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Specifications of Approved Drug Compound Library
Annexure-I : Specifications of Approved drug compound library The compounds should be structurally diverse, medicinally active, and cell permeable Compounds should have rich documentation with structure, Target, Activity and IC50 should be known Compounds which are supplied should have been validated by NMR and HPLC to ensure high purity Each compound should be supplied as 10mM solution in DMSO and at least 100µl of each compound should be supplied. Compounds should be supplied in screw capped vial arranged as 96 well plate format. -
Classification of Medicinal Drugs and Driving: Co-Ordination and Synthesis Report
Project No. TREN-05-FP6TR-S07.61320-518404-DRUID DRUID Driving under the Influence of Drugs, Alcohol and Medicines Integrated Project 1.6. Sustainable Development, Global Change and Ecosystem 1.6.2: Sustainable Surface Transport 6th Framework Programme Deliverable 4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Due date of deliverable: 21.07.2011 Actual submission date: 21.07.2011 Revision date: 21.07.2011 Start date of project: 15.10.2006 Duration: 48 months Organisation name of lead contractor for this deliverable: UVA Revision 0.0 Project co-funded by the European Commission within the Sixth Framework Programme (2002-2006) Dissemination Level PU Public PP Restricted to other programme participants (including the Commission x Services) RE Restricted to a group specified by the consortium (including the Commission Services) CO Confidential, only for members of the consortium (including the Commission Services) DRUID 6th Framework Programme Deliverable D.4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Page 1 of 243 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Authors Trinidad Gómez-Talegón, Inmaculada Fierro, M. Carmen Del Río, F. Javier Álvarez (UVa, University of Valladolid, Spain) Partners - Silvia Ravera, Susana Monteiro, Han de Gier (RUGPha, University of Groningen, the Netherlands) - Gertrude Van der Linden, Sara-Ann Legrand, Kristof Pil, Alain Verstraete (UGent, Ghent University, Belgium) - Michel Mallaret, Charles Mercier-Guyon, Isabelle Mercier-Guyon (UGren, University of Grenoble, Centre Regional de Pharmacovigilance, France) - Katerina Touliou (CERT-HIT, Centre for Research and Technology Hellas, Greece) - Michael Hei βing (BASt, Bundesanstalt für Straßenwesen, Germany). -
Rediscovery of Fexinidazole
New Drugs against Trypanosomatid Parasites: Rediscovery of Fexinidazole INAUGURALDISSERTATION zur Erlangung der Würde eines Doktors der Philosophie vorgelegt der Philosophisch-Naturwissenschaftlichen Fakultät der Universität Basel von Marcel Kaiser aus Obermumpf, Aargau Basel, 2014 Originaldokument gespeichert auf dem Dokumentenserver der Universität Basel edoc.unibas.ch Dieses Werk ist unter dem Vertrag „Creative Commons Namensnennung-Keine kommerzielle Nutzung-Keine Bearbeitung 3.0 Schweiz“ (CC BY-NC-ND 3.0 CH) lizenziert. Die vollständige Lizenz kann unter creativecommons.org/licenses/by-nc-nd/3.0/ch/ eingesehen werden. 1 Genehmigt von der Philosophisch-Naturwissenschaftlichen Fakultät der Universität Basel auf Antrag von Prof. Reto Brun, Prof. Simon Croft Basel, den 10. Dezember 2013 Prof. Dr. Jörg Schibler, Dekan 2 3 Table of Contents Acknowledgement .............................................................................................. 5 Summary ............................................................................................................ 6 Zusammenfassung .............................................................................................. 8 CHAPTER 1: General introduction ................................................................. 10 CHAPTER 2: Fexinidazole - A New Oral Nitroimidazole Drug Candidate Entering Clinical Development for the Treatment of Sleeping Sickness ........ 26 CHAPTER 3: Anti-trypanosomal activity of Fexinidazole – A New Oral Nitroimidazole Drug Candidate for the Treatment -
NINDS Custom Collection II
ACACETIN ACEBUTOLOL HYDROCHLORIDE ACECLIDINE HYDROCHLORIDE ACEMETACIN ACETAMINOPHEN ACETAMINOSALOL ACETANILIDE ACETARSOL ACETAZOLAMIDE ACETOHYDROXAMIC ACID ACETRIAZOIC ACID ACETYL TYROSINE ETHYL ESTER ACETYLCARNITINE ACETYLCHOLINE ACETYLCYSTEINE ACETYLGLUCOSAMINE ACETYLGLUTAMIC ACID ACETYL-L-LEUCINE ACETYLPHENYLALANINE ACETYLSEROTONIN ACETYLTRYPTOPHAN ACEXAMIC ACID ACIVICIN ACLACINOMYCIN A1 ACONITINE ACRIFLAVINIUM HYDROCHLORIDE ACRISORCIN ACTINONIN ACYCLOVIR ADENOSINE PHOSPHATE ADENOSINE ADRENALINE BITARTRATE AESCULIN AJMALINE AKLAVINE HYDROCHLORIDE ALANYL-dl-LEUCINE ALANYL-dl-PHENYLALANINE ALAPROCLATE ALBENDAZOLE ALBUTEROL ALEXIDINE HYDROCHLORIDE ALLANTOIN ALLOPURINOL ALMOTRIPTAN ALOIN ALPRENOLOL ALTRETAMINE ALVERINE CITRATE AMANTADINE HYDROCHLORIDE AMBROXOL HYDROCHLORIDE AMCINONIDE AMIKACIN SULFATE AMILORIDE HYDROCHLORIDE 3-AMINOBENZAMIDE gamma-AMINOBUTYRIC ACID AMINOCAPROIC ACID N- (2-AMINOETHYL)-4-CHLOROBENZAMIDE (RO-16-6491) AMINOGLUTETHIMIDE AMINOHIPPURIC ACID AMINOHYDROXYBUTYRIC ACID AMINOLEVULINIC ACID HYDROCHLORIDE AMINOPHENAZONE 3-AMINOPROPANESULPHONIC ACID AMINOPYRIDINE 9-AMINO-1,2,3,4-TETRAHYDROACRIDINE HYDROCHLORIDE AMINOTHIAZOLE AMIODARONE HYDROCHLORIDE AMIPRILOSE AMITRIPTYLINE HYDROCHLORIDE AMLODIPINE BESYLATE AMODIAQUINE DIHYDROCHLORIDE AMOXEPINE AMOXICILLIN AMPICILLIN SODIUM AMPROLIUM AMRINONE AMYGDALIN ANABASAMINE HYDROCHLORIDE ANABASINE HYDROCHLORIDE ANCITABINE HYDROCHLORIDE ANDROSTERONE SODIUM SULFATE ANIRACETAM ANISINDIONE ANISODAMINE ANISOMYCIN ANTAZOLINE PHOSPHATE ANTHRALIN ANTIMYCIN A (A1 shown) ANTIPYRINE APHYLLIC -
Designing Inhibitors Via Molecular Modelling Methods for Monoamine Oxidase Isozymes a and B Filiz Varnali Kadir Has Universit
DESIGNING INHIBITORS VIA MOLECULAR MODELLING METHODS FOR MONOAMINE OXIDASE ISOZYMES A AND B FİLİZ VARNALI KADİR HAS UNIVERSITY 2012 DESIGNING INHIBITORS VIA MOLECULAR MODELLING METHODS FOR MONOAMINE OXIDASE ISOZYMES A AND B FİLİZ VARNALI M.S. in Computational Biology and Bioinformatics, Kadir Has University, 2012 Submitted to the Graduate School of Science and Engineering in partial fulfilment of the requirements for the degree of Master of Science in Computational Biology and Bioinformatics KADİR HAS UNIVERSITY 2012 DESIGNING INHIBITORS VIA MOLECULAR MODELING METHODS FOR MONOAMINE OXIDASE ISOZYMES A AND B Abstract In drug development studies, a large number of new drug candidates (leads) have to be synthesized and optimized by changing several moieties of the leads in order to increase efficacies and decrease toxicities. Each synthesis of these new drug candidates include multi-steps procedures. Overall, discovering a new drug is a very time-consuming and very costly works. The development of molecular modelling programs and their applications in pharmaceutical research have been formalized as a field of study known computer assisted drug design (CADD) or computer assisted molecular design (CAMD). In this study, using the above techniques, Monoamine Oxidase isozymes, which play an essential role in the oxidative deamination of the biogenic amines, were studied. Compounds that inhibit these isozymes were shown to have therapeutic value in a variety of conditions including several psychiatric and neurological as well as neurodegenerative diseases. First, a series of new pyrazoline derivatives were screened using molecular modelling and docking methods and promising lead compounds were selected, and proposed for synthesis as novel selective MAO-A or –B inhibitors. -
Effects of the Antitussive Drug Cloperastine on Ventricular Repolarization in Halothane-Anesthetized Guinea Pigs
J Pharmacol Sci 120, 000 – 000 (2012) Journal of Pharmacological Sciences © The Japanese Pharmacological Society Full Paper Effects of the Antitussive Drug Cloperastine on Ventricular Repolarization in Halothane-Anesthetized Guinea Pigs Akira Takahara1,*, Kaori Fujiwara1, Atsushi Ohtsuki2, Takayuki Oka2, Iyuki Namekata2, and Hikaru Tanaka2 1Department of Pharmacology and Therapeutics, 2Department of Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, Funabashi, Chiba 274-8510, Japan Received May 13, 2012; Accepted August 29, 2012 Abstract. Cloperastine is an antitussive drug, which can be received as an over-the-counter cold medicine. The chemical structure of cloperastine is quite similar to that of the antihistamine drug diphenhydramine, which is reported to inhibit hERG K+ channels and clinically induce long QT syndrome after overdose. To analyze its proarrhythmic potential, we compared effects of cloperas- tine and diphenhydramine on the hERG K+ channels expressed in HEK293 cells. We further as- sessed their effects on the halothane-anesthetized guinea-pig heart under the monitoring of mono- phasic action potential (MAP) of the ventricle. Cloperastine inhibited the hERG K+ currents in a concentration-dependent manner with an IC50 value of 0.027 μM, whose potency was 100 times greater than that of diphenhydramine (IC50; 2.7 μM). In the anesthetized guinea pigs, cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT intervalPROOF and MAP duration without affecting PR interval or QRS width. Diphenhydramine at a therapeutic dose of 10 mg/kg prolonged the QT interval and MAP duration together with increase in PR interval and QRS width. The present re- sults suggest that cloperastine may be categorized as a QT-prolonging drug that possibly induces arrhythmia at overdoses like diphenhydramine does. -
Management of Major Depressive Disorder Clinical Practice Guidelines May 2014
Federal Bureau of Prisons Management of Major Depressive Disorder Clinical Practice Guidelines May 2014 Table of Contents 1. Purpose ............................................................................................................................................. 1 2. Introduction ...................................................................................................................................... 1 Natural History ................................................................................................................................. 2 Special Considerations ...................................................................................................................... 2 3. Screening ........................................................................................................................................... 3 Screening Questions .......................................................................................................................... 3 Further Screening Methods................................................................................................................ 4 4. Diagnosis ........................................................................................................................................... 4 Depression: Three Levels of Severity ............................................................................................... 4 Clinical Interview and Documentation of Risk Assessment............................................................... -
(12) United States Patent (10) Patent No.: US 6,264,917 B1 Klaveness Et Al
USOO6264,917B1 (12) United States Patent (10) Patent No.: US 6,264,917 B1 Klaveness et al. (45) Date of Patent: Jul. 24, 2001 (54) TARGETED ULTRASOUND CONTRAST 5,733,572 3/1998 Unger et al.. AGENTS 5,780,010 7/1998 Lanza et al. 5,846,517 12/1998 Unger .................................. 424/9.52 (75) Inventors: Jo Klaveness; Pál Rongved; Dagfinn 5,849,727 12/1998 Porter et al. ......................... 514/156 Lovhaug, all of Oslo (NO) 5,910,300 6/1999 Tournier et al. .................... 424/9.34 FOREIGN PATENT DOCUMENTS (73) Assignee: Nycomed Imaging AS, Oslo (NO) 2 145 SOS 4/1994 (CA). (*) Notice: Subject to any disclaimer, the term of this 19 626 530 1/1998 (DE). patent is extended or adjusted under 35 O 727 225 8/1996 (EP). U.S.C. 154(b) by 0 days. WO91/15244 10/1991 (WO). WO 93/20802 10/1993 (WO). WO 94/07539 4/1994 (WO). (21) Appl. No.: 08/958,993 WO 94/28873 12/1994 (WO). WO 94/28874 12/1994 (WO). (22) Filed: Oct. 28, 1997 WO95/03356 2/1995 (WO). WO95/03357 2/1995 (WO). Related U.S. Application Data WO95/07072 3/1995 (WO). (60) Provisional application No. 60/049.264, filed on Jun. 7, WO95/15118 6/1995 (WO). 1997, provisional application No. 60/049,265, filed on Jun. WO 96/39149 12/1996 (WO). 7, 1997, and provisional application No. 60/049.268, filed WO 96/40277 12/1996 (WO). on Jun. 7, 1997. WO 96/40285 12/1996 (WO). (30) Foreign Application Priority Data WO 96/41647 12/1996 (WO). -
Parkinson's Disease Fact Sheet
Parkinson’s Disease Fact Sheet About Parkinson’s Disease Parkinson’s disease is a progressive, incurable neurological disorder associated with a loss of dopamine-generating cells in the brain. It is primarily associated with progressive loss of motor control, but it results in a complex array of symptoms, including many non-motor symptoms. Parkinson’s impacts an estimated one million people in the United States. Critical Clinical Care Considerations • To avoid serious side effects, Parkinson’s patients need their medications on time, every time — do not skip or postpone doses. • Write down the exact times of day medications are to be administered so that doses are given on the same schedule the patient follows at home. • Do not substitute Parkinson’s medications or stop levodopa therapy abruptly. • Resume medications immediately following procedures, unless vomiting or severely incapacitated. • If an antipsychotic is necessary, use pimavanserin (Nuplazid), quetiapine (Seroquel) or clozapine (Clozaril). • Be alert for symptoms of dysphagia (trouble swallowing) and risk of pneumonia. • Ambulate as soon as medically safe. Patients may require assistance. Common Symptoms of Parkinson’s Disease Motor Non-Motor • Shaking or tremor at rest • Depression • Bradykinesia or freezing (being stuck • Anxiety in place when attempting to walk) • Constipation • Low voice volume or muffled speech • Cognitive decline and dementia • Lack of facial expression • Impulse control disorders • Stiffness or rigidity of the arms, legs • Orthostatic hypotension or -
Clinical Inquiries
CLINICAL INQUIRIES F ROM THE F AMILY P RACTICE I NQUIRIES N ETWORK What is the best way to evaluate patients with acute diarrhea. Using retrospective 6 acute diarrhea? reviews, Bauer and colleagues developed a pre- diction rule for cases of infectious diarrhea. The “modified 3-day rule” recommends stool cultures EVIDENCE-BASED ANSWER Limited evidence for patients with diarrhea beginning more than 3 delineates the relative probabilities of causes of acute days after hospitalization only when they fall into 1 diarrhea, typically defined as a diarrheal disease last- of the following groups: patients older than 65 ing 14 days or fewer, in the developed world. Viruses years with permanently altered organ function, (rotavirus, Norwalk, and other enteric viruses) are those with HIV or neutropenia, those hospitalized responsible for most cases. Stool culture helps to iden- during suspected nosocomial outbreaks, and those tify bacterial causes (Salmonella, Shigella, enterotoxic suspected of nondiarrheal manifestations of enteric Escherichia coli), especially in patients with fever and infection.6 When the modified rule was applied bloody stool. A modified 3-day rule (eg, performing prospectively, only 2 cases were missed. Both only Clostridium difficile toxin tests on low-risk patients were at risk for immunosuppression, patients who have been hospitalized for 3 or more although they did not strictly meet the modified cri- days) leads to a more rational use of stool cultures teria. Neither required treatment.6 without missing cases of clinically significant disease. (Grade of recommendation: D, based on limited stud- RECOMMENDATIONS FROM OTHERS The ies, reliance on expert opinion, and consensus.) Infectious Diseases Society of America’s practice guidelines for the evaluation and treatment of acute EVIDENCE SUMMARY More than 2 million cases diarrhea recommends that stool culture for bacteria of infectious diarrhea are documented in the United (including enterotoxic E coli) should be considered States annually. -
AMERSA) 125 Whipple Street, 3Rd Floor Providence, Rhode Island 02908
Strategic Plan for Interdisciplinary Faculty Development: Arming the Nation’s Health Professional Workforce for a New Approach to Substance Use Disorders Edited by MARY R. HAACK, PHD, RN, FAAN HOOVER ADGER, JR., MD, MPH Association for Medical Education and Research in Substance Abuse (AMERSA) 125 Whipple Street, 3rd Floor Providence, Rhode Island 02908 For more information: AMERSA Telephone: 401-349-0000 Fax: 877-418-8769 Web Sites: www.amersa.org and www.projectmainstream.net This publication has been produced by the Association for Medical Education and Research in Substance Abuse under a Cooperative Agreement (HRSA-#U78HP00001) with the Bureau of Health Professions, Health Resources and Services Administration (HRSA), in collaboration with the Center for Substance Abuse Treatment, Substance Abuse and Mental Health Services Administration (SAMHSA). The conclusions and opinions expressed herein are those of the authors and do not necessarily represent the views and policies of HRSA or of SAMHSA. September 2002 TABLE OF CONTENTS Table of Contents............................................................................................................................................................iii Contributors ....................................................................................................................................................................v Acknowledgments .........................................................................................................................................................vii -
Development and Validation of a LC-MS/MS Method for Detection and Quantification of 18 Antidepressants in Whole Blood
City University of New York (CUNY) CUNY Academic Works Student Theses John Jay College of Criminal Justice Spring 6-2019 Development and validation of a LC-MS/MS method for detection and quantification of 18 antidepressants in whole blood Linda Kim CUNY John Jay College, [email protected] How does access to this work benefit ou?y Let us know! More information about this work at: https://academicworks.cuny.edu/jj_etds/106 Discover additional works at: https://academicworks.cuny.edu This work is made publicly available by the City University of New York (CUNY). Contact: [email protected] Development and validation of a LC-MS/MS method for detection and quantification of 18 antidepressants in whole blood A Thesis Presented in Partial Fulfillment of the Requirements for the Degree of Master of Science in Forensic Science, John Jay College of Criminal Justice, City University of New York Linda Kim May 2019 Development and validation of a LC-MS/MS method for detection and quantification of 18 antidepressants in whole blood Linda Kim This Thesis has been presented to and accepted by the Office of Graduate Studies, John Jay College of Criminal Justice in Partial Fulfillment of the Requirements for the Degree of Master of Science in Forensic Science. Thesis Committee Thesis Advisor: Marta Concheiro-Guisan Second Reader: Shu-Yuan Cheng External Reader: Damon Borg i Acknowledgement I would like to thank Dr. Stripp for providing his laboratory for my research, and Dr. Borg and everyone in Cordant Laboratory for their guidance and support. I would like to thank Dr. Concheiro-Guisan for her time, patience, and information, and for making it possible to successfully complete this thesis.