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Current Protocols in Pharmacology最新文献

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Models of Inflammation: Carrageenan Air Pouch 炎症模型:卡拉胶气囊
Current Protocols in Pharmacology Pub Date : 2016-03-18 DOI: 10.1002/0471141755.ph0506s72
Djane B. Duarte, Michael R. Vasko, Jill C. Fehrenbacher
{"title":"Models of Inflammation: Carrageenan Air Pouch","authors":"Djane B. Duarte,&nbsp;Michael R. Vasko,&nbsp;Jill C. Fehrenbacher","doi":"10.1002/0471141755.ph0506s72","DOIUrl":"10.1002/0471141755.ph0506s72","url":null,"abstract":"<p>The subcutaneous air pouch is an in vivo model that can be used to study the components of acute and chronic inflammation, the resolution of the inflammatory response, the oxidative stress response, and potential therapeutic targets for treating inflammation. Injection of irritants into an air pouch in rats or mice induces an inflammatory response that can be quantified by the volume of exudate produced, the infiltration of cells, and the release of inflammatory mediators. The model presented in this unit has been extensively used to identify potential anti-inflammatory drugs. © 2016 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"72 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph0506s72","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50807033","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 22
In Vitro Binding of [3H]PSB-0413 to P2Y12 Receptors [3H]PSB-0413与P2Y12受体的体外结合
Current Protocols in Pharmacology Pub Date : 2015-12-08 DOI: 10.1002/0471141755.ph0135s71
Arnaud Dupuis, Véronique Heim, Philippe Ohlmann, Christian Gachet
{"title":"In Vitro Binding of [3H]PSB-0413 to P2Y12 Receptors","authors":"Arnaud Dupuis,&nbsp;Véronique Heim,&nbsp;Philippe Ohlmann,&nbsp;Christian Gachet","doi":"10.1002/0471141755.ph0135s71","DOIUrl":"10.1002/0471141755.ph0135s71","url":null,"abstract":"<p>The P2Y<sub>12</sub> /ADP receptor plays a central role in platelet activation. Characterization of this receptor is mandatory for studying disorders associated with a P2Y<sub>12</sub> receptor defect and for evaluating P2Y<sub>12</sub> receptor agonists and antagonists. In the absence of suitable anti-P2Y<sub>12</sub> antibodies, radioligand binding assays are the only way to conduct such studies. While various radioligands were employed in the past for this purpose, none were found to be suitable for routine use. Described in this unit are protocols for quantitatively and qualitatively assessing P2Y<sub>12</sub> receptors with [<sup>3</sup>H]PSB-0413, a selective antagonist for this site. The saturation and competition assays described herein make possible the determination of P2Y<sub>12</sub> receptor density on cells, as well as the potencies and affinities of test agents at this site. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"71 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph0135s71","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50803474","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Sigma Receptor Binding Assays Sigma受体结合试验
Current Protocols in Pharmacology Pub Date : 2015-12-08 DOI: 10.1002/0471141755.ph0134s71
Uyen B. Chu, Arnold E. Ruoho
{"title":"Sigma Receptor Binding Assays","authors":"Uyen B. Chu,&nbsp;Arnold E. Ruoho","doi":"10.1002/0471141755.ph0134s71","DOIUrl":"10.1002/0471141755.ph0134s71","url":null,"abstract":"<p>Sigma receptors, both Sigma-1(S1R) and Sigma-2 (S2R), are small molecule-regulated, primarily endoplasmic reticulum (ER) membrane-associated sites. A number of drugs bind to sigma receptors, including the antipsychotic haloperidol and (+)-pentazocine, an opioid analgesic. Sigma receptors are implicated in many central nervous system disorders, in particular Alzheimer's disease and conditions associated with motor control, such as Amyotrophic Lateral Sclerosis (ALS). Described in this unit are radioligand binding assays used for the pharmacological characterization of S1R and S2R. Methods detailed include a radioligand saturation binding assay for defining receptor densities and a competitive inhibition binding assay employing [<sup>3</sup>H]-(+)-pentazocine for identifying and characterizing novel ligands that interact with S1R. Procedures using [<sup>3</sup>H]-1,3-di(2-tolyl)guanidine ([<sup>3</sup>H]-DTG), a nonselective sigma receptor ligand, are described for conducting a saturation binding and competitive inhibition assays for the S2R site. These protocols are of value in drug discovery in identifying new sigma ligands and in the characterization of these receptors. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"71 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph0134s71","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50803233","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 22
Measurement of Glucose Uptake in Cultured Cells 培养细胞葡萄糖摄取的测定
Current Protocols in Pharmacology Pub Date : 2015-12-08 DOI: 10.1002/0471141755.ph1214s71
Norio Yamamoto, Manabu Ueda-Wakagi, Takuya Sato, Kengo Kawasaki, Keisuke Sawada, Kyuichi Kawabata, Mitsugu Akagawa, Hitoshi Ashida
{"title":"Measurement of Glucose Uptake in Cultured Cells","authors":"Norio Yamamoto,&nbsp;Manabu Ueda-Wakagi,&nbsp;Takuya Sato,&nbsp;Kengo Kawasaki,&nbsp;Keisuke Sawada,&nbsp;Kyuichi Kawabata,&nbsp;Mitsugu Akagawa,&nbsp;Hitoshi Ashida","doi":"10.1002/0471141755.ph1214s71","DOIUrl":"10.1002/0471141755.ph1214s71","url":null,"abstract":"<p>Facilitative glucose uptake transport systems are ubiquitous in animal cells and are responsible for transporting glucose across cell surface membranes. Evaluation of glucose uptake is crucial in the study of numerous diseases and metabolic disorders such as myocardial ischemia, diabetes mellitus, and cancer. Detailed in this unit are laboratory methods for assessing glucose uptake into mammalian cells. The unit is divided into five sections: (1) a brief overview of glucose uptake assays in cultured cells; (2) a method for measuring glucose uptake using radiolabeled 3-<i>O</i>-methylglucose; (3) a method for measuring glucose uptake using radiolabeled 2-deoxyglucose (2DG); (4) a microplate method for measuring 2DG-uptake using an enzymatic, fluorometric assay; and (5) a microplate-based method using a fluorescent analog of 2DG. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"71 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph1214s71","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50809072","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 119
A Human Induced Pluripotent Stem Cell−Derived Cardiomyocyte (hiPSC-CM) Multielectrode Array Assay for Preclinical Cardiac Electrophysiology Safety Screening 用于临床前心脏电生理安全性筛选的人诱导多能干细胞来源的心肌细胞(hiPSC-CM)多电极阵列检测
Current Protocols in Pharmacology Pub Date : 2015-12-08 DOI: 10.1002/0471141755.ph1118s71
Kate Harris
{"title":"A Human Induced Pluripotent Stem Cell−Derived Cardiomyocyte (hiPSC-CM) Multielectrode Array Assay for Preclinical Cardiac Electrophysiology Safety Screening","authors":"Kate Harris","doi":"10.1002/0471141755.ph1118s71","DOIUrl":"10.1002/0471141755.ph1118s71","url":null,"abstract":"<p>Cardiotoxicity is a leading cause of compound attrition during drug development. Preclinical models used to assess the risk for compound-induced effects on cardiac electrophysiology largely rely on animals that can differ in terms of sensitivity and specificity to the targeted clinical response. There is currently no in vitro human cardiomyocyte model for routine preclinical compound screening, as adult human cardiac tissue is unsuitable for such screening. The commercial availability of human induced pluripotent stem cell−derived cardiomyocytes (hiPSC-CMs) makes possible the development of assays for assessing compound-induced effects on cardiac function in a human cardiomyocyte-like model. Using multielectrode array (MEA) technology with hiPSC-CMs provides a facile screen for compound-induced effects on cardiac electrophysiology. The MEA data generated from hiPSC-CMs correlate well with the results of conventional preclinical assays and clinical findings. Described in this unit is a technique for measuring extracellular field potentials from hiPSC-CMs using MEA technology to screen for compound-induced effects on cardiac electrophysiology. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"71 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph1118s71","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50808981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 12
Using Bioluminescence Resonance Energy Transfer (BRET) to Characterize Agonist-Induced Arrestin Recruitment to Modified and Unmodified G Protein-Coupled Receptors 利用生物发光共振能量转移(BRET)表征激动剂诱导的阻滞蛋白募集到修饰和未修饰的G蛋白偶联受体
Current Protocols in Pharmacology Pub Date : 2015-09-01 DOI: 10.1002/0471141755.ph0214s70
Prashant Donthamsetti, Jose Rafael Quejada, Jonathan A. Javitch, Vsevolod V. Gurevich, Nevin A. Lambert
{"title":"Using Bioluminescence Resonance Energy Transfer (BRET) to Characterize Agonist-Induced Arrestin Recruitment to Modified and Unmodified G Protein-Coupled Receptors","authors":"Prashant Donthamsetti,&nbsp;Jose Rafael Quejada,&nbsp;Jonathan A. Javitch,&nbsp;Vsevolod V. Gurevich,&nbsp;Nevin A. Lambert","doi":"10.1002/0471141755.ph0214s70","DOIUrl":"10.1002/0471141755.ph0214s70","url":null,"abstract":"<p>G protein-coupled receptors (GPCRs) represent ∼25% of current drug targets. Ligand binding to these receptors activates G proteins and arrestins, which are involved in differential signaling pathways. Because functionally selective or biased ligands activate one of these two pathways, they may be superior medications for certain diseases states. The identification of such ligands requires robust drug screening assays for both G protein and arrestin activity. This unit describes protocols for two bioluminescence resonance energy transfer (BRET)-based assays used to monitor arrestin recruitment to GPCRs. One assay requires modification of GPCRs by fusion to a BRET donor or acceptor moiety, whereas the other can detect arrestin recruitment to unmodified GPCRs. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph0214s70","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33971605","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 41
Streptozotocin-Induced Diabetic Models in Mice and Rats 链脲佐菌素诱导的小鼠和大鼠糖尿病模型
Current Protocols in Pharmacology Pub Date : 2015-09-01 DOI: 10.1002/0471141755.ph0547s70
Brian L. Furman
{"title":"Streptozotocin-Induced Diabetic Models in Mice and Rats","authors":"Brian L. Furman","doi":"10.1002/0471141755.ph0547s70","DOIUrl":"10.1002/0471141755.ph0547s70","url":null,"abstract":"<p>Streptozotocin (STZ) is an antibiotic that produces pancreatic islet β-cell destruction and is widely used experimentally to produce a model of type 1 diabetes mellitus (T1DM). Detailed in this unit are protocols for producing STZ-induced insulin deficiency and hyperglycemia in mice and rats. Also described are protocols for creating animal models for type 2 diabetes using STZ. These animals are employed for assessing the pathological consequences of diabetes and for screening potential therapies for the treatment of this condition. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph0547s70","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33971607","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 934
Overview of Genetically Engineered Mouse Models of Breast Cancer Used in Translational Biology and Drug Development 乳腺癌基因工程小鼠模型在转化生物学和药物开发中的应用综述
Current Protocols in Pharmacology Pub Date : 2015-09-01 DOI: 10.1002/0471141755.ph1436s70
Kirsty R. Greenow, Matthew J. Smalley
{"title":"Overview of Genetically Engineered Mouse Models of Breast Cancer Used in Translational Biology and Drug Development","authors":"Kirsty R. Greenow,&nbsp;Matthew J. Smalley","doi":"10.1002/0471141755.ph1436s70","DOIUrl":"10.1002/0471141755.ph1436s70","url":null,"abstract":"<p>Breast cancer is a heterogeneous condition with no single standard of treatment and no definitive method for determining whether a tumor will respond to therapy. The development of murine models that faithfully mimic specific human breast cancer subtypes is critical for the development of patient-specific treatments. While the artificial nature of traditional in vivo xenograft models used to characterize novel anticancer treatments has limited clinical predictive value, the development of genetically engineered mouse models (GEMMs) makes it possible to study the therapeutic responses in an intact microenvironment. GEMMs have proven to be an experimentally tractable platform for evaluating the efficacy of novel therapeutic combinations and for defining the mechanisms of acquired resistance. Described in this overview are several of the more popular breast cancer GEMMs, including details on their value in elucidating the molecular mechanisms of this disorder. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph1436s70","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33971604","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 12
Models of Inflammation: Carrageenan- or Complete Freund's Adjuvant (CFA)–Induced Edema and Hypersensitivity in the Rat 炎症模型:卡拉胶或完全弗氏佐剂(CFA)诱导的大鼠水肿和过敏
Current Protocols in Pharmacology Pub Date : 2015-09-01 DOI: 10.1002/0471141755.ph0504s70
Kenneth E. McCarson
{"title":"Models of Inflammation: Carrageenan- or Complete Freund's Adjuvant (CFA)–Induced Edema and Hypersensitivity in the Rat","authors":"Kenneth E. McCarson","doi":"10.1002/0471141755.ph0504s70","DOIUrl":"10.1002/0471141755.ph0504s70","url":null,"abstract":"<p>Animal models of inflammation are used to assess the production of inflammatory mediators at sites of inflammation, the processing of pain sensation at CNS sites, the anti-inflammatory properties of agents such as nonsteroidal anti-inflammatory drugs (NSAIDs), and the efficacy of putative analgesic compounds in reversing cutaneous hypersensitivity. Detailed in this unit are methods to elicit and measure carrageenan- and complete Freund's adjuvant (CFA)–induced cutaneous inflammation. Due to possible differences between the dorsal root sensory system and the trigeminal sensory system, injections into either the footpad or vibrissal pad are described. In this manner, cutaneous inflammation can be assessed in tissue innervated by the lumbar dorsal root ganglion neurons (footpad) or by the trigeminal ganglion neurons (vibrissal pad). © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph0504s70","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33971606","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 41
Overview of KRAS-Driven Genetically Engineered Mouse Models of Non-Small Cell Lung Cancer kras驱动的非小细胞肺癌基因工程小鼠模型综述
Current Protocols in Pharmacology Pub Date : 2015-09-01 DOI: 10.1002/0471141755.ph1435s70
Clare Sheridan, Julian Downward
{"title":"Overview of KRAS-Driven Genetically Engineered Mouse Models of Non-Small Cell Lung Cancer","authors":"Clare Sheridan,&nbsp;Julian Downward","doi":"10.1002/0471141755.ph1435s70","DOIUrl":"10.1002/0471141755.ph1435s70","url":null,"abstract":"<p>KRAS, the most frequently mutated oncogene in non-small cell lung cancer, has been utilized extensively to model human lung adenocarcinomas. The results from such studies have enhanced considerably an understanding of the relationship between KRAS and the development of lung cancer. Detailed in this overview are the features of various KRAS-driven genetically engineered mouse models (GEMMs) of non-small cell lung cancer, their utilization, and the potential of these models for the study of lung cancer biology. © 2015 by John Wiley &amp; Sons, Inc.</p>","PeriodicalId":10871,"journal":{"name":"Current Protocols in Pharmacology","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/0471141755.ph1435s70","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33969550","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 10
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