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Novel Antagonists for the Human Adenosine
UvA-DARE (Digital Academic Repository) Novel antagonists for the human adenosine A2A and A3 receptor via purine nitration: synthesis and biological evaluation of C2-substituted 6- trifluoromethylpurines and 1-deazapurines Koch, M. Publication date 2011 Document Version Final published version Link to publication Citation for published version (APA): Koch, M. (2011). Novel antagonists for the human adenosine A2A and A3 receptor via purine nitration: synthesis and biological evaluation of C2-substituted 6-trifluoromethylpurines and 1- deazapurines. General rights It is not permitted to download or to forward/distribute the text or part of it without the consent of the author(s) and/or copyright holder(s), other than for strictly personal, individual use, unless the work is under an open content license (like Creative Commons). Disclaimer/Complaints regulations If you believe that digital publication of certain material infringes any of your rights or (privacy) interests, please let the Library know, stating your reasons. In case of a legitimate complaint, the Library will make the material inaccessible and/or remove it from the website. Please Ask the Library: https://uba.uva.nl/en/contact, or a letter to: Library of the University of Amsterdam, Secretariat, Singel 425, 1012 WP Amsterdam, The Netherlands. You will be contacted as soon as possible. UvA-DARE is a service provided by the library of the University of Amsterdam (https://dare.uva.nl) Download date:05 Oct 2021 Novel antagonists for the human adenosine A Novel antagonists for the human adenosine Uitnodiging Novel antagonists for the voor het bijwonen van human adenosine de openbare verdediging van het proefschrift van A2A and A3 receptor via purine nitration Melle Koch op vrijdag 21 oktober 2011 om 14:00 uur in de Agnietenkapel van de Universiteit van Amsterdam Synthesis and biological evaluation Oudezijds Voorburgwal 231 of C2-substituted te Amsterdam 2A Na afloop van de promotie and A 6-trifluoromethylpurines zal hier tevens de receptie . -
Guidelines for the Forensic Analysis of Drugs Facilitating Sexual Assault and Other Criminal Acts
Vienna International Centre, PO Box 500, 1400 Vienna, Austria Tel.: (+43-1) 26060-0, Fax: (+43-1) 26060-5866, www.unodc.org Guidelines for the Forensic analysis of drugs facilitating sexual assault and other criminal acts United Nations publication Printed in Austria ST/NAR/45 *1186331*V.11-86331—December 2011 —300 Photo credits: UNODC Photo Library, iStock.com/Abel Mitja Varela Laboratory and Scientific Section UNITED NATIONS OFFICE ON DRUGS AND CRIME Vienna Guidelines for the forensic analysis of drugs facilitating sexual assault and other criminal acts UNITED NATIONS New York, 2011 ST/NAR/45 © United Nations, December 2011. All rights reserved. The designations employed and the presentation of material in this publication do not imply the expression of any opinion whatsoever on the part of the Secretariat of the United Nations concerning the legal status of any country, territory, city or area, or of its authorities, or concerning the delimitation of its frontiers or boundaries. This publication has not been formally edited. Publishing production: English, Publishing and Library Section, United Nations Office at Vienna. List of abbreviations . v Acknowledgements .......................................... vii 1. Introduction............................................. 1 1.1. Background ........................................ 1 1.2. Purpose and scope of the manual ...................... 2 2. Investigative and analytical challenges ....................... 5 3 Evidence collection ...................................... 9 3.1. Evidence collection kits .............................. 9 3.2. Sample transfer and storage........................... 10 3.3. Biological samples and sampling ...................... 11 3.4. Other samples ...................................... 12 4. Analytical considerations .................................. 13 4.1. Substances encountered in DFSA and other DFC cases .... 13 4.2. Procedures and analytical strategy...................... 14 4.3. Analytical methodology .............................. 15 4.4. -
HIV and Substance Use October 2016
HIV and Substance Use October 2016 Fast Facts • Alcohol and other drugs can affect a person’s judgment and increase risk of getting or transmitting HIV. • In people living with HIV, substance use can worsen the overall consequences of HIV. • Social and structural factors make it difficult to prevent HIV among people who use substances. Substance use disorders, which are problematic patterns of using alcohol or another substance, such as crack cocaine, methamphetamine (“meth”), amyl nitrite (“poppers”), prescription opioids, and heroin, are closely associated with HIV and other sexually transmitted diseases. Injection drug use (IDU) can be a direct route of HIV transmission if people share needles, syringes, or other injection materials that are contaminated with HIV. However, drinking alcohol and ingesting, smoking, or inhaling drugs are also associated with increased risk for HIV. These substances alter judgment, which can lead to risky sexual behaviors (e.g., having sex without a condom, having multiple partners) that can make people more likely to get and transmit HIV. In people living with HIV, substance use can hasten disease progression, affect adherence to antiretroviral therapy (HIV medicine), and worsen the overall consequences of HIV. Commonly Used Substances and HIV Risk • Alcohol. Excessive alcohol consumption, notably binge drinking, can be an important risk factor for HIV because it is linked to risky sexual behaviors and, among people living with HIV, can hurt treatment outcomes. • Opioids. Opioids, a class of drugs that reduce pain, include both prescription drugs and heroin. They are associated with HIV risk behaviors such as needle sharing when injected and risky sex, and have been linked to a recent HIV outbreak. -
Amyl Nitrite Or 'Jungle Juice'
Young People and Other Drugs Amyl Nitrite or ‘Jungle Juice’ Amyl nitrite is an inhalant that belongs to a class As with any drug, the use of nitrites is not risk-free. of chemicals called alkyl nitrites. This group of Some of the harms associated with its use include: drugs can be called ‘poppers’. They are often injuries related to inhaling the vapour referred to by their brand name, with ‘Jungle (e.g., rashes, burns) Juice’ probably being the most well-known of these. allergic reactions accidents and falls Inhaling amyl nitrite relaxes the body and gives vision problems (isopropyl nitrite) a ‘rush’ that lasts for one to two minutes. It is commonly used to enhance sexual pleasure and in rare cases, blood disorders induce a feeling of euphoria and well-being. MOST IMPORTANTLY, AMYL NITRITE OR JUNGLE JUICE MUST NEVER BE DRUNK. Drinking amyl can result in death due to it interfering with the ability of the blood to transport oxygen. What is amyl nitrite? Over the years, to bypass legal restrictions, nitrites have been sold as such things as liquid incense or Amyl nitrite is an inhalant that belongs to a class of room odoriser. Jungle Juice, which can be sold as chemicals called alkyl nitrites. Amyl nitrite is a highly a leather cleaner, is a common product name of flammable liquid that is clear or yellowish in colour. amyl nitrite. It has a unique smell that is sometimes described as ‘dirty socks’. It is highly volatile and when exposed to the air evaporates almost immediately at How is Jungle Juice used? room temperature. -
Primary-Explosives
Improvised Primary Explosives © 1998 Dirk Goldmann No part of the added copyrighted parts (except brief passages that a reviewer may quote in a review) may be reproduced in any form unless the reproduced material includes the following two sentences: The copyrighted material may be reproduced without obtaining permission from anyone, provided: (1) all copyrighted material is reproduced full-scale. WARNING! Explosives are danegerous. In most countries it's forbidden to make them. Use your mind. You as an explosives expert should know that. 2 CONTENTS Primary Explosives ACETONE PEROXIDE 4 DDNP/DINOL 6 DOUBLE SALTS 7 HMTD 9 LEAD AZIDE 11 LEAD PICRATE 13 MEKAP 14 MERCURY FULMINATE 15 "MILK BOOSTER" 16 NITROMANNITE 17 SODIUM AZIDE 19 TACC 20 Exotic and Friction Primers LEAD NITROANILATE 22 NITROGEN SULFIDE 24 NITROSOGUANIDINE 25 TETRACENE 27 CHLORATE-FRICTION PRIMERS 28 CHLORATE-TRIMERCURY-ACETYLIDE 29 TRIHYDRAZINE-ZINC (II) NITRATE 29 Fun and Touch Explosives CHLORATE IMPACT EXPLOSIVES 31 COPPER ACETYLIDE 32 DIAMMINESILVER II CHLORATE 33 FULMINATING COPPER 33 FULMINATING GOLD 34 FULMINATING MERCURY 35 FULMINATING SILVER 35 NITROGEN TRICHLORIDE 36 NITROGEN TRIIODIDE 37 SILVER ACETYLIDE 38 SILVER FULMINATE 38 "YELLOW POWDER" 40 Latest Additions 41 End 3 PRIMARY EXPLOSIVES ACETONE PEROXIDE Synonyms: tricycloacetone peroxide, acetontriperoxide, peroxyacetone, acetone hydrogen explosive FORMULA: C9H18O6 VoD: 3570 m/s @ 0.92 g/cc. 5300 m/s @ 1.18 g/cc. EQUIVALENCE: 1 gram = No. 8 cap .75 g. = No. 6 cap SENSITIVITY: Very sensitive to friction, flame and shock; burns violently and can detonate even in small amounts when dry. DRAWBACKS: in 10 days at room temp. 50 % sublimates; it is best made immediately before use. -
Irreversible Activation and Stabilization of Soluble Guanylate Cyclase by The
Molecular Pharmacology Fast Forward. Published on November 14, 2017 as DOI: 10.1124/mol.117.109918 This article has not been copyedited and formatted. The final version may differ from this version. MOL #109918 Irreversible activation and stabilization of soluble guanylate cyclase by the protoporphyrin IX mimetic cinaciguat Alexander Kollau, Marissa Opelt, Gerald Wölkart, Antonius C.F. Gorren, Michael Russwurm, Doris Koesling, Bernd Mayer and Astrid Schrammel Downloaded from Department of Pharmacology and Toxicology, University of Graz, Austria molpharm.aspetjournals.org (A.K., M.O., G.W., A.C.F.G., B.M., A.S.) Department of Pharmacology and Toxicology, Ruhr University Bochum, Bochum, Germany (M.R., D.K.) at ASPET Journals on September 29, 2021 1 Molecular Pharmacology Fast Forward. Published on November 14, 2017 as DOI: 10.1124/mol.117.109918 This article has not been copyedited and formatted. The final version may differ from this version. MOL #109918 Running Title: Irreversible activation of sGC by cinaciguat Address correspondence to: Dr. Astrid Schrammel Department of Pharmacology and Toxicology Karl-Franzens-Universität Graz Humboldtstrasse 46, A-8010 Graz, Austria Downloaded from Tel.: +43-316-380-5559 Fax: +43-316-380-9890 e-mail: [email protected] molpharm.aspetjournals.org Number of text pages: 24 Number of tables: – at ASPET Journals on September 29, 2021 Number of figures: 3 Number of references: 27 Number of words in Abstract: 236 Introduction: 436 Discussion: 904 1Abbreviations: DEA/NO, 2,2-diethyl-1-nitroso-oxyhydrazine; DTT, dithiothreitol; IBMX, 3-isobutyl-1-methylxanthin; NO, nitric oxide; ODQ, 1H-[1,2,4]oxadiazolo-[4,3- a]quinoxalin-1-one; PDE, phosphodiesterase; sGC, soluble guanylate cyclase; 2 Molecular Pharmacology Fast Forward. -
Download Transcript
Clinical Education Initiative [email protected] ECHO: CHEM SEX Hansel Arroyo, MD 12/04/2019 ECHO: Chem Sex [video transcript] 00:10 Okay, so on the same vein of this case. My presentation is called Chem sex. Neo formerly club drugs. 00:21 I have no disclosures. Like I said, I'm the Director of Psychiatry and Behavioral Medicine at the Institute for Advanced Medicine and Surgery. 00:31 The objectives are 00:35 just for the use of club drugs in the context of sexual performance raves and circuit parties describe the most commonly used synthesized chemicals during Chem sex, and explore the additive properties and potential treatments of club drugs. Oh, 00:50 you know, let's just start with this idea that 00:53 like all things are poison, right, Paracelsus said this for there's nothing without poisonous quality is only the dose, which makes a thing poison. And this is a little bit of how I approach patients who come in with any sort of altering drug use 01:12 to not automatically define them as 01:18 psychiatric disorder, right, I do not automatically give them a diagnosis of substance abuse disorder, regardless of what substance is using, but really, it's the issue of functional impairment is this substance causing some functional impairment like in the case, the patient was very severely impaired without the drug, he was unable to function. He was completely isolated, had no you know, social interactions outside of the world of, 01:49 of drug use. He was lucky that he is very smart and was able to, like do the same kind of compartmentalizes work and not sort of end up 02:01 1 essentially, like on the streets like many of our patients end up. -
Methamphetamine Use Disorder: Getting up to Speed on Trends & Treatments
Northwest ATTC & CTN Western States Node present: Methamphetamine Use Disorder: Getting Up to Speed on Trends & Treatments Methamphetamine Use Disorder Robrina Walker, PhD • Associate Professor, Dept. of Psychiatry, U Texas Southwestern Medical Center • Helped lead CTN Texas Node • Co-Lead Investigator of CTN-0068 • Co-Investigator of CTN-0090 • Co-Investigator of the COMEBACK study Methamphetamine Use Disorder: Getting Up to Speed on Trends and Treatments Robrina Walker, PhD Associate Professor University of Texas Southwestern Medical Center February 25, 2020 Disclosures . Disclosures . Alkermes: Provided injectable extended-release naltrexone (Vivitrol®) for CTN-0054 ADAPT-MD . Alkermes: Provided injectable extended-release naltrexone (Vivitrol®) and matched injectable placebo for CTN-0068 ADAPT-2 . Funding . NIDA UG1 DA020024 (PI: Trivedi) . NIDA R34 DA045592 (PI: Nijhawan) Opioids are a Huge and Necessary Focus… https://www.statnews.com/2016/09/29/why-fentanyl-is-deadlier-than-heroin/ …Why talk about Methamphetamine? https://www.webmd.com/mental-health/addiction/news/20180403/experts-warn-of-emerging-stimulant-epidemic …Why talk about Methamphetamine? https://www.webmd.com/mental-health/addiction/news/20180403/experts-warn-of-emerging-stimulant-epidemic https://www.npr.org/sections/health-shots/2018/10/25/656192849/methamphetamine-roils-rural-towns-again-across-the-u-s …Why talk about Methamphetamine? https://www.webmd.com/mental-health/addiction/news/20180403/experts-warn-of-emerging-stimulant-epidemic https://www.npr.org/sections/health-shots/2018/10/25/656192849/methamphetamine-roils-rural-towns-again-across-the-u-s http://time.com/5460632/meth-hospitalizations- opioids/?utm_source=twitter.com&utm_medium=social&utm_campaign=time&xid=time_socialflow_twitter Objectives 1. Describe trends in the use of methamphetamine 2. -
1,3-Oxazolidin-2-One Derivatives Useeful As Cetp Inhibitors
(19) TZZ Z Z_T (11) EP 2 029 560 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 263/22 (2006.01) C07D 413/04 (2006.01) 24.04.2013 Bulletin 2013/17 C07D 413/10 (2006.01) C07D 417/10 (2006.01) C07D 417/14 (2006.01) A61K 31/421 (2006.01) (2006.01) (2006.01) (21) Application number: 06849136.4 A61K 31/422 A61K 31/427 A61K 31/443 (2006.01) A61P 9/00 (2006.01) (22) Date of filing: 29.12.2006 (86) International application number: PCT/US2006/049494 (87) International publication number: WO 2007/079186 (12.07.2007 Gazette 2007/28) (54) 1,3-OXAZOLIDIN-2-ONE DERIVATIVES USEEFUL AS CETP INHIBITORS 1,3-OXAZOLIDIN-2-ON-DERIVATIVE, DIE ZUR VERWENDUNG ALS CETP-INHIBITOREN GEEIGNET SIND DERIVES DE 1,3-OXAZOLIDIN-2-ONE EN TANT QU’INHIBITEURS DE CETP (84) Designated Contracting States: • SINCLAIR, Peter, J. AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Rahway, New Jersey 07065-0907 (US) HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI • CHEN, Yi-Heng SK TR Rahway, New Jersey 07065-0907 (US) • SMITH, Cameron, J. (30) Priority: 30.12.2005 US 755284 P Rahway, New Jersey 07065-0907 (US) • LI, Hong (43) Date of publication of application: Rahway, New Jersey 07065-0907 (US) 04.03.2009 Bulletin 2009/10 (74) Representative: Hussain, Deeba (73) Proprietor: Merck Sharp & Dohme Corp. Merck & Co., Inc. Rahway, NJ 07065-0907 (US) Patent Department Hertford Road (72) Inventors: Hoddesdon • ALI, Amjad Hertfordshire EN11 9BU (GB) Rahway, New Jersey 07065-0907 (US) • LU, Zhijian (56) References cited: Rahway, New Jersey 07065-0907 (US) EP-A1- 0 294 995 EP-A1- 0 605 729 WO-A-2006/014413 Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. -
Doctor of Philosophy University of London
ASPECTS OF THIONITRITES AND NITRIC OXIDE IN CHEMISTRY AND BIOLOGY A Thesis Presented by Marta Cavero Tomas In Partial Fulfilment of the Requirements for the Award of the Degree of DOCTOR OF PHILOSOPHY OF THE UNIVERSITY OF LONDON Christopher Ingold Laboratories, Department of Chemistry, University College London, London WC IN OAJ October 1999 ProQuest Number: 10797749 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a com plete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. uest ProQuest 10797749 Published by ProQuest LLC(2018). Copyright of the Dissertation is held by the Author. All rights reserved. This work is protected against unauthorized copying under Title 17, United States C ode Microform Edition © ProQuest LLC. ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, Ml 48106- 1346 ABSTRACT This thesis is divided into three parts: Part one is comprised of six chapters and provides a topical review of the main aspects of the chemistry and biology of nitric oxide and of thionitrites. The first chapter is a general introduction to the topic. The second chapter reviews the biology of nitric oxide. The third chapter provides a survey of some of the known chemistry of nitric oxide, with particular emphasis on those aspects which might be relevant in biological systems. The fourth chapter describes the biology of thionitrites in relation to NO. -
Guanylate Cyclase
Guanylate Cyclase Guanylate cyclase (guanylyl cyclase, GC), which catalyzes the formation of cGMP from GTP, exists in both the soluble and particulate fractions of cells. Guanylyl cyclases signal via the production of the second messenger cGMP. The GC family consists of particulate GC (pGC) and a nitric oxide-activated soluble GC (sGC). Seven pGC isoforms have yet been found (pGC-A to pGC-G). pGCs are activated by binding of peptide ligands to their extracellular domains. sGC is a receptor for endogenous and exogenous nitric oxide and is activated several-fold upon its binding, constituting a core enzyme in the nitric oxide signal transduction pathway. cGMP generated by sGC is an important second messenger that regulates activity of several enzymes triggering such important physiologic reactions as vasodilation, smooth muscle relaxation and platelet aggregation. www.MedChemExpress.com 1 Guanylate Cyclase Inhibitors, Agonists & Activators (4-Acetamidocyclohexyl) nitrate (Rac)-BI 703704 (BM121307) Cat. No.: HY-100295 Cat. No.: HY-117962 (4-Acetamidocyclohexyl) nitrate (BM121307) is a (Rac)-BI 703704 is a potent soluble guanylyl guanylate cyclase activator. cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg (Rac)-MGV354 BAY 41-2272 Cat. No.: HY-117917 Cat. No.: HY-12376 (Rac)-MGV354 is the racemate of MGV354. MGV354 is BAY 41-2272 is a soluble guanylate cyclases (sGC) a soluble guanylate cyclase (sGC) activator with activator. -
UC Berkeley UC Berkeley Electronic Theses and Dissertations
UC Berkeley UC Berkeley Electronic Theses and Dissertations Title On the Molecular Mechanisms of Functional and Dysfunction NO Signaling in Mammalian Physiology Permalink https://escholarship.org/uc/item/2cq0g1wq Author Fernhoff, Nathaniel Bernard Publication Date 2010 Peer reviewed|Thesis/dissertation eScholarship.org Powered by the California Digital Library University of California On the Molecular Mechanisms of Functional and Dysfunction NO Signaling in Mammalian Physiology By Nathaniel Bernard Fernhoff A dissertation submitted in partial satisfaction of the requirements for the degree of Doctor of Philosophy in Molecular and Cell Biology in the Graduate Division of the University of California, Berkeley Committee in charge: Professor Michael A. Marletta, Chair Professor Susan Marqusee Professor Judith P. Klinman Professor Matthew B. Francis Spring 2010 On the Molecular Mechanisms of Functional and Dysfunction NO Signaling in Mammalian Physiology © 2010 Nathaniel Bernard Fernhoff Abstract On the Molecular Mechanisms of Functional and Dysfunction NO Signaling in Mammalian Physiology by Nathaniel Bernard Fernhoff Doctor of Philosophy in Molecular and Cell Biology University of California, Berkeley Professor Michael A. Marletta, Chair Nitric oxide (NO) is an important physiological mediator of vasodilation, platelet aggregation, and neurotransmission. An NO signal regulates these processes by signal transduction through the enzyme soluble guanylate cyclase (sGC), and dysfunction in this pathway manifests in human disease. NO activates sGC several hundred fold to produce the second messenger cGMP, and the mechanism of activation was previously thought to result exclusively from NO binding to the sGC heme. However, recent studies have shown that heme-bound NO only partially activates sGC and additional NO binding to a nonheme site is required for maximal NO activation.