产品编号 A105809 | CAS号 103-90-2 | Aladdin
货号 规格 库存 价格 数量
A105809-250mg 分析标准品,≥99.5% 上海(>10)


敏感性 对光敏感
熔点 168-172°C


产品介绍 水中溶解度: 14 g/l (20°C) 溶于乙醇、丙酮、甲醇、DMF, 二氯乙烷和乙酸乙酯,实际上不溶于石油醚、戊烷和苯。
别名 4'-羟基乙酰苯胺;N-乙酰对氨基酚;对羟基乙酰苯胺;对羟基苯基乙酰胺;N-(4-羟基苯基)乙酰胺;4-乙酰胺基苯酚;醋氨酚;4-乙酰氨基酚;对乙酰氨基酚;扑热息痛;APAP ;Acetaminophen; APAP; Paracetamol; p-Hydroxyacetanilide;
应用 有机合成中间体,过氧化氢的稳定剂,照相化学药品,非抗炎解热镇痛药。
只有注册的用户才可以写评论。请 登录 创建帐户
标识符号 GHS07 GHS07
信号词 Warning
风险声明 (欧洲) R22;R36/38;R52/53
安全声明(欧洲) S26;S37/39;S61
警示性声明 P261,P305+P351+P338
危害码(欧洲) Xn
危害声明 H302,H315,H319,H335
个人防护设备 dust mask type N95 (US),Eyeshields,Gloves
RTECS AE4200000
WGK德国 1
Merck Index 47
A Guerra, N E Campillo, J A Páez
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with...Read More
Takeki Uehara, Atsushi Ono, Toshiyuki Maruyama, Ikuo Kato, Hiroshi Yamada, Yasuo Ohno, Tetsuro Urushidani
Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted appr...Read More
Alan A Talevi, Mohammad M Goodarzi, Erlinda V EV Ortiz, Pablo R PR Duchowicz, Carolina L CL Bellera, Guido G Pesce, Eduardo A EA Castro, Luis E LE Bruno-Blanch
In order to minimize the high attrition rate that usually characterizes drug research and development projects, current medicinal chemists aim to characterize both pharmacological and ADME profiles at...Read More
Bram B Baert, Eric E Deconinck, Mireille M Van Gele, Marian M Slodicka, Paul P Stoppie, Samuel S Bodé, Guido G Slegers, Yvan Y Vander Heyden, Jo J Lambert, Johan J Beetens, Bart B De Spiegeleer
Transdermal penetration was studied as a function of selected descriptors in QSPR using CART, boosted CART and MLR models....Read More
Alessio Innocenti, Mika Hilvo, Andrea Scozzafava, Seppo Parkkila, Claudiu T Supuran
We're sorry this abstract is currently not available....Read More
Alessio Innocenti, Daniela Vullo, Andrea Scozzafava, Claudiu T Supuran
Inhibition of 12 mammalian isoforms of the metalloenzyme carbonic anhydrase (CA, EC, CA I-XIV, with a series of phenols was investigated. The inhibition profile by phenols of these CAs was di...Read More
Tony K L TK Kiang, Mary H H MH Ensom, Thomas K H TK Chang
UDP-glucuronosyltransferase (UGT) enzymes catalyze the conjugation of various endogenous substances (e.g., bilirubin) and exogenous compounds (e.g., drugs). The human UGT superfamily is comprised of 2...Read More
Kevin Guo, Liang Li
We report a new quantitative metabolome profiling technique based on differential (12)C-/(13)C-isotope dansylation labeling of metabolites, fast liquid chromatography (LC) separation and electrospray ...Read More
R Scott RS Obach, Franco F Lombardo, Nigel J NJ Waters
We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic ...Read More
Manthena V S Varma, Bo Feng, R Scott Obach, Matthew D Troutman, Jonathan Chupka, Howard R Miller, Ayman El-Kattan
Kidney plays an important role in the elimination of drugs, especially with low or negligible hepatic clearance. An analysis of the interrelation of physicochemical properties and the human renal clea...Read More
Manthena V S MV Varma, R Scott RS Obach, Charles C Rotter, Howard R HR Miller, George G Chang, Stefanus J SJ Steyn, Ayman A El-Kattan, Matthew D MD Troutman
Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh). In this study, using a database comprised ...Read More
S Ekins, A J Williams, J J Xu
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...Read More
Francesco F Epifano, Salvatore S Genovese, Silvio S Sosa, Aurelia A Tubaro, Massimo M Curini
The synthesis of ester derivatives of the title acid and their anti-inflammatory activity are reported....Read More
Francisco J Prado-Prado, Xerardo García-Mera, Humberto González-Díaz
There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one pa...Read More
Masaaki Fujikawa, Kazuya Nakao, Ryo Shimizu, Miki Akamatsu
To investigate PAMPA permeability of hydrophobic compounds, we experimentally measured the P"a"p"p"-"p"a"m"p"a of compounds with high hydrophobicity, inclu...Read More
Nigel N Greene, Lilia L Fisk, Russell T RT Naven, Reine R RR Note, Mukesh L ML Patel, Dennis J DJ Pelletier
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...Read More
Naomi L NL Kruhlak, Sydney S SS Choi, Joseph F JF Contrera, James L JL Weaver, James M JM Willard, Kenneth L KL Hastings, Lawrence F LF Sancilio
ABSTRACT Drug-induced phospholipidosis (PL) is a condition characterized by the accumulation of phospholipids and drug in lysosomes, and is found in a variety of tissue types. PL is frequently manifes...Read More
Bo Ahrén, Maria S?rhede Winzell
Exogenous administration of islet amyloid polypeptide (IAPP) has been shown to inhibit both insulin and glucagon secretion. This study examined alpha-cell function in mice with beta-cell specific over...Read More
Atsushi Kambe, Hiroki Yoshioka, Hideki Kamitani, Takashi Watanabe, Seung Joon Baek, Thomas E Eling
EP4 expression in human glioblastoma cells correlates with growth on soft agar. The cyclooxygenase inhibitor sulindac sulfide first altered specificity protein-1 (Sp-1) and early growth response gene-...Read More
Bridget M Kuehn
We're sorry this abstract is currently not available....Read More
Janice Pettie, Margaret Dow
Paracetamol is a low cost, effective analgesic that is widely available in the UK. Paracetamol is the drug most commonly taken in overdose and can lead to acute liver failure, which can be fatal. This...Read More
V Rao Kadam, R M Van Wijk, J I Moran, D Miller
Transversus abdominis plane block is an effective postoperative analgesic technique after abdominal surgery, but no study has compared continuous transversus abdominis plane block with continuous epid...Read More
Randall Y Kam
We're sorry this abstract is currently not available....Read More
Robert Weinkove, Jennifer Clay, Catherine Wood
To assess the attitudes of clinicians to temperature management in haematology patients with febrile neutropenia.An online scenario-based survey was circulated to consultant members of the New Zealand...Read More
Sathees Waran Thayapararajah, Irene Gulka, Ahmed Al-Amri, Sujut Das, G Bryan Young
Acute fulminant hepatic failure (AFHF) is common in tertiary care centres with transplant facilities. Cerebral edema frequently threatens the lives of such patients. We reviewed our cases of AFHF, not...Read More
Nabil A Khan, Maria A Sullivan, Michael G Vitale, Mary Ellen Tresgallo, John M Saroyan
Addiction to painkillers or other substances in pediatric and adolescent cases of noncancer chronic pain is an understudied phenomenon, even amidst documented increases in rates of prescription opioid...Read More
Ying-Jen Jeffrey Wu, Alexander J Neuwelt, Leslie L Muldoon, Edward A Neuwelt
Ovarian cancer is commonly treated with cisplatin/paclitaxel but many tumors become resistant. Acetaminophen reduced glutathione and enhanced chemotherapy efficacy in hepatic cancer treatment. The obj...Read More
Aarti Singla, Paul Sloan
Hydrocodone/acetaminophen is not only the most commonly prescribed opioid in the United States but also the most common prescription medication written in America. Although original and early trials c...Read More
Lars E Schmidt
N-acetylcysteine (NAC) is acknowledged as an effective antidote for paracetamol overdose. However, adverse effects to NAC are common and may be a point of concern for the patient and the treating phys...Read More
Roselyn Jan W Clemente-Fuentes, Heather Pickett, Misty Carney
Acetaminophen is safe for use in pregnancy but lacks evidence of efficacy....Read More
R P Olonisakin, S D Amanor-Boadu, A O Akinyemi
The study evaluated the morphine sparing effect of intravenous Paracetamol and the incidence of side effects in the recovery room following lower abdominal gynaecological surgery.Fifty six, ASA I and ...Read More
Sung Han Kang, Young-Ho Jung, Hyung Young Kim, Ju-Hee Seo, Jung-Yong Lee, Ji-Won Kwon, Byoung-Ju Kim, Hyo Bin Kim, So Yeon Lee, Gwang Cheon Jang, Dae Jin Song, Woo-Kyung Kim, Jung Yeon Shim, Jae-Hee Kim, Mi-Jin Kang, Ho-Sung Yu, Jinho Yu, Soo-Jong Hong
Recent studies have identified an increase in the prevalence of asthma associated with paracetamol use.To identify the relationship among asthma, biomarkers, genes, and paracetamol use in preschool ch...Read More
Karel Allegaert, Brian Anderson, Sinno Simons, Bart van Overmeire
There remains a need for alternative medical treatments for patent ductus arteriosus (PDA) closure in extreme preterm neonates because of therapeutic failure and adverse effects associated with non-se...Read More
Mitchell R McGill, Margitta Lebofsky, Hye-Ryun K Norris, Matthew H Slawson, Mary Lynn Bajt, Yuchao Xie, C David Williams, Diana G Wilkins, Douglas E Rollins, Hartmut Jaeschke
At therapeutic doses, acetaminophen (APAP) is a safe and effective analgesic. However, overdose of APAP is the principal cause of acute liver failure in the West. Binding of the reactive metabolite of...Read More
Alexandre R R Péry, Céline Brochot, Florence A Zeman, Enrico Mombelli, Sophie Desmots, Manuela Pavan, Elena Fioravanzo, José-Manuel Zaldívar
In the present legislations, the use of methods alternative to animal testing is explicitly encouraged, to use animal testing only 'as a last resort' or to ban it. The use of alternative met...Read More
Olivier Lasnier, Christian El-Hadad, Rosanne Superstein
We're sorry this abstract is currently not available....Read More
H K Ruben Thanacoody, Alasdair Gray, James W Dear, Judy Coyle, Euan A Sandilands, David J Webb, Steff Lewis, Michael Eddleston, Simon Hl Thomas, D Nicholas Bateman
Paracetamol (acetaminophen) poisoning remains the commonest cause of acute liver injury in Europe and North America. The intravenous (IV) N-acetylcysteine (NAC) regimen introduced in the 1970s has con...Read More
Marta Krasny, Ma?gorzata Zadurska, Grzegorz Cessak, Piotr Fiedor
In view of high availability and diversity of non-steroidal anti-inflammatory drugs (NSAIDs) on Polish market it is important for orthodontists to be aware of NSAID effect on the range of orthodontic ...Read More
Usama W Hawas, Ghadir M Soliman, Lamia T Abou El-Kassem, Abdel Razik H Farrag, Khaled Mahmoud, Francisco León
A new flavonoid C-glycoside, kaempferol 8-C-beta-galactoside, along with twelve known glycosidic flavonoids was isolated from the aqueous methanolic extract of Solanum elaeagnifolium Cav. (Solanaceae)...Read More
Carlos Sanz-Garcia, Gemma Ferrer-Mayorga, Agueda González-Rodríguez, Angela M Valverde, Antonio Martín-Duce, Juan P Velasco-Martín, Javier Regadera, Margarita Fernández, Susana Alemany
Cot/tpl2 (MAP3K8) activates MKK1/2-Erk1/2 following stimulation of the Toll-like/IL-1 receptor superfamily. Here, we investigated the role of Cot/tpl2 in sterile inflammation and drug-induced liver to...Read More
Eve C A Morgenstern, Konrad Heintze
We're sorry this abstract is currently not available....Read More
Manoj K Saxena, Colman B Taylor, Naomi E Hammond, Paul J Young, Ian M Seppelt, Parisa Glass, John A Myburgh, John A Myburgh, John A Myburgh
Given the scientific uncertainty of the efficacy and safety of normothermia (36.0°C to 37.5°C) on disability and death after acute neurological lesions, we sought to understand how temperature is ma...Read More
Charles R Meyer
We're sorry this abstract is currently not available....Read More
Amel Chaabane, Nadia Ben Fredj, Zohra Chadly, Naceur A Boughattas, Karim Aouam
We're sorry this abstract is currently not available....Read More
Marine Auffret, Johana Béné, Marie Lachatre, Marc Lambert, Sophie Gautier
We're sorry this abstract is currently not available....Read More
J Loader, T Brooks
We're sorry this abstract is currently not available....Read More
Lihai Zhang, Terrence Gavin, Brian C Geohagen, Qiang Liu, Katherine J Downey, Richard M Lopachin
Our previous research showed that enolates formed from 1,3-dicarbonyl compounds, such as 2-acetylcyclopentanone (2-ACP), could provide protection in cell culture models from electrophile- or oxidative...Read More
Yuchen Sheng, Qingning Liang, Zhongping Deng, Lili Ji, Zhengtao Wang
Acetaminophen (AP) is widely used as the antipyretic and analgesic drug in clinic, and it can induce serious liver injury in the case of excessive abuse. The present study showed that AP (400 mg/kg) i...Read More
M M Lifshitz, O O Weinstein, V V Gavrilov, G G Rosenthal, T T Lifshitz
This study was designed to measure acetaminophen (paracetamol) levels in tears, and to compare it to serum levels. Paracetamol levels were measured in 20 paired tears and serum samples from 10 healthy...Read More
Kenneth L KL Muldrew, Laura P LP James, Leslie L Coop, Sandra S SS McCullough, Howard P HP Hendrickson, Jack A JA Hinson, Philip R PR Mayeux
Acetaminophen-induced hepatotoxicity has been attributed to covalent binding of the reactive metabolite N-acetyl-p-benzoquinone imine to cysteine groups on proteins as an acetaminophen-cysteine conjug...Read More
R R Vanbinst, J J Koenig, V V Di Fazio, A A Hassoun
Bile is, in certain cases, collected together with blood from different sites (heart, brain, femoral), urine and other organs or matrices. This study reports comparative results obtained from the anal...Read More
Peggy Gandia, Marie-Pierre Bareille, Sylvie Saivin, Anne Pavy Le-Traon, Michel Lavit, Antonio Guell, Georges Houin
This study evaluated the effect of simulated weightlessness on gastric emptying, using acetaminophen as a probe and -6 degrees head-down bed rest to simulate zero gravity. Eighteen volunteers were giv...Read More
J Barden, J Edwards, A Moore, H McQuay
Paracetamol (acetaminophen) and non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for the relief of mild and moderate pain arising from headache, musculoskeletal conditions and dysmenorrh...Read More
Edward E Munsterhjelm, Nina M NM Munsterhjelm, Tomi T TT Niemi, Olavi O Ylikorkala, Pertti J PJ Neuvonen, Per H PH Rosenberg
Acetaminophen (paracetamol) is widely used for postoperative analgesia. Its mechanism of action is inhibition of prostaglandin synthesis in the central nervous system, and acetaminophen is traditional...Read More
Hartmut H Jaeschke
Acetaminophen (AAP) overdose and the resulting hepatotoxicity is an important clinical problem. In addition, AAP is widely used as a prototype hepatotoxin to study mechanisms of chemical-induced cell ...Read More
A A Kunkel, H H W?tzig
A number of pharmaceuticals (e.g., acetaminophen, salicylic acid, sulfamethoxazole, theophylline, tolbutamide and trimethoprim) have been determined in human plasma by micellar electrokinetic chromato...Read More
Mahmoud M Mohammadi, Mohammad R MR Mohebbi, Fariba F Naderi
The present study was done to explore the relationship between the cerebrospinal fluid (CSF) glucose concentration, body temperature, seizure duration, and acetaminophen administration. Retrospective ...Read More
J C JC Griener, M E ME Msall, R E RE Cooke, G B GB Corcoran
In this study we evaluated subjects with Down's syndrome for the possibility that direct or indirect gene dosage effects of trisomy 21 alter the fate of acetaminophen. We also investigated the us...Read More
J R JR Bales, J K JK Nicholson, P J PJ Sadler
Two-dimensional proton-proton correlated NMR spectra of concentrated urine from a subject who had ingested a 1-g dose of acetaminophen are reported. These "maps" provide a considerable simpl...Read More
J R JR Bales, P J PJ Sadler, J K JK Nicholson, J A JA Timbrell
Acetaminophen and its glucuronide, sulfate, N-acetyl-L-cysteinyl, and L-cysteinyl metabolites can be rapidly detected by 1H NMR spectroscopy of intact, untreated human urine. Study of the time course ...Read More
N N Watari, M M Iwai, N N Kaneniwa
Pharmacokinetic studies of the fate of acetaminophen and its major metabolites, acetaminophen sulfate (AS) and acetaminophen glucuronide (AG), were made in rats. The rates of conjugate formation were ...Read More
A J AJ Quattrone, R S RS Putnam
Simultaneous and semi-automated determinations of theophylline, acetaminophen, and ethosuximide from human serum are possible through use of a programmable autoinjector, an isocratic mobile phase, and...Read More
J W JW Findlay, R L RL DeAngelis, M F MF Kearney, R M RM Welch, J M JM Findlay
The disposition of salicylic acid, phenacetin, caffeine, and codeine, and two metabolites, acetaminophen and morphine, was studied in breast milk and plasma of two lactating mothers after single oral ...Read More
Z Z Smilgin, M M Dro?dzik, B B Gawrońska-Szklarz, J J Wójcicki, S S Tustanowski, W W Górnik
The aim of this study was to evaluate the health state of a random group of subjects occupationally exposed to polyvinyl chloride. The emphasis was put on the hepatic functional tests in comparison wi...Read More
S M SM de Morais, J P JP Uetrecht, P G PG Wells
Gilbert's syndrome occurs in 5%-7% of the human population and is caused by an inherited deficiency in the glucuronidation of endogenous bilirubin, resulting in its accumulation and jaundice. The...Read More
Garry G GG Graham, Kieran F KF Scott, Richard O RO Day
The excellent tolerability of therapeutic doses of paracetamol (acetaminophen) is a major factor in the very wide use of the drug. The major problem in the use of paracetamol is its hepatotoxicity aft...Read More
Susruta S Majumdar, Kenneth B KB Sloan
The ability of N-alkyl-N-alkyloxycarbonylaminomethyl promoiety to act as soft alkylating agent and its influence in increasing membrane permeation for phenols, imides and thiols have been probed....Read More
Anthony L AL Vaccarino, Dennis D Paul, Pranab K PK Mukherjee, Elena B EB Rodríguez de Turco, Victor L VL Marcheselli, Liang L Xu, Mark L ML Trudell, J M JM Minguez, M P MP Matía, Carlos C Sunkel, Julio J Alvarez-Builla, Nicolas G NG Bazan
We're sorry this abstract is currently not available....Read More
Tiago L Moda, Carlos A Montanari, Adriano D Andricopulo
We're sorry this abstract is currently not available....Read More
Dennis J Pelletier, Daniel Gehlhaar, Anne Tilloy-Ellul, Theodore O Johnson, Nigel Greene
The identification of phospholipidosis (PPL) during preclinical testing in animals is a recognized problem in the pharmaceutical industry. Depending on the intended indication and dosing regimen, PPL ...Read More
Wolfgang W Friebolin, Beate B Jannack, Nicole N Wenzel, Julien J Furrer, Thomas T Oeser, Cecilia P CP Sanchez, Michael M Lanzer, Vanessa V Yardley, Katja K Becker, Elisabeth E Davioud-Charvet
Plasmodium parasites are exposed to higher fluxes of reactive oxygen species and need high activities of intracellular antioxidant systems providing a steady glutathione flux. As a future generation o...Read More
Muhammad M Alimuddin, Daniel D Grant, Daryl D Bulloch, Noelle N Lee, Martin M Peacock, Russell R Dahl
A method for log D (pH 7.4) measurement was developed using microfluidic liquid-liquid extraction. Values were determined for 26 compounds and compared to results obtained via shake-flask methods. Exc...Read More
Gustav G Ahlin, Johan J Karlsson, Jenny M JM Pedersen, Lena L Gustavsson, Rolf R Larsson, P?r P Matsson, Ulf U Norinder, Christel A S CA Bergstr?m, Per P Artursson
The liver-specific organic cation transport protein (OCT1; SLC22A1) transports several cationic drugs including the antidiabetic drug metformin and the anticancer agents oxaliplatin and imatinib. In t...Read More
Christian Sinning, Bernhard Watzer, Ovidiu Coste, Rolf M Nüsing, Ingo Ott, Alessia Ligresti, Vincenzo Di Marzo, Peter Imming
N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide (AM404) is a metabolite of the well-known analgesic paracetamol. AM404 inhibits endocannabinoid cellular uptake, binds weakly to CB1 an...Read More
Mojca M Brunskole, Bogdan B Stefane, Karmen K Zorko, Marko M Anderluh, Jure J Stojan, Tea T Lanisnik Rizner, Stanislav S Gobec
A series of compounds were screened on trihydroxynaphthalene reductase from Curvularia lunata, a known plant pathogen and an opportunistic human pathogen, and several structurally diverse hits were ob...Read More
Lorena dos Santos, Luíse Azevedo Lima, Valdir Cechinel-Filho, Rogério Corrêa, Fátima de Campos Buzzi, Ricardo José Nunes
New 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives have been synthesized and tested for their anti-nociceptive activity in different models of pain and compared to some...Read More
Arthur E Kümmerle, Marina M Vieira, Martine Schmitt, Ana LP Miranda, Carlos AM Fraga, Jean-Jacques Bourguignon, Eliezer J Barreiro
A set of six azaheterocycles were designed as conformationnaly-constrained N-acylhydrazones and tested as analgesics....Read More
Amal AM Eissa, Nahla AH Farag, Gamal AH Soliman
8-Acetyl-7-hydroxy-4-phenyl-2H-benzopyran-2-one as starting material a number of 8-substituted derivatives (i.e., hydrazones 2a,b, imine 2c, chalcones 3, pyrazoles 4, 3-cyano-2-oxo-dihydropyridines 5,...Read More
Haiyan Li, Jin Sun, Xiaofan Sui, Jianfang Liu, Zhongtian Yan, Xiaohong Liu, Yinghua Sun, Zhonggui He
The first-principle, quantitative structure-hepatic clearance relationship for 50 drugs was constructed based on selected molecular descriptors calculated by TSAR software. The R^2 of the predicted an...Read More
E Philip Jesudason, S K Sridhar, E J Padma Malar, P Shanmugapandiyan, Mohammed Inayathullah, V Arul, D Selvaraj, R Jayakumar
A novel series of N-Mannich bases of benzimidazole derivatives were synthesized and characterized by ^1H NMR, IR spectral studies and elemental analysis. The compounds were screened for analgesic and ...Read More
Maria Let?-cia de Castro Barbosa, Gabriela Muniz de Albuquerque Melo, Yolanda Karla Cupertino da Silva, Raquel de Oliveira Lopes, Everton Ten?3rio de Souza, Aline Cavalcanti de Queiroz, Salete Smaniotto, Magna Suzana Alexandre-Moreira, Eliezer J Barreiro,
In this paper we report the design, synthesis and pharmacological evaluation of a series of N-phenyl-acetamide sulfonamide derivatives (5a-g), planned by structural modification on the prototype parac...Read More
Elena Dreassi, Alessandra Tania Zizzari, Federico Falchi, Silvia Schenone, Annalisa Santucci, Giovanni Maga, Maurizio Botta
A library of 23 pyrazolo-pyrimidine compounds Src tyrosine kinase (TK) inhibitors, that reduced proliferation of a human osteogenic sarcoma cell line, was taken to investigate lack of correlation betw...Read More
Xiaofan Sui, Jin Sun, Haiyan Li, Yongjun Wang, Jianfang Liu, Xiaohong Liu, Wenping Zhang, Lijiang Chen, Zhonggui He
We developed an improved Lombardeo's method (J. Med. Chem., 2004) for prediction of VD"s"s in human. With ElogD substituted by logk"I"A"M, together with f"i" &#...Read More
Valentina V Onnis, Cenzo C Congiu, Emmelie E Bj?rklund, Franziska F Hempel, Emma E S?derstr?m, Christopher J CJ Fowler
Fatty acid amide hydrolase (FAAH) is the key hydrolytic enzyme for the endogenous cannabinoid receptor ligand anandamide. The synthesis and evaluation for their FAAH inhibitory activities of a series ...Read More
Padraick J Dornbush, Cynric Cho, Elizabeth S Chang, Lu Xu, Wade A Russu, Lisa A Wrischnik, Kirkwood M Land
Trichomonas vaginalis, a human-infectious protozoan, can display resistance to treatment by metronidazole. A library of 3,4-dichloroaniline amides based on propanil, an herbicide, has been synthesized...Read More
Huaping H Mo, Kathryn M KM Balko, David A DA Colby
A simple and rapid NMR method is described to determine the logP of pharmaceutical agents. This method is highly versatile and efficient, because it does not require the use of deuterated solvents or ...Read More
Martha C Rosales-Hernández, Jessica E Mendieta-Wejebe, José G Trujillo-Ferrara, José Correa-Basurto
Since many drugs are metabolized by cytochrome P450 (CYP450), biotransformation studies using these enzymes are valuable in drug development. In this work, the biotransformation by CYP1A1 and CYP2B1 o...Read More
H Devarajan-Ketha, KB Sloan
N,N'-Dialkylaminoalkylcarbonyl (DAAC) and aminoalkylcarbonyl (AAC) prodrugs of phenolic drugs acetaminophen (APAP) and naltrexone (NTX) are reported. The effects of incorporation of a basic amine...Read More
Rafael Gozalbes, Mary Jacewicz, Robert Annand, Katya Tsaioun, Antonio Pineda-Lucena
A QSAR model was developed for predicting intestinal drug permeability, one of the most important parameters when evaluating compounds in drug discovery projects. First, a set of relevant properties f...Read More
Chun-Wa CW Chung, Anthony W AW Dean, James M JM Woolven, Paul P Bamborough
Bromodomain-containing proteins are key epigenetic regulators of gene transcription and readers of the histone code. However, the therapeutic benefits of modulating this target class are largely unexp...Read More
Miaozong Wu, Anjaiah Katta, Murali K Gadde, Hua Liu, Sunil K Kakarla, Jacqueline Fannin, Satyanarayana Paturi, Ravi K Arvapalli, Kevin M Rice, Yeling Wang, Eric R Blough, Jose Vina
Aged skeletal muscle is characterized by an increased incidence of metabolic and functional disorders, which if allowed to proceed unchecked can lead to increased morbidity and mortality. The mechanis...Read More
Zhichao Liu, Qiang Shi, Don Ding, Reagan Kelly, Hong Fang, Weida Tong
Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...Read More
Cynthia D CD Selassie, Sanjay S Kapur, Rajeshwar P RP Verma, Melissa M Rosario
In this comprehensive study on the caspase-mediated apoptosis-inducing effect of 51 substituted phenols in a murine leukemia cell line (L1210), we determined the concentrations needed to induce caspas...Read More
Denis Fourches, Julie C Barnes, Nicola C Day, Paul Bradley, Jane Z Reed, Alexander Tropsha
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...Read More
Peter J McNamara, Rae Ellen Syverson, Kathy Milligan-Myhre, Olga Frolova, Sarah Schroeder, Joshua Kidder, Thanh Hoang, Richard A Proctor
Menstrual toxic shock syndrome is a rare but potentially life-threatening illness manifest through the actions of Staphylococcus aureus toxic shock syndrome toxin 1 (TSST-1). Previous studies have sho...Read More
Nikolaos Psychogios, David D Hau, Jun Peng, An Chi Guo, Rupasri Mandal, Souhaila Bouatra, Igor Sinelnikov, Ramanarayan Krishnamurthy, Roman Eisner, Bijaya Gautam, Nelson Young, Jianguo Xia, Craig Knox, Edison Dong, Paul Huang, Zsuzsanna Hollander, Theresa
Continuing improvements in analytical technology along with an increased interest in performing comprehensive, quantitative metabolic profiling, is leading to increased interest pressures within the m...Read More
David S DS Wishart, Michael J MJ Lewis, Joshua A JA Morrissey, Mitchel D MD Flegel, Kevin K Jeroncic, Yeping Y Xiong, Dean D Cheng, Roman R Eisner, Bijaya B Gautam, Dan D Tzur, Summit S Sawhney, Fiona F Bamforth, Russ R Greiner, Liang L Li
With continuing improvements in analytical technology and an increased interest in comprehensive metabolic profiling of biofluids and tissues, there is a growing need to develop comprehensive referenc...Read More