Known Bioactive Library: Microsource Discovery 1
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Monoamine Oxydases Et Athérosclérose : Signalisation Mitogène Et Études in Vivo
UNIVERSITE TOULOUSE III - PAUL SABATIER Sciences THESE Pour obtenir le grade de DOCTEUR DE L’UNIVERSITE TOULOUSE III Discipline : Innovation Pharmacologique Présentée et soutenue par : Christelle Coatrieux le 08 octobre 2007 Monoamine oxydases et athérosclérose : signalisation mitogène et études in vivo Jury Monsieur Luc Rochette Rapporteur Professeur, Université de Bourgogne, Dijon Monsieur Ramaroson Andriantsitohaina Rapporteur Directeur de Recherche, INSERM, Angers Monsieur Philippe Valet Président Professeur, Université Paul Sabatier, Toulouse III Madame Nathalie Augé Examinateur Chargé de Recherche, INSERM Monsieur Angelo Parini Directeur de Thèse Professeur, Université Paul Sabatier, Toulouse III INSERM, U858, équipes 6/10, Institut Louis Bugnard, CHU Rangueil, Toulouse Résumé Les espèces réactives de l’oxygène (EROs) sont impliquées dans l’activation de nombreuses voies de signalisation cellulaires, conduisant à différentes réponses comme la prolifération. Les EROs, à cause du stress oxydant qu’elles génèrent, sont impliquées dans de nombreuses pathologies, notamment l’athérosclérose. Les monoamine oxydases (MAOs) sont deux flavoenzymes responsables de la dégradation des catécholamines et des amines biogènes comme la sérotonine ; elles sont une source importante d’EROs. Il a été montré qu’elles peuvent être impliquées dans la prolifération cellulaire ou l’apoptose du fait du stress oxydant qu’elles génèrent. Ce travail de thèse a montré que la MAO-A, en dégradant son substrat (sérotonine ou tyramine), active une voie de signalisation mitogène particulière : la voie métalloprotéase- 2/sphingolipides (MMP2/sphingolipides), et contribue à la prolifération de cellules musculaire lisses vasculaires induite par ces monoamines. De plus, une étude complémentaire a confirmé l’importance des EROs comme stimulus mitogène (utilisation de peroxyde d’hydrogène exogène), et a décrit plus spécifiquement les étapes en amont de l’activation de MMP2, ainsi que l’activation par la MMP2 de la sphingomyélinase neutre (première enzyme de la cascade des sphingolipides). -
(PAC) Rev 24 Based on Applicable Aegls, Erpgs, Or Teels (Chemicals Listed by CASRN) PAC Rev 24 – August 2008
Table 3: Protective Action Criteria (PAC) Rev 24 based on applicable AEGLs, ERPGs, or TEELs (Chemicals listed By CASRN) PAC Rev 24 – August 2008 Table 3 presents a listing of chemicals and PAC data based on the Chemical Abstract Service Registry Numbers (CASRNs)1 of the chemicals. Chemicals without an identified CASRN number are issued an identification number, preceded by the letter “z,” for purposes of the PAC data set. The columns presented in Table 3 provide the following information: Heading Definition No. The ordered numbering of the chemicals as they appear in this listing by CASRN. Chemical Name The common name of the chemical. CASRN The Chemical Abstract Service Registry Number for this chemical. TEEL-0 This is the threshold concentration below which most people will experience no appreciable risk of health effects. This PAC is always based on TEEL-0 because AEGL-0 or ERPG-0 values do not exist. PAC-1 Based on the applicable AEGL-1, ERPG-1, or TEEL-1 value. PAC-2 Based on the applicable AEGL-2, ERPG-2, or TEEL-2 value. PAC-3 Based on the applicable AEGL-3, ERPG-3, or TEEL-3 value. Units The units for the PAC values (ppm or mg/m3). Additional information on the chemicals presented here is provided in PAC Tables 1, 2, and 4. Table 3, other PAC Tables, introductory/explanatory material (including a glossary of acronyms and abbreviations), definitions of PAC values, and alternative methods of displaying PAC information are available electronically at: http://www.hss.energy.gov/HealthSafety/WSHP/chem_safety/teel.html. -
(12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig. -
Lindane Lotion USP, 1% RX Only WARNINGS
Lindane Lotion USP, 1% RX Only WARNINGS: Lindane Lotion should only be used in patients who cannot tolerate or have failed first-line treatment with safer medications for the treatment of scabies. (See INDICATIONS AND USAGE.) Neurologic Toxicity Seizures and deaths have been reported following Lindane Lotion use with repeat or prolonged application, but also in rare cases following a single application used according to directions. Lindane lotion should be used with caution for infants, children, the elderly, and individuals with other skin conditions (e.g, atopic dermatitis, psoriasis) and in those who weigh < 110 lbs (50 kg) as they may be at risk of serious neurotoxicity. Contraindications Lindane Lotion is contraindicated in premature infants and individuals with known uncontrolled seizure disorders. Proper Use Instruct patients on the proper use of Lindane Lotion, the amount to apply, how long to leave it on, and avoiding re-treatment. Inform patients that itching occurs after the successful killing of scabies and is not necessarily an indication for re-treatment with Lindane Lotion. (See DOSAGE AND ADMINISTRATION.) DESCRIPTION Lindane Lotion USP, 1%, is an ectoparasiticide and ovicide. In addition to the active ingredient, lindane, it contains glycerol monostearate, cetyl alcohol, stearic acid, trolamine, carrageenan, 2- amino-2-methyl-1-propanol, methylparaben, butylparaben, perfume and water to form a lotion. Lindane is the gamma isomer of 1,2,3,4,5,6-hexachlorocyclohexane having the following structural formula: C6H6Cl6 M.W. 290.83 CLINICAL PHARMACOLOGY Lindane Lotion USP, 1%, is an ectoparasiticide and ovicide effective against Sarcoptes scabiei (scabies). Lindane exerts its parasiticidal action by being directly absorbed into the parasites and 1 their ova. -
Revised Use-Function Classification (2007)
INTERNATIONAL PROGRAMME ON CHEMICAL SAFETY IPCS INTOX Data Management System (INTOX DMS) Revised Use-Function Classification (2007) The Use-Function Classification is used in two places in the INTOX Data Management System: the Communication Record and the Agent/Product Record. The two records are linked: if there is an agent record for a Centre Agent that is the subject of a call, the appropriate Intended Use-Function can be selected automatically in the Communication Record. The Use-Function Classification is used when generating reports, both standard and customized, and for searching the case and agent databases. In particular, INTOX standard reports use the top level headings of the Intended Use-Functions that were selected for Centre Agents in the Communication Record (e.g. if an agent was classified as an Analgesic for Human Use in the Communication Record, it would be logged as a Pharmaceutical for Human Use in the report). The Use-Function classification is very important for ensuring harmonized data collection. In version 4.4 of the software, 5 new additions were made to the top levels of the classification provided with the system for the classification of organisms (items XIV to XVIII). This is a 'convenience' classification to facilitate searching of the Communications database. A taxonomic classification for organisms is provided within the INTOX DMS Agent Explorer. In May/June 2006 INTOX users were surveyed to find out whether they had made any changes to the Use-Function Classification. These changes were then discussed at the 4th and 5th Meetings of INTOX Users. Version 4.5 of the INTOX DMS includes the revised pesticides classification (shown in full below). -
Parkinson's Disease Glossary
Parkinson's Disease Glossary A guide to the scientific language of Parkinson’s disease Acetylcholine: One of the chemical neurotransmitters in the brain and other areas of the central and peripheral nervous system. It is highly concentrated in the basal ganglia, where it influences movement. It is located in other regions of the brain as well, and plays a role in memory. Drugs that block acetylcholine receptors (so-called anticholinergics) are utilized in the treatment of PD. Acetylchlinesterase Inhibitors: A drug that inhibits the enzyme that breaks down acetylcholine resulting in increased activity of the chemical neurotransmitter acetylcholine. Used to treat mild to moderate dementia in Parkinson’s disease. Agonist: A chemical or drug that can activate a neurotransmitter receptor. Dopamine agonists, such as pramipexole, ropinirole, bromocriptine and apomorphine, are used in the treatment of PD. Aggregate: A whole formed by the combination of several elements. In Parkinson’s disease, there is a clumping of many proteins inside neurons, including alpha-synuclein. Levy bodies are a kind of aggregate found in PD. Akinesia: Literally, means loss of movement also described as a difficulty with initiating voluntary movements. It is commonly used interchangeably with bradykinesia, however bradykinesia means slow movement. Alpha-synuclein: A protein present in nerve cells where it can be found in their cell body, their nucleus and their terminals. The accumulation and aggregation of this protein is a pathologic finding in PD. The first genetic mutation found in PD was discovered in the gene for alpha-synuclein (SNCA), and was called PARK1. Alpha-synuclein also accumulates in multiple system atrophy (MSA) and in Lewy Body Disease. -
Rutamarin: Efficient Liquid–Liquid Chromatographic Isolation from Ruta Graveolens L
molecules Article Rutamarin: Efficient Liquid–Liquid Chromatographic Isolation from Ruta graveolens L. and Evaluation of Its In Vitro and In Silico MAO-B Inhibitory Activity Ewelina Kozioł 1, Simon Vlad Luca 2,3, Hale Gamze A˘galar 4 , Begüm Nurpelin Sa˘glık 4 , Fatih Demirci 4,5, Laurence Marcourt 6 , Jean-Luc Wolfender 6 , Krzysztof Jó´zwiak 7 and Krystyna Skalicka-Wo´zniak 1,* 1 Independent Laboratory of Natural Products Chemistry, Department of Pharmacognosy, Medical University of Lublin, 20-093 Lublin, Poland; [email protected] 2 Department of Pharmacognosy, Grigore T. Popa University of Medicine and Pharmacy Iasi, 700115 Iasi, Romania; [email protected] 3 Biothermodynamics, TUM School of Life and Food Sciences Weihenstephan, Technical University of Munich, 85354 Freising, Germany 4 Department of Pharmacognosy, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey; [email protected] (H.G.A.); [email protected] (B.N.S.); [email protected] (F.D.) 5 Faculty of Pharmacy, Eastern Mediterranean University, Famagusta 99628, Cyprus 6 Institute of Pharmaceutical Sciences of Western Switzerland, IPSWS, University of Geneva, CMU, 1211 Geneva 4, Switzerland; [email protected] (L.M.); [email protected] (J.-L.W.) 7 Department of Biopharmacy, Medical University of Lublin, 20-093 Lublin, Poland; [email protected] * Correspondence: [email protected] Academic Editors: Tomasz Tuzimski and James Barker Received: 29 April 2020; Accepted: 5 June 2020; Published: 9 June 2020 Abstract: Naturally occurring coumarins are a group of compounds with many documented central nervous system (CNS) activities. However, dihydrofuranocoumarins have been infrequently investigated for their bioactivities at CNS level. -
NO-1886 Decreases Ectopic Lipid Deposition and Protects Pancreatic Cells in Diet-Induced Diabetic Swine
399 NO-1886 decreases ectopic lipid deposition and protects pancreatic cells in diet-induced diabetic swine W Yin*,1,2,5, D Liao*,1,2, M Kusunoki6,SXi1, K Tsutsumi3, Z Wang1, X Lian1, T Koike4, J Fan4, Y Yang5 and C Tang5 1Department of Biochemistry and Biotechnology, Nanhua University School of Life Sciences and Technology, Hengyang, Hunan 421001, China 2Department of Pathophysiology, Central South University Xiangya Medical College, Changsha, Hunan, China 3Research and Development, Otsuka Pharmaceutical Factory Inc., Tokushima, Japan 4Laboratory of Cardiovascular Disease, Department of Pathology, Institute of Basic Medical Sciences, University of Tsukuba, Tsukuba 305-8575, Japan 5Institute of Cardiovascular Research, Nanhua University Medical School, Hengyang, Hunan 421001, China 6Department of Internal Medicine, Faculty of Medicine, Aichi Medical University, Nagakute-cho, Aichigunte, Aichi 480-11, Japan (Requests for offprints should be addressed to W Yin, Department of Biochemistry and Molecular Biology, Nanhua University School of Life Sciences and Technology, Hengyang, Hunan 421001, China; Email: [email protected]) *W Yin and D Liao contributed equally to this paper Abstract The synthetic compound NO-1886 (ibrolipim) is a lipo- skeletal muscle, liver and pancreas, and also caused pan- protein lipase activator that has been proven to be highly creatic cell damage. However, supplementing 1% NO- effective in lowering plasma triglycerides. Recently, we 1886 (200 mg/kg per day) into the high-fat/high-sucrose found that NO-1886 also reduced plasma free fatty acids diet decreased ectopic lipid deposition, improved insulin and glucose in high-fat/high-sucrose diet-induced dia- resistance, and alleviated the cell damage. These results betic rabbits. -
Customs Tariff - Schedule
CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2020 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, UST, following to be employed in commercial fishing or the commercial MT, MUST, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels. -
Theranostics and Contrast Agents for Magnetic Resonance Imaging Yohan Jeong, Hee Sook Hwang and Kun Na*
Jeong et al. Biomaterials Research (2018) 22:20 https://doi.org/10.1186/s40824-018-0130-1 REVIEW Open Access Theranostics and contrast agents for magnetic resonance imaging Yohan Jeong, Hee Sook Hwang and Kun Na* Abstract Background: Magnetic resonance imaging is one of the diagnostic tools that uses magnetic particles as contrast agents. It is noninvasive methodology which provides excellent spatial resolution. Although magnetic resonance imaging offers great temporal and spatial resolution and rapid in vivo images acquisition, it is less sensitive than other methodologies for small tissue lesions, molecular activity or cellular activities. Thus, there is a desire to develop contrast agents with higher efficiency. Contrast agents are known to shorten both T1 and T2. Gadolinium based contrast agents are examples of T1 agents and iron oxide contrast agents are examples of T2 agents. In order to develop high relaxivity agents, gadolinium or iron oxide-based contrast agents can be synthesized via conjugation with targeting ligands or functional moiety for specific interaction and achieve accumulation of contrast agents at disease sites. Main body: This review discusses the principles of magnetic resonance imaging and recent efforts focused on specificity of contrast agents on specific organs such as liver, blood, lymph nodes, atherosclerotic plaque, and tumor. Furthermore, we will discuss the combination of theranostic such as contrast agent and drug, contrast agent and thermal therapy, contrast agent and photodynamic therapy, and neutron capture therapy, which can provide for cancer diagnosis and therapeutics. Conclusion: These applications of magnetic resonance contrast agents demonstrate the usefulness of theranostic agents for diagnosis and treatment. -
Topical and Systemic Antifungal Therapy for Chronic Rhinosinusitis (Protocol)
CORE Metadata, citation and similar papers at core.ac.uk Provided by University of East Anglia digital repository Cochrane Database of Systematic Reviews Topical and systemic antifungal therapy for chronic rhinosinusitis (Protocol) Head K, Sacks PL, Chong LY, Hopkins C, Philpott C Head K, Sacks PL, Chong LY, Hopkins C, Philpott C. Topical and systemic antifungal therapy for chronic rhinosinusitis. Cochrane Database of Systematic Reviews 2016, Issue 11. Art. No.: CD012453. DOI: 10.1002/14651858.CD012453. www.cochranelibrary.com Topical and systemic antifungal therapy for chronic rhinosinusitis (Protocol) Copyright © 2016 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. TABLE OF CONTENTS HEADER....................................... 1 ABSTRACT ...................................... 1 BACKGROUND .................................... 1 OBJECTIVES ..................................... 3 METHODS ...................................... 3 ACKNOWLEDGEMENTS . 8 REFERENCES ..................................... 9 APPENDICES ..................................... 10 CONTRIBUTIONSOFAUTHORS . 25 DECLARATIONSOFINTEREST . 26 SOURCESOFSUPPORT . 26 NOTES........................................ 26 Topical and systemic antifungal therapy for chronic rhinosinusitis (Protocol) i Copyright © 2016 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. [Intervention Protocol] Topical and systemic antifungal therapy for chronic rhinosinusitis Karen Head1, Peta-Lee Sacks2, Lee Yee Chong1, Claire Hopkins3, Carl Philpott4 1UK Cochrane Centre, -
Study Protocol C31002 Protocol a M End Ment 2
Title: Phase 1 Study to Evaluate the Effect of MLN0128 on the QTc Interval in Patients With Advanced Solid Tumors NCT Number: NCT02197572 Protocol Approve Date: 28 November 2017 Certain information within this protocol has been redacted (ie, specific content is masked irreversibly from view with a black/blue bar) to protect either personally identifiable information (PPD) or company confidential information (CCI). This may include, but is not limited to, redaction of the following: Named persons or organizations associated with the study. Proprietary information, such as scales or coding systems, which are considered confidential information under prior agreements with license holder. Other information as needed to protect confidentiality of Takeda or partners, personal information, or to otherwise protect the integrity of the clinical study. M L N 0 1 2 8 Clinical Study Protocol C31002 Protocol A m end ment 2 CLINICAL STUDY PROTOCOL C31002 PROTOCOL A MEND MENT 2 M L N 0 1 2 8 A P h as e 1 St u d y t o E v al u at e t h e Eff e ct of M L N 0 1 2 8 o n t h e Q T c I nt er v al i n P ati e nts Wit h Advanced Solid Tu mors Protocol Nu mber: C 3 1 0 0 2 Indication: Ad vanced solid tu mors P h as e: 1 S p o ns o r: Mill e n ni u m P h ar m a c e uti c als, I n c. Eudra CT Nu mber: N ot a p pli c a bl e Therapeutic Area: O n c o l og y Protocol History Ori gi n al 29 October 2013 Protocol A mend ment 1 26 June 2014 Protocol A mend ment 2 28 Nove mber 2017 Mill e n ni u m P h ar m a c e uti c als, I n c.