CAS: 13367-85-6; Prostaglandinb2

该化合物是一种稳定的代谢物;PGB2因其在HPLC和LC-MS等分析技术中作为参考标准的作用,在生化研究中被广泛使用;其结构特征,包括α,β-不饱和克酮细胞,使它成为调查反应性碳基物种及其与细胞核素相互作用的宝贵探测器;PGB2还用于研究炎症,脂肪过氧化和酶动力学,提供对plesglandin代谢和相关生物过程的洞察.

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CAS号13345-50-1 前列腺素 A2 | CAS号31753-19-2 Prostaglandin A... | CAS号87692-38-4 15α-O-(t-butyld...

合成工艺路线路线简述

    📜前列腺素a2置于phosphate Buffer,二甲基环糊精体系中,化学反应生成前列腺素 B2
    参考文献:通过与甲基化的β-环糊精包合复合物来提高前列腺素e2和前列腺素a2的水稳定性.
    标题:通过与甲基化的β-环糊精包合复合物来提高前列腺素e2和前列腺素a2的水稳定性.
    摘要:研究了两种甲基化的β-环糊精,七羟甲基(2,6-二-O-甲基)-β-环糊精(dm-β-Cyd)和七羟甲基(2,3,6-三-O-甲基)-β-环糊精(tm-β-Cyd)对水性碱性溶液中前列腺素e2(pge2)脱水速率和前列腺素a2(pga2)异构化速率的影响,并与天然β-环糊精(β-Cyd)进行了比较.与β-Cyd的加速效应相反,Dm-β-Cyd和tm-β-Cyd均显著减缓了反应速率.其中,Dm-β-Cyd的稳定效应大于tm-β-Cyd.基于1:1的包合物形成,稳定常数和复合物的速率常数通过动力学测定.数据表明,Dm-β-Cyd在水溶液中对前列腺素e和前列腺素a的稳定化具有实用价值.
    Doi:10.1248/cpb.32.4237

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    专利信息


    专利号:US-2003050305-A1
    优先权日:2000-05-22
    标题:Thromboxane inhibitors, compositions and methods of use
    发明人:TEJADA INIGO SAENZ DE
    摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, and, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.

    专利号:US-5905091-A
    优先权日:1996-07-03
    标 题 :Enhancement of skin pigmentation by prostaglandins
    发明人:FULLER BRYAN B
    权利人:UNIV OKLAHOMA
    摘要:A composition comprising a carrier and prostaglandin effective in stimulating synthesis of melanin in a human melanocyte thereby enhancing pigmentation of the human skin and optionally comprising a lysosomotropic agent, a phosphodiesterase inhibitor, and/or methylxanthines, and a method of use of the composition. Use of this composition promotes tanning of the human skin and increases photoprotection from ultraviolet radiation.

    专利号:US-7772278-B2
    优先权日:1999-03-01
    标 题:Nitrosated and nitrosylated prostaglandins, compositions and methods of use
    发明人:GARVEY DAVID S; GASTON RICKY D; LETTS L GORDON; DE TEJADA INIGO SAENZ; TAM SANG WILLIAM; WORCEL MANUEL
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E 1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.

    专利号:WO-0054773-A1
    优先权日:1999-03-12
    标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC; GARVEY DAVID S
    摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

    专利号:US-5530114-A
    优先权日:1990-04-30
    标 题:Oligonucleotide modulation of arachidonic acid metabolism
    发明人:BENNETT CLARENCE F; ECKER DAVID J; CROOKE STANLEY T; MIRABELLI CHRISTOPHER K
    权利人:ISIS PHARMACEUTICALS INC
    摘要:PCT No. PCT/US91/02628 Sec. 371 Date Apr. 3, 1992 Sec. 102(e) Date Apr. 3, 1992 PCT Filed Apr. 17, 1991 PCT Pub. No. WO91/16901 PCT Pub. Date Nov. 14, 1991.Compositions and methods are provided for the treatment and diagnosis of diseases amenable to modulation of the synthesis or metabolism of arachidonic acid and related compounds. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically hybridizable with nucleic acids encoding 5-lipoxygenase, 5-lipoxygenase activating proteins, LTA4 hydrolase, phospholipase A2, phospholipase C, and coenzyme A-independent transacylase. The oligonucleotide comprises nucleotide units sufficient in identity and number to effect said specific hybridization. In other preferred embodiments, the oligonucleotides are specifically hybridizable with a transcription initiation site, a translation initiation site, and intron/exon junction. Methods of treating animals suffering from disease amenable to therapeutic intervention by modulating arachidonic acid synthesis or metabolism with an oligonucleotide or oligonucleotide analog specifically hybridizable with RNA or DNA corresponding to one of the foregoing proteins are disclosed. Methods for treatment of diseases responding to modulation of arachidonic acid synthesis or metabolism are disclosed.

    专利号:US-11976052-B2
    优先权日:2019-01-11
    标题:Leukotriene synthesis inhibitors
    发明人:BURGOYNE DAVID L; DEBRUIN ERIN; FONAREV JULIA; YEE JAMES GEE KEN; LANGLANDS JOHN MICHAEL
    权利人:NAEGIS PHARMACEUTICALS INC
    摘要:Provided are specific leukotriene synthesis inhibitor compounds and pharmaceutical compositions comprising the compounds and methods of using the compounds and the pharmaceutical compositions in treating, for example, inflammatory diseases or conditions.

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    主要参考文献

    参考标题:Prostaglandins And Congeners. 22. Synthesis Of 11-Substituted Derivatives Of 11-Deoxyprostaglandins E1 And E2. Potential Bronchodilators
    作者:M. Brawner Floyd,Robert E. Schaub,Gerald J. Siuta,Jerauld S. Skotnicki,Charles V. Grudzinskas,Martin J. Weiss,Franz Dessy,L. Vanhumbeeck |发布日期:1980.8
    摘要:The Interesting Bronchodilator Activity Of L-11-Deoxy-11 Alpha-[(2-Hydroxyethyl)Thio]Prostaglandin E2 Methyl Ester (3A) Is Described. The Preparation Of 3A And Its Analogues By Michael-Type Additions To Various Members Of The Pga Series Or By Total Synthesis Using The Lithiocuprate Conjugate Addition Process Is Also Described. Structure-Activity Relationships In This Series Are Discussed.

    合成参考文献


    参考文献:10.1046/j.1432-1327.2000.01109.x
    摘要:Tassin-Moindrot S, Caille A, Douliez JP, Marion D, Vovelle F. The wide binding properties of a wheat nonspecific lipid transfer protein. Solution structure of a complex with prostaglandin B2. Eur J Biochem. 2000 Feb;267(4):1117–24. doi: 10.1046/j.1432-1327.2000.01109.x.
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