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Report on a Novel Emerging Class of Highly Potent Benzimidazole NPS Opioids: Chemical and in Vitro Functional Characterization of Isotonitazene
Received: 29 August 2019 Revised: 12 November 2019 Accepted: 13 November 2019 DOI: 10.1002/dta.2738 RESEARCH ARTICLE Report on a novel emerging class of highly potent benzimidazole NPS opioids: Chemical and in vitro functional characterization of isotonitazene Peter Blanckaert1† | Annelies Cannaert2† | Katleen Van Uytfanghe2 | Fabian Hulpia3 | Eric Deconinck4 | Serge Van Calenbergh3 | Christophe Stove2 1Scientific Direction Epidemiology and Public Health, Section Lifestyle and Chronic Diseases, Abstract Belgian Early Warning System Drugs This paper reports on the identification and full chemical characterization of (BEWSD), Sciensano, Brussels, Belgium isotonitazene (N,N-diethyl-2-[5-nitro-2-({4-[(propan-2-yl)oxy]phenyl}methyl)-1H-ben- 2Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical zimidazol-1-yl]ethan-1-amine), a potent NPS opioid and the first member of the Sciences, Ghent University, Ghent, Belgium benzimidazole class of compounds to be available on online markets. Interestingly, 3Laboratory for Medicinal Chemistry, Department of Pharmaceutics, Faculty of this compound was sold under the name etonitazene, a structural analog. Identifica- Pharmaceutical Sciences, Ghent University, tion of isotonitazene was performed by gas chromatography mass spectrometry Ghent, Belgium (GC–MS) and liquid chromatography time-of-flight mass spectrometry (LC-QTOF- 4Scientific Direction Chemical and Physical Health Risks, Service of Medicines and Health MS), the latter identifying an exact-mass m/z value of 411.2398. All chromatographic Products, Sciensano, Brussels, Belgium data indicated the presence of a single, highly pure compound. Confirmation of the 1 13 Correspondence specific benzimidazole regio-isomer was performed using H and C NMR spectros- copy, after which the chemical characterization was finalized by recording Fourier- Christophe Stove, Laboratory of Toxicology, Department of Bioanalysis, Faculty of transform (FT-IR) spectra. -
Ehealth DSI [Ehdsi V2.2.2-OR] Ehealth DSI – Master Value Set
MTC eHealth DSI [eHDSI v2.2.2-OR] eHealth DSI – Master Value Set Catalogue Responsible : eHDSI Solution Provider PublishDate : Wed Nov 08 16:16:10 CET 2017 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 1 of 490 MTC Table of Contents epSOSActiveIngredient 4 epSOSAdministrativeGender 148 epSOSAdverseEventType 149 epSOSAllergenNoDrugs 150 epSOSBloodGroup 155 epSOSBloodPressure 156 epSOSCodeNoMedication 157 epSOSCodeProb 158 epSOSConfidentiality 159 epSOSCountry 160 epSOSDisplayLabel 167 epSOSDocumentCode 170 epSOSDoseForm 171 epSOSHealthcareProfessionalRoles 184 epSOSIllnessesandDisorders 186 epSOSLanguage 448 epSOSMedicalDevices 458 epSOSNullFavor 461 epSOSPackage 462 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 2 of 490 MTC epSOSPersonalRelationship 464 epSOSPregnancyInformation 466 epSOSProcedures 467 epSOSReactionAllergy 470 epSOSResolutionOutcome 472 epSOSRoleClass 473 epSOSRouteofAdministration 474 epSOSSections 477 epSOSSeverity 478 epSOSSocialHistory 479 epSOSStatusCode 480 epSOSSubstitutionCode 481 epSOSTelecomAddress 482 epSOSTimingEvent 483 epSOSUnits 484 epSOSUnknownInformation 487 epSOSVaccine 488 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 3 of 490 MTC epSOSActiveIngredient epSOSActiveIngredient Value Set ID 1.3.6.1.4.1.12559.11.10.1.3.1.42.24 TRANSLATIONS Code System ID Code System Version Concept Code Description (FSN) 2.16.840.1.113883.6.73 2017-01 A ALIMENTARY TRACT AND METABOLISM 2.16.840.1.113883.6.73 2017-01 -
Pharmaceutical Appendix to the Tariff Schedule 2
Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9 -
Alcohol and Drug Abuse Subchapter 9
Chapter 8 – Alcohol and Drug Abuse Subchapter 9 Regulated Drug Rule 1.0 Authority This rule is established under the authority of 18 V.S.A. §§ 4201 and 4202 which authorizes the Vermont Board of Health to designate regulated drugs for the protection of public health and safety. 2.0 Purpose This rule designates drugs and other chemical substances that are illegal or judged to be potentially fatal or harmful for human consumption unless prescribed and dispensed by a professional licensed to prescribe or dispense them and used in accordance with the prescription. The rule restricts the possession of certain drugs above a specified quantity. The rule also establishes benchmark unlawful dosages for certain drugs to provide a baseline for use by prosecutors to seek enhanced penalties for possession of higher quantities of the drug in accordance with multipliers found at 18 V.S.A. § 4234. 3.0 Definitions 3.1 “Analog” means one of a group of chemical components similar in structure but different with respect to elemental composition. It can differ in one or more atoms, functional groups or substructures, which are replaced with other atoms, groups or substructures. 3.2 “Benchmark Unlawful Dosage” means the quantity of a drug commonly consumed over a twenty-four-hour period for any therapeutic purpose, as established by the manufacturer of the drug. Benchmark Unlawful dosage is not a medical or pharmacologic concept with any implication for medical practice. Instead, it is a legal concept established only for the purpose of calculating penalties for improper sale, possession, or dispensing of drugs pursuant to 18 V.S.A. -
ATP, 489 Absolute Configuration Benzomotphans, 204 Levotphanol
Index AIDA, 495 Affinity labeling, analogs of (Cont.) cAMP, 409, 489 motphine,448 ATP, 409, 489 naltrexone, 449 [3H] ATP, 489 norlevotphanol,449 Absolute configuration normetazocine, 181 benzomotphans, 204 norpethidine, 232 levotphanol, 115 oripavine, 453 methadone and analogs, 316 oxymotphone, 449 motphine, 86 K-Agonists, 179,405,434 phenoperidine, 234 Aid in Interactive Drug Analysis, 495 piperazine derivatives, 399 [L-Ala2] dermotphin, 363 prodines and analogs, 272 [D-Ala, D-Leu] enkephalin (DADL), 68, 344 sinomenine, 28, 115 [D-Ala2 , Bugs] enkephalinamide, 347, 447 viminol, 400 [D-Ala2, Met'] enkephalinamide, 337, 346, Ac 61-91,360 371,489 Acetylcholine, 5, 407 [D-Ala2]leu-enkephalin, 344, 346, 348 Acetylcholine analogs, 186, 191 [D-Ala2] met-enkephalin, 348 l-Acetylcodeine, 32 [D-Ala2] enkephalins, 347 Acetylmethadols (a and (3) Alfentanil, 296 maintenance of addicts by a-isomer, 304, 309 (±)-I1(3-Alkylbenzomotphans, 167, 170 metabolism, 309 11(3-Alkylbenzomotphans, 204 N-allyl and N-CPM analogs, 310, 431 7-Alkylisomotphinans, 146 stereochemistry, 323 N-Alkylnorketobemidones, 431 synthesis, 309 N-Alkylnorpethidines, 233 X-ray crystallography, 327 N-Allylnormetazocine, 420 6-Acetylmotphine, receptor binding, 27 N-Allylnormotphine, 405 Acetylnormethadol, 323 N-Allylnorpethidine, 233 8(3-Acyldihydrocodeinones, 52 3-Allylprodines (a and (3), 256 14-Acyl-4,5-epoxymotphinans, 58 'H-NMR and stereochemistry, 256 7-Acylhydromotphones, 128 X-ray crystallography, 256 Addiction, 4 N-Allylnormetazocine, 420 Adenylate cyclase, 6, 409, 413, 424, -
Alcohol and Drug Abuse Subchapter 9 Regulated Drug Rule 1.0 Authority
Chapter 8 – Alcohol and Drug Abuse Subchapter 9 Regulated Drug Rule 1.0 Authority This rule is established under the authority of 18 V.S.A. §§ 4201 and 4202 which authorizes the Vermont Board of Health to designate regulated drugs for the protection of public health and safety. 2.0 Purpose This rule designates drugs and other chemical substances that are illegal or judged to be potentially fatal or harmful for human consumption unless prescribed and dispensed by a professional licensed to prescribe or dispense them, and used in accordance with the prescription. The rule restricts the possession of certain drugs above a specified quantity. The rule also establishes benchmark unlawful dosages for certain drugs to provide a baseline for use by prosecutors to seek enhanced penalties for possession of higher quantities of the drug in accordance with multipliers found at 18 V.S.A. § 4234. 3.0 Definitions 3.1 “Analog” means one of a group of chemical components similar in structure but different with respect to elemental composition. It can differ in one or more atoms, functional groups or substructures, which are replaced with other atoms, groups or substructures. 3.2 “Benchmark Unlawful Dosage” means the quantity of a drug commonly consumed over a twenty-four hour period for any therapeutic purpose, as established by the manufacturer of the drug. Benchmark Unlawful dosage is not a medical or pharmacologic concept with any implication for medical practice. Instead, it is a legal concept established only for the purpose of calculating penalties for improper sale, possession, or dispensing of drugs pursuant to 18 V.S.A. -
Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0 -
Eu Early Warning System Situation Report
EU EARLY WARNING SYSTEM SITUATION REPORT Situation report 1 — June 2020 SITREP ID: EU-EWS-SITREP-2020-0001 Issued by: EMCDDA Date issued: 16/06/2020 Transmitted by: Action on New Drugs Sector, EMCDDA Recipients: Early Warning System Network Contents 1. Purpose 2 2. General update of the NPS situation 2 3. Operational matters 7 4. Subject focus: Potential impact of the COVID-19 pandemic on the drug markets and risks to people who use drugs 8 5. Update from the national early-warning systems 11 6. Publications and resources of interest 11 7. New psychoactive substances notified in 2020 — provisional list, 1 January–16 June 2020 13 8. References 15 EU-EWS-SITREP-2020-0001 1 of 16 1. Purpose The purpose of this situation report is to: provide a summary of recent information reported to the EU Early Warning System, including formal notifications and other important signals; highlight important operational issues; and, provide other resources identified by the EMCDDA. This report may contain information that might be under verification. The information and resources in this report are intended to strengthen situational awareness within the Network, as well as to help the Network to prepare for, respond to, and recover from public health and social threats caused by new psychoactive substances (NPS) and other substances of interest. A specific focus of this report is to: • highlight recent resources that examine the potential impact of the COVID-19 pandemic on the drug markets and risks to people who use drugs; and, • request that the Network expedite reporting of any event, especially those related to the pandemic, that you consider may have a potential high impact on public health. -
The Next Opioid on the Deadly New Psychoactive
Journal of Analytical Toxicology, 2020;44:937–946 doi:10.1093/jat/bkaa094 Advance Access Publication Date: 3 August 2020 Article Article First Report on Brorphine: The Next Opioid on the Deadly New Psychoactive Substance Downloaded from https://academic.oup.com/jat/article/44/9/937/5879253 by Ghent University user on 07 May 2021 Horizon? Nick Verougstraete1,2,#, Marthe M. Vandeputte1,#, Cathelijne Lyphout3, Annelies Cannaert1, Fabian Hulpia4, Serge Van Calenbergh4, Alain G. Verstraete2,5 and Christophe Stove1,* 1Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium; 2Department of Laboratory Medicine, Ghent University Hospital, Ghent, Belgium; 3Emergency Department, Ghent University Hospital, Ghent, Belgium; 4Laboratory for Medicinal Chemistry, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium and 5Department of Diagnostic Sciences, Ghent University, Ghent, Belgium #These authors contributed equally to this work. *Author to whom correspondence should be addressed. Email: [email protected] Abstract New psychoactive substances continue to appear on the drug market. Until recently, new syn- thetic opioids, which are among the most dangerous new psychoactive substances, primarily encompassed analogs of the potent analgesic fentanyl. Lately, also other new synthetic opioids have increasingly started to surface. This is the first report on the identification and full chemical characterization of brorphine, a novel potent synthetic opioid with a piperidine benzimidazolone structure. A powder, identified as brorphine, was obtained from a patient seeking medical helpfor detoxification. Brorphine was also found in a serum sample of the patient. Liquid chromatography– high-resolution mass spectrometry (LC–HRMS) identified an exact mass of m/z 400.1020 and 402.1005 for the compound, corresponding to both bromine isotopes. -
(12) Patent Application Publication (10) Pub. No.: US 2005/0137194A1 Cristoph (43) Pub
US 2005O137194A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0137194A1 Cristoph (43) Pub. Date: Jun. 23, 2005 (54) COMBINATION OF SELECTED OPIOIDS (30) Foreign Application Priority Data WITH OTHER ACTIVE COMPOUNDS FOR TREATMENT OF URINARY INCONTINENCE May 29, 2002 (DE)..................................... 102 24 107.4 (75) Inventor: Thomas Cristoph, Aachen (DE) Publication Classification Correspondence Address: CROWELL & MORING LLP (51) Int. Cl." .................... A61K 31/5377; A61K 31/485 INTELLECTUAL PROPERTY GROUP (52) U.S. Cl. ......................................... 514/235.2; 514/282 P.O. BOX 14300 WASHINGTON, DC 20044-4300 (US) (73) Assignee: Gruenenthal GmbH, Aachen (DE) (57) ABSTRACT (21) Appl. No.: 10/998,164 The invention relates to the combination of compounds of (22) Filed: Nov. 29, 2004 group A, especially opioids, with compounds of group B for for the treatment of urinary urgency or urinary incontinence. Related U.S. Application Data The invention also relates to corresponding pharmaceutical formulations and to methods for treating urinary urgency or (63) Continuation of application No. PCT/EP03/05529, urinary incontinence with a compound of group A and a filed on May 27, 2003. compound of group B. US 2005/0137194A1 Jun. 23, 2005 COMBINATION OF SELECTED OPODS WITH urinary tract (Wein, A. J., 1998, Urology 51 (Suppl. 21): OTHER ACTIVE COMPOUNDS FOR TREATMENT 43-47). These are usually medicaments which have an OF URINARY INCONTINENCE inhibiting action on the detrusor muscle, which is respon sible for the internal bladder pressure. These medicaments CROSS REFERENCE TO RELATED are e.g. parasympatholytics, Such as Oxybutynin, propiverine APPLICATIONS or tolterodine, tricyclic antidepressants, Such as imipramine, or muscle relaxants, Such as flavoxate. -
New Psychoactive Substances: Global Markets, Glocal Threats and the COVID-19 Pandemic
New psychoactive substances: global markets, glocal threats and the COVID-19 pandemic An update from the EU Early Warning System December 2020 Front cover photos 1. ‘Ching’ typically sold as a ‘legal’ replacement to cocaine. In this case the product contained methoxyacetylfentanyl. Credit: Slovenian National Forensic Laboratory (Police). 2. Plant material from a ‘Spice’ product that contained CP-47,497 C8 homolog. Credit: Slovenian National Forensic Laboratory (Police). 3. Package containing CUMYL-4CN-BINACA powder that shipped from China. Credit: Slovenian National Forensic Laboratory (Police). 4. Fake Xanax tablets that contained cyclopropylfentanyl. Credit: WR Brede, H-M Krabseth and co-workers, St. Olav University Hospital, Trondheim, Norway. New psychoactive substances: global markets, glocal threats and the COVID-19 pandemic An update from the EU Early Warning System December 2020 I Legal notice This publication of the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) is protected by copyright. The EMCDDA accepts no responsibility or liability for any consequences arising from the use of the data contained in this document. The contents of this publication do not necessarily reflect the official opinions of the EMCDDA’s partners, any EU Member State or any agency or institution of the European Union. Luxembourg: Publications Office of the European Union, 2020 © European Monitoring Centre for Drugs and Drug Addiction, 2020 Reproduction is authorised provided the source is acknowledged. For any use or reproduction of photos that are not under EMCDDA copyright, permission must be sought directly from the copyright holders. Photo credits for the front cover images: Laboratorio de Drogas (Servicio de Química), Instuto Nacional de Toxicología y Ciencias Forenses (INTyCF) Barcelona (1, 2), Hungarian Institute for Forensic Sciences (3), P. -
WO 2014/006004 Al 9 January 2014 (09.01.2014) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2014/006004 Al 9 January 2014 (09.01.2014) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 9/20 (2006.01) A61K 31/485 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (21) International Application Number: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, PCT/EP2013/06385 1 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, 1 July 20 13 (01 .07.2013) KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (25) Filing Language: English OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, (26) Publication Language: English SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: PA 2012 70405 6 July 2012 (06.07.2012) DK (84) Designated States (unless otherwise indicated, for every 61/668,741 6 July 2012 (06.07.2012) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (71) Applicant: EGALET LTD.