標(biāo)題: Titlebook: Optimization in Drug Discovery; In Vitro Methods Gary W. Caldwell,Zhengyin Yan Book 2014Latest edition Springer Science+Business Media New [打印本頁(yè)] 作者: 磨損 時(shí)間: 2025-3-21 19:48
書目名稱Optimization in Drug Discovery影響因子(影響力)
書目名稱Optimization in Drug Discovery影響因子(影響力)學(xué)科排名
書目名稱Optimization in Drug Discovery網(wǎng)絡(luò)公開度
書目名稱Optimization in Drug Discovery網(wǎng)絡(luò)公開度學(xué)科排名
書目名稱Optimization in Drug Discovery被引頻次
書目名稱Optimization in Drug Discovery被引頻次學(xué)科排名
書目名稱Optimization in Drug Discovery年度引用
書目名稱Optimization in Drug Discovery年度引用學(xué)科排名
書目名稱Optimization in Drug Discovery讀者反饋
書目名稱Optimization in Drug Discovery讀者反饋學(xué)科排名
作者: cardiac-arrest 時(shí)間: 2025-3-21 20:23
Dennis Kalamaridis,Nayan Patelbe ich vor lauter Lampenfieber morgens vor dem Seminar nichts essen k?nnen. über drei Jahre lang, vier bis sechs Tage in der Woche nur Pfefferminztee und bis mittags einen knurrenden Magen! - Und je gr??er die Gruppe, desto mehr Stre? hatte ich. Viele Zuh?rer, die mich heute als Redner vor gro?en Gr作者: Anhydrous 時(shí)間: 2025-3-22 02:49
Dennis Kalamaridis,Karen DiLoretotatistik) ist die Be- schreibung des interessierenden Untersuchungsobjektes. Zur Erfüllung dieser Aufgabe sind in einem ersten Schritt die relevanten Daten des Untersuchungsob- jektes vollst?ndig zu erheben. Das dabei gewonnene, in der Regel sehr umfang- reiche Datenmaterial ist in einem zweiten Sch作者: chronology 時(shí)間: 2025-3-22 05:10
Gary W. Caldwell,Chrissa Ferguson,Robyn Buerger,Lovonia Kulp,Zhengyin Yanbe ich vor lauter Lampenfieber morgens vor dem Seminar nichts essen k?nnen. über drei Jahre lang, vier bis sechs Tage in der Woche nur Pfefferminztee und bis mittags einen knurrenden Magen! - Und je gr??er die Gruppe, desto mehr Stre? hatte ich. Viele Zuh?rer, die mich heute als Redner vor gro?en Gr作者: 人工制品 時(shí)間: 2025-3-22 12:39
Maria Markowska,L. Mark Kaotatistik) ist die Be- schreibung des interessierenden Untersuchungsobjektes. Zur Erfüllung dieser Aufgabe sind in einem ersten Schritt die relevanten Daten des Untersuchungsob- jektes vollst?ndig zu erheben. Das dabei gewonnene, in der Regel sehr umfang- reiche Datenmaterial ist in einem zweiten Sch作者: BRACE 時(shí)間: 2025-3-22 14:40 作者: Mirage 時(shí)間: 2025-3-22 20:05
Carlo Sensenhausertatistik (auch: deskriptive Statistik) ist die Be- schreibung des interessierenden Untersuchungsobjektes. Zur Erfüllung dieser Aufgabe sind in einem ersten Schritt die relevanten Daten des Untersuchungsob- jektes vollst?ndig zu erheben. Das dabei gewonnene, in der Regel sehr umfang- reiche Datenmaterial ist in einem zweiten Sch978-3-322-96538-7作者: travail 時(shí)間: 2025-3-22 23:48 作者: 必死 時(shí)間: 2025-3-23 03:22 作者: Accomplish 時(shí)間: 2025-3-23 06:24
Metabolic Stability Assessed by Liver Microsomes and Hepatocytes,tability for chemotypes suffering from high turnover, and predict . clearance. The latter is of particular importance to understand . correlations and select compounds with appropriate pharmacokinetics in humans. This chapter provides details on the methods used to investigate metabolic stability of作者: 出價(jià) 時(shí)間: 2025-3-23 13:00 作者: Palter 時(shí)間: 2025-3-23 15:42 作者: 序曲 時(shí)間: 2025-3-23 21:34 作者: 以煙熏消毒 時(shí)間: 2025-3-23 23:16
DNA Binding (Gel Retardation Assay) Analysis for Identification of Aryl Hydrocarbon (Ah) Receptor Aism of the test compounds. The GRA can also be used with nuclear extracts obtained from treated cells to further identify and/or characterize compounds capable of stimulating nuclear translocation and DNA binding of the AhR in intact cells. The methods described here can be applied to cytosolic, nuc作者: SPURN 時(shí)間: 2025-3-24 04:31
Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) Activators,c manner where the magnitude of reporter gene induction is directly proportional to the concentration and potency of the inducing chemical. The AhR agonist activity of positive test chemicals can be confirmed by demonstrating their ability to stimulate expression of CYP1A1, an endogenous AhR-respons作者: Amplify 時(shí)間: 2025-3-24 09:21
In Vitro CYP Induction Using Human Hepatocytes,gold standard for such . assays. Where appropriate in the chapter recent guidelines will be highlighted by regulatory agencies, such as, the Food and Drug Administration (FDA) and the European Medicines Agency (EMA).作者: 命令變成大炮 時(shí)間: 2025-3-24 12:02
Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomesors were calculated at different incubation time intervals. Plotting IC. values vs. incubation time revealed three different patterns for test inhibitors that could be used to distinguish reversible and time-dependent inhibitors. IC. values of reversible inhibitors either maintained within a narrow 作者: NOVA 時(shí)間: 2025-3-24 15:58 作者: placebo-effect 時(shí)間: 2025-3-24 22:00
Book 2014Latest edition candidates..Comprehensive and up-to-date, .Optimization in Drug Discovery: In Vitro Methods, Second Edition. aims to guide researchers down the difficult path to successful drug discovery and development..作者: 偏離 時(shí)間: 2025-3-25 02:33 作者: CAMP 時(shí)間: 2025-3-25 07:00 作者: GLARE 時(shí)間: 2025-3-25 09:37
978-1-4939-6070-5Springer Science+Business Media New York 2014作者: 簡(jiǎn)略 時(shí)間: 2025-3-25 13:13
Optimization in Drug Discovery978-1-62703-742-6Series ISSN 1557-2153 Series E-ISSN 1940-6053 作者: Irascible 時(shí)間: 2025-3-25 17:18 作者: 民間傳說(shuō) 時(shí)間: 2025-3-25 23:46
https://doi.org/10.1007/978-1-62703-742-6Biopharmaceutics; Drug candidates; In vitro and in situ assays; Pharmacodynamic; Pharmacokinetics; Toxico作者: Antagonist 時(shí)間: 2025-3-26 02:11
Gary W. Caldwell,Zhengyin YanProvides updated variations on assays as well as numerous new protocols for drug discovery optimization.Features readily reproducible methods and protocols that are lab-tested and successful.Includes 作者: 通便 時(shí)間: 2025-3-26 06:26
Gary W. Caldwell,Becki Hasting,John A. Masucci,Zhengyin Yanglischlehrers Gernot Ossiek unter einer Klassenarbeit aus dem 9. Schuljahr markieren in etwa den Startpunkt meiner Lern- karriere. Vermutlich hat sich Herr Ossiek genausowenig tr?umen lassen wie ich selbst, da? ich keine 20 Jahre sp?ter mit einer Amerikanerin verheiratet sein würde und meine Frau Me作者: Flat-Feet 時(shí)間: 2025-3-26 11:22 作者: reperfusion 時(shí)間: 2025-3-26 15:41
Dennis Kalamaridis,Karen DiLoreton- formiert werden. Ohne das Datenmaterial w?ren die Planung, Steuerung und Kontrolle des gesamten Unternehmensgeschehens nicht m?glich. Die erforderli- chen Daten werden dabei zum einen in ihrer ursprünglichen Form verwendet, zum anderen müssen sie für die Verwendung zuerst zweckorientiert aufberei作者: effrontery 時(shí)間: 2025-3-26 18:58
Gary W. Caldwell,Chrissa Ferguson,Robyn Buerger,Lovonia Kulp,Zhengyin Yanglischlehrers Gernot Ossiek unter einer Klassenarbeit aus dem 9. Schuljahr markieren in etwa den Startpunkt meiner Lern- karriere. Vermutlich hat sich Herr Ossiek genausowenig tr?umen lassen wie ich selbst, da? ich keine 20 Jahre sp?ter mit einer Amerikanerin verheiratet sein würde und meine Frau Me作者: bile648 時(shí)間: 2025-3-26 23:41
Maria Markowska,L. Mark Kaon- formiert werden. Ohne das Datenmaterial w?ren die Planung, Steuerung und Kontrolle des gesamten Unternehmensgeschehens nicht m?glich. Die erforderli- chen Daten werden dabei zum einen in ihrer ursprünglichen Form verwendet, zum anderen müssen sie für die Verwendung zuerst zweckorientiert aufberei作者: SLUMP 時(shí)間: 2025-3-27 03:11
Kevin J. Coe,Tatiana Koudriakovan- formiert werden. Ohne das Datenmaterial w?ren die Planung, Steuerung und Kontrolle des gesamten Unternehmensgeschehens nicht m?glich. Die erforderli- chen Daten werden dabei zum einen in ihrer ursprünglichen Form verwendet, zum anderen müssen sie für die Verwendung zuerst zweckorientiert aufberei作者: Etching 時(shí)間: 2025-3-27 06:12
Carlo Sensenhauser au?erhalb des Unternehmens in- formiert werden. Ohne das Datenmaterial w?ren die Planung, Steuerung und Kontrolle des gesamten Unternehmensgeschehens nicht m?glich. Die erforderli- chen Daten werden dabei zum einen in ihrer ursprünglichen Form verwendet, zum anderen müssen sie für die Verwendung zu作者: 慌張 時(shí)間: 2025-3-27 13:31 作者: Hdl348 時(shí)間: 2025-3-27 14:38
Assessment of Drug Plasma Protein Binding in Drug Discovery,es because the free drug concentration at the site of action is responsible for the pharmacological activity. This chapter will describe various methods commonly used for the . determination of plasma protein binding including classical equilibrium dialysis (CED), rapid equilibrium dialysis (RED), a作者: 宮殿般 時(shí)間: 2025-3-27 18:25
Drug Partition in Red Blood Cells,ertain therapeutic compounds have a high degree of affinity for the red blood cell fraction of whole blood and have large RBC-to-plasma concentration ratios. Knowledge of . RBC partitioning of compounds is important to the interpretation and understanding of the compounds pharmacokinetic profile and作者: palette 時(shí)間: 2025-3-27 23:25
Permeability Assessment Using 5-day Cultured Caco-2 Cell Monolayers,ormat. The 5-day accelerated Caco-2 assay is based on previous literature protocols where inserts are coated with collagen protein and the culturing cell media contains sodium butyrate to modify differentiation and growth properties of the cell line. Protocol conditions for the accelerated 5 day Cac作者: Nausea 時(shí)間: 2025-3-28 02:29
In Situ Single Pass Perfused Rat Intestinal Model, System (BCS) classification. BCS classification of drug candidates can influence the drug development path, specifically around formulation development, and the potential route used for drug administration. The . single pass perfused rat intestinal model has been shown to be highly predictive of hu作者: 嘮叨 時(shí)間: 2025-3-28 09:29
Metabolic Stability Assessed by Liver Microsomes and Hepatocytes,t undergo extensive metabolism. Drug metabolism can be assessed in a variety of . test systems, including microsomes, cytosol or S9 fractions, hepatocytes (suspension or plated), and isolated liver slices. In drug discovery, metabolic stability is typically determined by measuring the depletion of t作者: 作繭自縛 時(shí)間: 2025-3-28 13:53
Metabolic Assessment in Alamethicin-Activated Liver Microsomes: Co-activating CYPs and UGTs,lic pathways in microsomes. Alamethicin, a pore-forming peptide, was used to activate UGTs in human liver microsomes. An alamethicin-microsomal activated system in which both CYPs and UGTs were active can be used for studies of metabolic stability and . metabolite profiling. For compounds with minor作者: GENRE 時(shí)間: 2025-3-28 16:59 作者: HUMP 時(shí)間: 2025-3-28 22:12
In Vitro CYP/FMO Reaction Phenotyping, drug might be susceptible to changes in its exposure or to cause changes in the exposure of concomitantly administered drugs. The semi-quantitative assessment of the relative contributions of these pathways can provide early insight to the potential for drug-drug interactions or to possible affinit作者: 發(fā)酵劑 時(shí)間: 2025-3-29 00:57
Human Pregnane X Receptor (hPXR) Activation Assay in Stable Cell Lines,eractions (DDIs) is a wildly used technique among . assays. Direct assessment of PXR activation is a cell-based assay that requires two major components, the PXR and a reporter gene linked to the promoter and enhancer regions of the CYP3A gene. Because of species differences in the ligand binding re作者: 半導(dǎo)體 時(shí)間: 2025-3-29 04:22
Characterization of Constitutive Androstane Receptor (CAR) Activation,ous hepatic drug-metabolizing enzymes and transporters in response to various xenobiotic exposures. Unlike most prototypical nuclear receptors, however, CAR can be activated . both direct ligand-binding and ligand-independent indirect mechanisms. Moreover, whereas CAR predominantly resides in the cy作者: 設(shè)施 時(shí)間: 2025-3-29 07:21 作者: MOTIF 時(shí)間: 2025-3-29 12:58
Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) Activators,tructurally diverse synthetic and naturally occurring chemicals. The role of the AhR and its signaling pathway in endogenous physiological functions and its involvement in immune cell development and human diseases has made it a target for development of therapeutic agents. The ability of the AhR to作者: Estimable 時(shí)間: 2025-3-29 17:37
In Vitro CYP Induction Using Human Hepatocytes,ar receptors (NRs), respectively, is routinely determined during small molecule drug development. Significant CYP induction can result in therapeutic failure from clinical exposure of a compound outside the therapeutic window, if the respective enzymes are responsible for a significant portion of th作者: aristocracy 時(shí)間: 2025-3-29 22:57 作者: CLAY 時(shí)間: 2025-3-30 02:03
Evaluation of Time-Dependent CYP3A4 Inhibition Using Human Hepatocytes, a clinical interaction from pre-clinical TDI data have been lacking. Although more complex prediction algorithms have been developed, the accuracy has still improved little. This suggests alternate methods to collect input data may improve prediction robustness. Historically, human liver microsomes作者: Obstreperous 時(shí)間: 2025-3-30 04:02 作者: 以煙熏消毒 時(shí)間: 2025-3-30 11:06
Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM),t in clinically relevant drug-drug interactions (DDIs). Drugs that are time dependent inhibitors (TDIs) of CYPs have been reported to cause severe DDIs, leading to prescription adjustments and, in certain cases, have been withdrawn from the market (Zhou et al., Ther Drug Monit 29:687–710, 2007). Oft作者: Cpap155 時(shí)間: 2025-3-30 15:22
CYP Time-Dependent Inhibition (TDI) Using an IC50 Shift Assay with Stable Isotopic Labeled Substratstrates. The assay is performed in a 96-well format and can be fully automated and extended to a 384-well format if desired. Since the IC. shift assay requires parallel paired incubations to obtain two inhibition curves for comparison, the use of stable isotopic labeled probe substrates and non-labe作者: engender 時(shí)間: 2025-3-30 20:35
Book 2014Latest editioning formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity ass作者: Goblet-Cells 時(shí)間: 2025-3-31 00:11
1557-2153 s and protocols that are lab-tested and successful.Includes .Thoroughly revised and updated, .Optimization in Drug Discovery: In Vitro Methods, Second Edition. presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UD作者: 虛情假意 時(shí)間: 2025-3-31 01:48 作者: 亂砍 時(shí)間: 2025-3-31 07:25
Assessment of CYP3A4 Time-Dependent Inhibition in Plated and Suspended Human Hepatocytes,The metabolite 1′-hydroxymidazolam is then quantified by LC/MS/MS. The TDI potential of the test compound may then be evaluated by determining the enzyme activity remaining after each condition. Methods to determine K. and k. values from these data, as well as tips and considerations for robust assay outcomes are also provided.作者: wall-stress 時(shí)間: 2025-3-31 11:54
In Situ Single Pass Perfused Rat Intestinal Model, a complete radial mixing model. This model is an effective approach used for selecting drug candidates with a desired BCS classification, which ultimately could improve the success rate in the selection of new chemical entities for eventual clinical use.作者: critique 時(shí)間: 2025-3-31 13:35
Drug Partition in Red Blood Cells,rmination of blood-to-plasma ratios at the discovery level of development where species comparisons can be an important determinant in the design and interpretation of some observed pharmacokinetic study results. Methods employing the use of both radiolabeled and cold materials will also be discussed using a variety of analytical tools.作者: 消音器 時(shí)間: 2025-3-31 19:47 作者: JOG 時(shí)間: 2025-3-31 22:09 作者: LIEN 時(shí)間: 2025-4-1 04:16
Evaluation of Time-Dependent CYP3A4 Inhibition Using Human Hepatocytes,d the kinetic data derived from this matrix may provide a better prediction for assessing clinical interactions related to TDI. This chapter reviews a detailed method to assess TDI related to CYP3A in human hepatocytes.作者: Interstellar 時(shí)間: 2025-4-1 07:29 作者: Fabric 時(shí)間: 2025-4-1 10:44
Immune Function in Obese, Diabetic, Hyperinsulinemic C57BL/KsJ-db+/db+ and C57BL/6J-ob/ob Micetrations are markedly elevated in the range of 300–600 μU/ml. After approximately 6 months of age, plasma insulin concentrations fall to within the normal range of 10–100 μU/ml. Early in the course of the disease, during the period of hyperinsulinemia, the islets of Langerhans are characterized by β作者: Congestion 時(shí)間: 2025-4-1 15:47 作者: 逢迎白雪 時(shí)間: 2025-4-1 19:09
many diverse, although closely integrated, economies, a common characteristic is the significance of a sizeable and rapidly expanding SME sector. However, given such diversity, it can be reasonably expected that the SMEs in these economies are at different stages of development, their contributions
