liudan20061216 2020-07-02 13:20
1、动物:最好为大鼠或小鼠; 2、药品:口服的固体制剂(片剂、胶囊剂、颗粒剂都可以); 3、一整套项目研发资料,可将公司名称、关键技术数据打码,资料主要用于个人学习药物代谢动力学的研究方法和思路,不作商业用途。   [更多]
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crxdwa 2018-09-20 11:14
1、主要用于妇科、男科疾病 2、用于脑血栓、脑出血引起的后遗症   [更多]
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东陞家金线莲 2018-03-08 13:18
金线莲13大类含量及作用 金线莲的化学成分与含量中具有重要药理活性的物质主要为: 黄酮类化合物(槲皮素、异鼠李素): 黄酮类化合物是一类存在于自然界的、具有2-苯基色原酮(flavone)结构的化合物。它们分子中有一个酮式羰基,第一位上的氧原子具碱性,能与强酸成盐,其羟基衍生物多具黄色,故又称黄碱素或黄酮。黄酮类化合物在植物体中通常与糖结合成苷类,小部分以游离态(苷元)的形式存在。绝大多数植物体内都含有黄酮类化合物,它在植物的生长、发育、开花、结果以及抗菌防病等方起着重要的作用。 甾体类化合物(24~异丙烯基胆甾醇、开唇兰甾醇、麦角甾醇、豆甾醇、菜油甾醇、β-谷甾醇等): 化学结构中都具有甾体母核,即它的基本碳架具有一个“环戊烷并多氢菲”的母核和三个侧链。这类成分的甾体母核上,都在C3有羟基,并可和糖结合成苷,而C17侧链上育显著差别,根据C17链不同可以分为胆酸类、强心苷、甾醇和昆虫变态激素、C21甾体类、甾体皂苷和甾体生物碱等。甾体化合物广泛存在于动植物体内,许多具有各种生物活性,它们的应用非常广泛,有些被采用治疗疾病或发展生产,如治疗过敏性疾病的氢化可的松、避孕药黄体酮、利尿剂安体舒通、合成甾体激素的薯蓣皂甙元、强心作用的狄戈辛、蟾毒甙等都是甾体化合物。 三萜类化合物(木栓酮、琥珀酸、香豆酸、阿魏酸、胡萝卜苷、棕榈酸、齐墩果酸、熊果酸): 大部分为30个碳原子,少部分含27个碳原子的萜类化合物。三萜类成分(又叫灵芝酸)在自然界分布很广,鲨鱼油、甘草、五味子的有效成分中都有三萜类物质。灵芝三萜类成分有五环萜和四环三萜两类,按分子所含碳原子数可分为C30、C27、C24三大类,根据其所含功能团和不同的侧链,还可分成7种基本骨架。 多糖: 由15个分子的单糖所组成的大分子的糖叫多糖。由几种多糖组成的多糖,叫复合多糖。多糖是细胞的组成,又是细胞功能的重要基石,尤其能对免疫功能起到重要的调节作用,免疫多糖对免疫的调节是高效,无毒副作用的,而且作用点包括细胞免疫和体液免疫,作用点是全面、双向的,当免疫力低下时免疫多糖能提升,当免疫功能过高时能加以调节,使之正常化,并且通过神经-内分泌-免疫网络达到免疫的自稳和平衡。因此免疫多糖是当今世界公认的优良免疫调节剂。 低聚糖: 低聚糖集营养、保健、食疗于一体,广泛应用于食品、保健品、饮料、医药、饲料添加剂等领域。它是替代蔗糖的新型功能性糖源,是面向二十一世纪“未来型”新一代功效食品。是一种具有广泛适用范围和应用前景的新产品,近年来国际上颇为流行。美国、日本、欧洲等地均有规模化生产,我国低聚糖的开发和应用起于90年代中期,近几年发展迅猛。 还原糖: 还原糖是指具有还原性的糖类。在糖类中,分子中含有游离醛基或酮基的单糖和含有游离醛基的二糖都具有还原性。还原性糖包括葡萄糖、果糖、半乳糖、乳糖、麦芽糖等。 生物碱: 生物碱是存在于自然界(主要为植物,但有的也存在于动物)中的一类含氮的碱性有机化合物,有似碱的性质,所以过去又称为赝碱。大多数有复杂的环状结构,氮素多包含在环内,有显著的生物活性,是中草药中重要的有效成分之一。具有光学活性。有些不含碱性而来源于植物的含氮有机化合物,有明显的生物活性,故仍包括在生物碱的范围内。而有些来源于天然的含氮有机化合物,如某些维生素、氨基酸、肽类,习惯上又不属于“生物碱\"。 强心甙类: (Glycosides) 甙,又称配糖体或苷,是由糖或糖的衍生物(如糖醛酸)的半缩醛羟基与另一非糖物质中的羟基以缩醛键(甙键)脱水缩合而成的环状缩醛衍生物。水解后能生成糖与非糖化合物,非糖部分称为甙元(Ag1ycone),通常有酚类、蒽醌类、黄酮类等化合物。 酯类: 酸(羧酸或无机含氧酸)与醇起反应生成的一类有机化合物叫做酯。 分子通式为R-COO-R'(R可以是烃基,也可以是氢原子,R'不能为氢原子,否则就是羧基) 酯的官能团是-COO-,饱和一元酯的通式为CnH2nO2(n≥2,n为正整数)。 牛磺酸: 牛磺酸(Taurine)又称β-氨基乙磺酸,最早由牛黄中分离出来,故得名。纯品为无色或白色斜状晶体,无臭,牛磺酸化学性质稳定,不溶于乙醚等有机溶剂,是一种含硫的非蛋白氨基酸,在体内以游离状态存在,不参与体内蛋白的生物合成。牛磺酸虽然不参与蛋白质合成,但它却与胱氨酸、半胱氨酸的代谢密切相关。人体合成牛磺酸的半胱氨酸亚硫酸羧酶(CSAD)活性较低,主要依靠摄取食物中的牛磺酸来满足机体需要。 多种氨基酸: 氨基酸(amino   [更多]
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yuan89 2017-07-26 09:00
1、calcitonin C 是鲑降钙素的一个杂质。 2、最好是比较权威的资料或者文献,在业内有一定的认可。 3、多少的日用剂量对人体是安全的。   [更多]
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richard16 2016-08-26 14:32
当药物引起的胃肠道毒性发生时,通过细胞毒性,抑制细胞增殖,或者药物对受体和酶的不良影响,损害表现为各种临床症状,包括恶心,呕吐,溃疡,和腹泻。理解这一点的重要性并且减少这些负面效果。阿斯利康公司寻求体外模型,有关胃肠道毒性起效和恢复的研究。 实验论证稿件请于2016年10月26日发送到: https://www.innocentive.com/ar/challenge/9933828   [更多]
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lyj19721101 2015-05-14 17:30
阿斯利康提出需求:在大多数的慢性肾脏疾病的情况下有关肾小球滤过屏障功能受损的研究。缺少良好的肾小球体外模型,就不能在细胞学和病理学的范畴详细理解肾小球的功能。 阿斯利康正在寻找方法来开发一个肾小球模型系统。理想情况下,体外模型应该包含一个独立的微型药学单元,有适当的介质,流体流动和所受压力。可以调整模拟体内黏膜所需条件属性,最终建立形成一个功能肾小球滤过屏障。 具体看下面内容: https://www.innocentive.com/ar/challenge/9933748The majority of all cases of chronic kidney disease, a key research area within AstraZeneca, originate in the glomerulus when filtration barrier function is compromised. However, a detailed cellular understanding of the functioning and pathology of the glomerulus has been limited by the lack of good in vitro models of glomerular function. AstraZeneca is looking for approaches to develop a glomerular model system. Ideally, the in vitro model should incorporate a self-contained microphysiological unit where biologically appropriate media, fluid flow and shear stress can be modulated to simulate in vivo properties that will ultimately recapitulate the conditions necessary for endothelial and podocyte cell types to form a functional glomerular filtration barrier. This is an ideation challenge and only requires a written solution. Source: InnoCentive Challenge ID: 9933748 Challenge Overview The majority of all cases of chronic kidney disease, a key research area within AstraZeneca, originate in the glomerulus when filtration barrier is compromised. The coordinated efforts of the podocytes and endothelium together with their underlying basement membrane establish the glomerular filtration barrier and injury to these cells can lead to loss of kidney function. There are currently no human in vitro models that mimic a functional or diseased glomerulus. Development of a human glomerular filtration barrier biomimetic system will thus address gaps in in vitro models for simulating human kidney disease, toxicity and DMPK. We are looking for innovative approaches to developing a glomerular model that incorporates a self-contained microphysiological unit, ideally including podocytes, the endothelium, and   [更多]
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lyj19721101 2015-05-14 17:09
肾近端小管是肾单位的一部分(肾脏的功能部件),是人体高专属性参与重吸收和排泄各种物质(包括盐和矿物质)的器官,盐和矿物质的重吸收对身体是非常重要的,否则会失去在尿液中。此外,肾近端小管对许多药物的处理也是至关重要的,所谓的外源性物质,来自外面的身体和环境(如许多人造物质,包括潜在的毒素)。然而,没有好的体外模型可以描述和模仿肾近端小管的功能。建立肾近端小管一个有力的模型是非常必要的,特别是在肾近端小管在药物的相互影响方面有至关重要的作用,因为它是会由于药物毒性和药物之间的作用而非常容易受到伤害导致肾脏疾病。在体外开发肾近端小管模型的系统可以帮助填补肾脏疾病研究中药物毒性和药物处理方面的一些空白。 具体看 https://www.innocentive.com/ar/challenge/9933749 The proximal tubule, a part of the kidney nephron (the functional unit of the kidney), has highly specialized properties to do with the salvage and excretion of various compounds, salts and minerals that are very important to the body and would otherwise be lost in the urine. In addition, the proximal tubule is essential for the handling of many drugs and so-called xenobiotics that come from outside the body and from the environment (e.g., many artificial substances, including potential toxins). However, there are no good human models in vitro that can recapitulate and reproduce the function of the proximal tubule. A robust model for the proximal tubule is needed, especially since the proximal tubule has an essential role in drug clearance, because it is highly susceptible to damage in many kidney diseases, and it is also a target for drug-drug interactions and drug toxicity. Development of a proximal tubule model system in vitro could help to address some of the gaps in laboratory models for the study of kidney disease, toxicity, and drug handling. AstraZeneca is seeking innovative approaches to developing a model system of the proximal tubule in vitro. Ideally, the model should incorporate a self-contained microphysiological unit in which biologically appropriate media, fluid flow, and shear stress can be modulated to reproduce the properties of the proximal tubule in vivo and ultimately recapitulate the structural and cellular conditions necessary for integrated proximal tubular function. This is an ideation challenge and only requires a written solution. Source: InnoCentive Challenge ID:   [更多]
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lyj19721101 2015-01-27 15:01
抑制细胞外神经信号的作用可以通过抑制受体或去除配位体来产生。我们需要一个实例或证据来证明抑制受体和损耗配体是怎么阻断信号的,比如可以变构小分子或大分子或竞争性抑制。具体看下面链接: https://www.innocentive.com/ar/challenge/9933720 AWARD: $20,000 USD | DEADLINE: 2/25/15 | ACTIVE SOLVERS: 19 | POSTED: 1/26/15 Inhibition of extracellular signaling can occur through an inhibition of a receptor or removal of a ligand. What evidence is there that one method of inhibition is more efficient or efficacious than the other at blocking signaling? The Seeker is specifically looking for well-supported examples of receptor/ligand inhibition where both methods of inhibition exist. This Challenge requires only a written proposal. Source: InnoCentive Challenge ID: 9933720 Challenge Overview Inhibition of extracellular neuronal signaling can occur through the inhibition of a receptor or removal of a ligand. What evidence is there (or lack of) that one method of inhibition (inhibition of the receptor versus depletion of the ligand) is more efficient or efficacious than the other at blocking signaling? Inhibition can be allosteric or competitive, small molecule or large molecule. The Seeker is specifically looking for well-supported examples of receptor/ligand inhibition where both methods of inhibition exist. Submissions to this Challenge must be received by 11:59 PM (US Eastern Time) on February 25, 2015. Late submissions will not be considered.   [更多]
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lyj19721101 2015-01-24 14:08
药物代谢酶的过程中,肝脏是主要负责将药物基质脂溶性化合物转化为水溶性代谢物,可以很容易地通过肾脏排泄的。偶尔,这些代谢产物也会不恰当地和血蛋白结合,从而导致药物的不良反应。阿斯利康希望寻找一种定量测定共价结合细胞蛋白质的新方法。具体的链接请看下面: https://www.innocentive.com/ar/challenge/9933662 AWARD: $25,000 USD | DEADLINE: 3/16/15 | ACTIVE SOLVERS: 74 | POSTED: 1/16/15 Drug metabolism is the enzymatic process by which the body modifies pharmaceutical substrates. The liver is primarily responsible for reactions which convert lipid-soluble compounds into water-soluble metabolites that can easily be excreted by the kidney. Occasionally, these metabolites exhibit chemically reactivity towards host proteins, leading to inappropriate binding that may result in adverse drug reactions. AstraZeneca desires an innovative approach for the quantitative measurement of covalent binding to cellular proteins. This Challenge requires only a written proposal. Source: InnoCentive Challenge ID: 9933662 Challenge Overview When new medicines are introduced to the market, not only does the drug need to have a proven therapeutic benefit, but it also must possess an acceptable safety profile. To this end, drug development focuses on minimizing adverse drug reactions (ADRs) and idiosyncratic drug toxicities. ADRs are a major complication of drug therapy and come as a result of drug accumulation and/or the formation of chemically reactive metabolites (CRMs). Formation of CRMs within a cell poses an undesirable chemical liability and for this reason, AstraZeneca desires an innovative approach for the quantitative measurement of covalent binding of metabolites to cellular proteins. ABOUT THE SEEKER AstraZeneca is a global, research-based, biopharmaceutical company with a focus on five key therapeutic areas: 1) cardiovascular & metabolic diseases, 2) oncology, 3) respiratory, inflammation & autoimmunity, 4) neuroscience, and 5) infection. As an innovation-driven, research organization, AstraZeneca recognizes that great ideas come from many sources. Open innovation is an   [更多]
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lyj19721101 2014-12-16 15:54
重性抑郁障碍(MDD)是一种使人衰弱的精神障碍,在美国约有20000000流行病例。然而不同的抗抑郁药可用于治疗不同的抑郁症,,约50%的抑郁症患者的初始治疗结果不理想。最近有证据表明,在发病的几个小时内氯胺酮给药治疗难治性抑郁症已经显著有所改善。勃林格殷格翰公司寻找氯胺酮在人体中反应和持续的抗抑郁作用的机理。 Boehringer Ingelheim Challenge: Understanding the Antidepressant Effect of Ketamine TAGS: Nature, Chemistry, Life Sciences, Ideation AWARD: $21,000 USD | DEADLINE: 1/15/15 | ACTIVE SOLVERS: 20 | POSTED: 12/15/14 1. The Challenge and qualification for the award Major depressive disorder (MDD) is a debilitating psychiatric disorder with about 20 million prevalent cases in the United States. Various antidepressants are available for treatment of patients suffering from MDD, however, about 50% of MDD patients do not respond adequately to initial treatments. Recent evidence shows that ketamine administered to patients with treatment resistant depression has resulted in marked improvement within hours of treatment. Boehringer Ingelheim (the Seeker) desires a working hypothesis for ketamine’s mechanism of action and sustained antidepressant effect. The submitted solutions will be considered for the award. There will be a guaranteed award for at least one submitted solution. The total payout will be $21,000, with at least one award being no smaller than $12,000 and no award being smaller than $3,000. 2. Additional application for Research Funding In addition to consideration for the award for the submitted Solutions, Solvers with appropriate qualifications and expertise having access to a suitable research laboratory and equipment can apply for research funding (“Research Funding”) to execute a research plan that is proposed in the Solution. The requested funding should not exceed a funding period of 2 years and a total budget of $200,000. The selection of candidates for Research Funding will be conducted after completion of this Challenge, and will require the submission of additional information. The decision to fund research will be at the discretion of the Seeker.   [更多]
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