A
优先权日:1990-02-26
标 题:Compositions and methods of treatment of sympathetically maintained pain
发明人：CAMPBELL JAMES N
权利人:ARC 1
摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-adrenergic antagonist, α-1-adrenergic antagonist, α2 adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine. Examples demonstrate relief of pain by application of phentolamine or clonidine.

专利号:US-9371387-B2
优先权日:2011-11-10
标题 :Composition for prevention or treatment of ischemic cardiac disease, comprising inhibitor against age-albumin synthesis or release of mononuclear phagocyte system cells as active ingredient
发明人：LEE BONG HEE; BYUN KYUNG HEE
权利人:UNIV GACHON IND ACAD COOP FOUND
摘要:Disclosed is a pharmaceutical composition for the prevention or treatment of ischemic heart diseases, comprising as an active ingredient an inhibitor which acts to restrain mononuclear phagocyte system cells from synthesizing or releasing AGE-albumin, which induces the apoptosis of cardiomyocytes upon the onset of the ischemic heart disease. Also, a method is provided for screening an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells. Inhibitory or suppressive of AGE-albumin-induced cell death, the pharmaceutical composition comprising as an active ingredient an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells can be applied to the prevention or treatment of a wide spectrum of ischemic heart diseases including myocardial infarction.

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications