Methylone Latest Revision: September 25, 2013

Total Page:16

File Type:pdf, Size:1020Kb

Methylone Latest Revision: September 25, 2013 Methylone Latest Revision: September 25, 2013 O O NH CH3 CH O 3 1. GENERAL INFORMATION IUPAC Name: 1-(1,3-benzodioxol-5-yl)-2-(methylamino)propan-1-one CFR: Schedule I CAS#: 186028-79-5 (base), 186028-80-8 (HCl) Synonyms: bk-MDMA, b-ketone-MDMA, bk-methylenedioxymethamphetamine, MDMC, 3,4-methylenedioxymethcathinone, N-methyl-MDC, 3,4-methylenedioxy-N-methylcathinone, N-methyl-3,4-methylenedioxycathinone Source: DEA Reference Material Collection Appearance: White powder (HCl) Kovat's Index: Pending UVmax (nm): 234.0, 281.9, 320.1 2. CHEMICAL AND PHYSICAL DATA 2.1 CHEMICAL DATA Form Chemical Formula Molecular Weight Melting Point (oC) Base C11H13NO3 207 Not Determined . HCl C11H13NO3 HCl 243 248.4 3. ADDITIONAL RESOURCES http://forendex.southernforensic.org/index.php/detail/index/1094Forendex http://en.wikipedia.org/wiki/MethyloneWikipedia Page 1 of 4 Page 2 of 6 4. QUALITATIVE DATA 4.1 NUCLEAR MAGNETIC RESONANCE Method NMR D2O Sample Preparation: Dilute analyte to ~25 mg/mL in d euterium oxide (D2O) containing TSP for 0 ppm reference and maleic acid as quantitative internal standard. Instrument: 400 MHz NMR spectrometer Parameters: Spectral width: at least containing -3 ppm through 13 ppm Pulse angle: 90o Delay between pulses: 45 seconds 1 H NMR: Methylone HCl; Lot N1P25; D2O; 400 MHz HDO 10 9 8 7 Maleic acid (ISTD) 6 5 4 3 2 TSP 1 1 1 1 2 1 3 3 7 6 5Chemical Shift4 (ppm) 3 2 1 0 4 7.5 3 2 5.0 1 2.5 1 1 1 2 1 3 3 0.5757.650 0.5507.4750.5257.425 7.000 6.100 5.025 2.8250.5752.775 0.5251.600 Page 2 of 4 4.2 Gas Chromatography/Mass Spectrometry Sample Preparation: Dilute analyte ~ 1 mg/mL base extracted into chloroform Instrument: Agilent gas chromatograph operated in split mode with MS detector Column: DB-1 MS (or equivalent); 30m x 0.25 mm x 0.25 mm Carrier Gas: Helium at 1 mL/min Temperatures: Injector: 280oC MSD transfer line: 280oC MS Source: 230oC MS Quad: 150oC Oven program: 1) 100oC initial temperature for 1.0 min 2) Ramp to 300oC at 12 oC/min 3) Hold final temperature for 9.0 min Injection Parameters: Split Ratio = 20:1, 1 mL injected MS Parameters: Mass scan range: 30-550 amu Threshold: 100 Tune file: stune.u Acquisition mode: scan Retention Time: 9.462 min EI Mass Spectrum: Methylone HCl; Lot N1P25 ] 58 6 [x 10 Intensity 0.50 0.25 56 63 65 121 30 149 42 91 74 135 162 176 189 207 40 60 80 100 120 140 160 180 200 m/z ] 4 30 42 56 58 63 65 91 121 149 [x 10 135 74 162 176 189 207 Intensity 40 60 80 100 120 140 160 180 200 m/z Page 3 of 4 4.3 INFRARED SPECTROSCOPY (FTIR) Insrument: FTIR with diamond ATR attachment (3 bounce) Scan Parameters: Number of scans: 32 Number of background scans: 32 Resolution: 4 cm-1 Sample gain: 8 Aperture: 150 FTIR ATR (Diamond, 3 Bounce): Methylone HCl; Lot N1P25 2459 %Transmittance 2908 80 584 1348 519 1500 2731 1603 1120 72 837 1421 741 1028 1676 879 64 928 1450 1090 56 1259 48 3500 3000 2500 2000 1500 Wavenumber (cm-1) 471 1169 1196 %Transmittance 652 422 1308 80 584 1383 1298 1348 451 519 1500 715 1603 1120 768 820 1470 808 72 837 1007 1421 741 991 1036 1028 1676 879 887 64 928 1450 1090 56 1259 48 1700 1600 1500 1400 1300 1200 1100 1000 900 800 700 Wavenumber (cm-1) Page 4 of 4.
Recommended publications
  • Recommended Methods for the Identification and Analysis of Synthetic Cathinones in Seized Materialsd
    Recommended methods for the Identification and Analysis of Synthetic Cathinones in Seized Materials (Revised and updated) MANUAL FOR USE BY NATIONAL DRUG ANALYSIS LABORATORIES Photo credits:UNODC Photo Library; UNODC/Ioulia Kondratovitch; Alessandro Scotti. Laboratory and Scientific Section UNITED NATIONS OFFICE ON DRUGS AND CRIME Vienna Recommended Methods for the Identification and Analysis of Synthetic Cathinones in Seized Materials (Revised and updated) MANUAL FOR USE BY NATIONAL DRUG ANALYSIS LABORATORIES UNITED NATIONS Vienna, 2020 Note Operating and experimental conditions are reproduced from the original reference materials, including unpublished methods, validated and used in selected national laboratories as per the list of references. A number of alternative conditions and substitution of named commercial products may provide comparable results in many cases. However, any modification has to be validated before it is integrated into laboratory routines. ST/NAR/49/REV.1 Original language: English © United Nations, March 2020. All rights reserved, worldwide. 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. Mention of names of firms and commercial products does not imply the endorse- ment of the United Nations. This publication has not been formally edited. Publishing production: English, Publishing and Library Section, United Nations Office at Vienna. Acknowledgements The Laboratory and Scientific Section of the UNODC (LSS, headed by Dr. Justice Tettey) wishes to express its appreciation and thanks to Dr.
    [Show full text]
  • 2015-02 Toxicology Rapid Testing Panel
    SOUTH CAROLINA LAW ENFORCEMENT DIVISION NIKKI R. HALEY MARK A. KEEL Governor Chief FORENSIC SERVICES LABORATORY CUSTOMER NOTICE 2015-02 REGARDING TOXICOLOGY RAPID TESTING PANEL August 12, 2015 This notice is to inform the Coroners of South Carolina of a new testing panel available through the SLED Toxicology Department. On Monday, August 17th, the Toxicology Department will begin offering both a Rapid Testing Panel in addition to the already available Expanded Testing Panel. This Rapid Testing Panel is to be utilized in cases where the Expanded Testing Panel is not warranted, specifically where a cause of death has already been established. The Rapid Testing Panel will consist of volatiles analysis, to include, ethanol, acetone, isopropanol and methanol, drug screens, and drug confirmation/quantitation of positive screens. The cases assigned to the Rapid Testing Panel will have an expedited turnaround time. Targeted turn around times will be two weeks for negative cases and six weeks or less for positive cases. While every effort will be made to adhere to these time frames, additional time may be required on occasion due to the nature of postmortem samples. Submitters will be notified if there is a problem with a particular sample. Please see attachment regarding specifically which substances are covered by the Rapid Testing Panel and the Expanded Testing Panel. As always, a detailed case history and list of drugs suspected is appreciated. Rapid Panel and Expanded Panel will be choices available in iLAB. Please contact Lt. Dustin Smith (803-896-7385) with additional questions. ALI-359-T An Accredited Law Enforcement Agency P.O.
    [Show full text]
  • 3,4-Methylenedioxymethcathinone (Methylone) [“Bath Salt,” Bk-MDMA, MDMC, MDMCAT, “Explosion,” “Ease,” “Molly”] December 2019
    Drug Enforcement Administration Diversion Control Division Drug & Chemical Evaluation Section 3,4-Methylenedioxymethcathinone (Methylone) [“Bath salt,” bk-MDMA, MDMC, MDMCAT, “Explosion,” “Ease,” “Molly”] December 2019 Introduction: discriminate DOM from saline. 3,4-Methylenedioxymethcathinone (methylone) is a Because of the structural and pharmacological similarities designer drug of the phenethylamine class. Methylone is a between methylone and MDMA, the psychoactive effects, adverse synthetic cathinone with substantial chemical, structural, and health risks, and signs of intoxication resulting from methylone pharmacological similarities to 3,4-methylenedioxymeth- abuse are likely to be similar to those of MDMA. Several chat amphetamine (MDMA, ecstasy). Animal studies indicate that rooms discussed pleasant and positive effects of methylone when methylone has MDMA-like and (+)-amphetamine-like used for recreational purpose. behavioral effects. When combined with mephedrone, a controlled schedule I substance, the combination is called User Population: “bubbles.” Other names are given in the above title. Methylone, like other synthetic cathinones, is a recreational drug that emerged on the United States’ illicit drug market in 2009. It is perceived as being a ‘legal’ alternative to drugs of Licit Uses: Methylone is not approved for medical use in the United abuse like MDMA, methamphetamine, and cocaine. Evidence States. indicates that youths and young adults are the primary users of synthetic cathinone substances which include methylone. However, older adults also have been identified as users of these Chemistry: substances. O H O N CH3 Illicit Distribution: CH O 3 Law enforcement has encountered methylone in the United States as well as in several countries including the Netherlands, Methylone United Kingdom, Japan, and Sweden.
    [Show full text]
  • (19) United States (12) Patent Application Publication (10) Pub
    US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist.
    [Show full text]
  • 10.30.19 Didactic
    STIMULANTS PART II Michael H. Baumann, Ph.D. Designer Drug Research Unit (DDRU), Intramural Research Program, NIDA, NIH Baltimore, MD 21224 Chronology of Stimulant Misuse 1. 2000s: Methamphetamine 2. 2010s: Bath Salts 3. Summary 2 Topics Covered for Each Substance Chemistry Formulations and Methods of Use Pharmacokinetics and Metabolism Desired and Adverse Effects Chronic and Withdrawal Effects Neurobiology Treatments 2000s: Methamphetamine Methamphetamine, a synthetic stimulant 5 Formulations and Methods of Use Methamphetamine (i.e., Ice or Crystal) Smoking using pipes Methamphetamine HCl Intravenous injection of solutions using needle and syringe Intranasal snorting of crystals Pharmacokinetics and Metabolism Pharmacokinetics Smoked and intravenous drugs reach brain within seconds Intranasal drug reaches brain within minutes Much longer half-life than cocaine Metabolism N-demethylation to form amphetamine (bioactive) Hydroxylation to form inactive metabolites Desired Effects Enhanced Mood and Euphoria Increased Attention and Alertness Decreased Need for Sleep Appetite Suppression Sexual Arousal Adverse Effects Psychosis Arrhythmias, Palpitations, Heart Attack Hypertension, Stroke Hyperthermia, Rhabdomyolysis Multisystem Organ Failure 11 www.facesofmeth.us. “METH Mouth” 12 Molecular Sites of Action SLC6 Monoamine Transporters Dopamine transporter (DAT) Norepinephrine transporter (NET) 5-HT transporter (SERT) Other sites Vesicular Monoamine Transporter 2 (VMAT2) Trace amine-associated receptors (TAAR1)
    [Show full text]
  • AGENDA Friday, September 9, 2016 7:00 A.M
    Needham Board of Health AGENDA Friday, September 9, 2016 7:00 a.m. – 9:00 a.m. Charles River Room – Public Services Administration Building 500 Dedham Avenue, Needham MA 02492 • 7:00 to 7:05 - Welcome & Review of Minutes (July 29 & August 29) • 7:05 to 7:30 - Director and Staff Reports (July & August) • 7:30 to 7:45 - Discussion about Proposed Plastic Bag Ban Christopher Thomas, Needham Resident • 7:45 to 7:50 - Off-Street Drainage Bond Discussion & Vote • 7:50 to 8:00 - Update on Wingate Pool Variance Application * * * * * * * * * * * * * Board of Health Public Hearing • 8:00 to 8:40 - Hearing for Proposed New or Amended BOH Regulations o Body Art o Synthetic Marijuana o Drug Paraphernalia • 8:40 to 8:50 - Board Discussion of Policy Positions • Other Items (Healthy Aging, Water Quality) • Next Meeting Scheduled for Friday October 14, 2016 • Adjournment (Please note that all times are approximate) 1471 Highland Avenue, Needham, MA 02492 781-455-7500 ext 511 (tel); 781-455-0892 (fax) E-mail: [email protected] Web: www.needhamma.gov/health NEEDHAM BOARD OF HEALTH July 29, 2016 MEETING MINUTES PRESENT: Edward V. Cosgrove, PhD, Chair, Jane Fogg, Vice-Chair, M.D., and Stephen Epstein, M.D STAFF: Timothy McDonald, Director, Donna Carmichael, Catherine Delano, Maryanne Dinell, Tara Gurge GUEST: Kevin Mulkern, Aquaknot Pools, Inc., Keith Mulkern, Aquaknot Pools, Inc., David Friedman, Wingate, Paul Humphreys, Michael Tomasello, Callahan, Inc. CONVENE: 7:00 a.m. – Public Services Administration Building (PSAB), 500 Dedham Avenue, Needham MA 02492 DISCUSSION: Call To Order – 7:06 a.m. – Dr. Cosgrove, Chairman APPROVE MINUTES: Upon motion duly made and seconded, the minutes of the BOH meeting of June 17, 2016 were approved as submitted.
    [Show full text]
  • Application of High Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances Joshua Zolton Seither [email protected]
    Florida International University FIU Digital Commons FIU Electronic Theses and Dissertations University Graduate School 4-25-2018 Application of High Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances Joshua Zolton Seither [email protected] DOI: 10.25148/etd.FIDC006565 Follow this and additional works at: https://digitalcommons.fiu.edu/etd Part of the Chemistry Commons Recommended Citation Seither, Joshua Zolton, "Application of High Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances" (2018). FIU Electronic Theses and Dissertations. 3823. https://digitalcommons.fiu.edu/etd/3823 This work is brought to you for free and open access by the University Graduate School at FIU Digital Commons. It has been accepted for inclusion in FIU Electronic Theses and Dissertations by an authorized administrator of FIU Digital Commons. For more information, please contact [email protected]. FLORIDA INTERNATIONAL UNIVERSITY Miami, Florida APPLICATION OF HIGH RESOLUTION MASS SPECTROMETRY FOR THE SCREENING AND CONFIRMATION OF NOVEL PSYCHOACTIVE SUBSTANCES A dissertation submitted in partial fulfillment of the requirements for the degree of DOCTOR OF PHILOSOPHY in CHEMISTRY by Joshua Zolton Seither 2018 To: Dean Michael R. Heithaus College of Arts, Sciences and Education This dissertation, written by Joshua Zolton Seither, and entitled Application of High- Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances, having been approved in respect to style and intellectual content, is referred to you for judgment. We have read this dissertation and recommend that it be approved. _______________________________________ Piero Gardinali _______________________________________ Bruce McCord _______________________________________ DeEtta Mills _______________________________________ Stanislaw Wnuk _______________________________________ Anthony DeCaprio, Major Professor Date of Defense: April 25, 2018 The dissertation of Joshua Zolton Seither is approved.
    [Show full text]
  • Written Witness Statement for U.S. Sentencing Commission's Public
    STATEMENT OF TERRENCE L. BOOS, PH.D. SECTION CHIEF DRUG AND CHEMICAL EVALUATION SECTION DIVERSION CONTROL DIVISION DRUG ENFORCEMENT ADMINISTRATION and CASSANDRA PRIOLEAU, PH.D. DRUG SCIENCE SPECIALIST DRUG AND CHEMICAL EVALUATION SECTION DIVERSION CONTROL DIVISION DRUG ENFORCEMENT ADMINISTRATION - - - BEFORE THE UNITED STATES SENTENCING COMMISSION - - - HEARING ON SENTENCING POLICY FOR SYNTHETIC DRUGS - - - OCTOBER 4, 2017 WASHINGTON, D.C. 1 Introduction New Psychoactive Substances (NPS) are substances trafficked as alternatives to well- studied controlled substances of abuse. NPS have demonstrated adverse health effects such as paranoia, psychosis, and seizures to name a few. Cathinones, cannabinoids, and fentanyl-related substances are the most common NPS drug classes encountered on the illicit drug market, all with negative consequences for the user to include serious injury and death. Our early experience saw substances being introduced from past research efforts in an attempt to evade controls. This has evolved to NPS manufacturers structurally altering substances at a rapid pace with unknown outcomes to targeting specific user populations. These substances represent an unprecedented level of diversity and consequences. Due to clandestine manufacture and unscrupulous trafficking, the user is at great risk. A misconception exists that these substances carry a lower risk of harm In reality, published reports from law enforcement, emergency room physicians and scientists, accompanied with autopsies from medical examiners, have clearly demonstrated the harmful and potentially deadly consequences of using synthetic cathinones. These substances are introduced in an attempt to circumvent drug controls and the recent flood of NPS remains a challenge for law enforcement and public health. The United Nations Office on Drugs and Crime reported over 700 NPS encountered.1 The manufacturers and traffickers make minor changes in the chemical structure of known substances of abuse and maintain the pharmacological effect.
    [Show full text]
  • Model Scheduling New/Novel Psychoactive Substances Act (Third Edition)
    Model Scheduling New/Novel Psychoactive Substances Act (Third Edition) July 1, 2019. This project was supported by Grant No. G1799ONDCP03A, awarded by the Office of National Drug Control Policy. Points of view or opinions in this document are those of the author and do not necessarily represent the official position or policies of the Office of National Drug Control Policy or the United States Government. © 2019 NATIONAL ALLIANCE FOR MODEL STATE DRUG LAWS. This document may be reproduced for non-commercial purposes with full attribution to the National Alliance for Model State Drug Laws. Please contact NAMSDL at [email protected] or (703) 229-4954 with any questions about the Model Language. This document is intended for educational purposes only and does not constitute legal advice or opinion. Headquarters Office: NATIONAL ALLIANCE FOR MODEL STATE DRUG 1 LAWS, 1335 North Front Street, First Floor, Harrisburg, PA, 17102-2629. Model Scheduling New/Novel Psychoactive Substances Act (Third Edition)1 Table of Contents 3 Policy Statement and Background 5 Highlights 6 Section I – Short Title 6 Section II – Purpose 6 Section III – Synthetic Cannabinoids 13 Section IV – Substituted Cathinones 19 Section V – Substituted Phenethylamines 23 Section VI – N-benzyl Phenethylamine Compounds 25 Section VII – Substituted Tryptamines 28 Section VIII – Substituted Phenylcyclohexylamines 30 Section IX – Fentanyl Derivatives 39 Section X – Unclassified NPS 43 Appendix 1 Second edition published in September 2018; first edition published in 2014. Content in red bold first added in third edition. © 2019 NATIONAL ALLIANCE FOR MODEL STATE DRUG LAWS. This document may be reproduced for non-commercial purposes with full attribution to the National Alliance for Model State Drug Laws.
    [Show full text]
  • 4-Fluoroamphetamine (4-FA) Critical Review Report Agenda Item 4.3
    4-Fluoroamphetamine (4-FA) Critical Review Report Agenda Item 4.3 Expert Committee on Drug Dependence Thirty-ninth Meeting Geneva, 6-10 November 2017 39th ECDD (2017) Agenda item 4.3 4-FA Contents Acknowledgements.................................................................................................................................. 4 Summary...................................................................................................................................................... 5 1. Substance identification ....................................................................................................................... 6 A. International Nonproprietary Name (INN).......................................................................................................... 6 B. Chemical Abstract Service (CAS) Registry Number .......................................................................................... 6 C. Other Chemical Names ................................................................................................................................................... 6 D. Trade Names ....................................................................................................................................................................... 6 E. Street Names ....................................................................................................................................................................... 6 F. Physical Appearance ......................................................................................................................................................
    [Show full text]
  • Neurotoxicity Screening of New Psychoactive Substances (NPS): Effects on Neuronal Activity in Rat Cortical Cultures Using Microelectrode Arrays (MEA)
    Accepted Manuscript Title: Neurotoxicity screening of new psychoactive substances (NPS): effects on neuronal activity in rat cortical cultures using microelectrode arrays (MEA) Authors: Anne Zwartsen, Laura Hondebrink, Remco HS Westerink PII: S0161-813X(18)30086-X DOI: https://doi.org/10.1016/j.neuro.2018.03.007 Reference: NEUTOX 2313 To appear in: NEUTOX Received date: 25-10-2017 Revised date: 9-3-2018 Accepted date: 19-3-2018 Please cite this article as: Zwartsen A, Hondebrink L, Westerink RH, Neurotoxicity screening of new psychoactive substances (NPS): effects on neuronal activity in rat cortical cultures using microelectrode arrays (MEA), Neurotoxicology (2010), https://doi.org/10.1016/j.neuro.2018.03.007 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Neurotoxicity screening of new psychoactive substances (NPS): effects on neuronal activity in rat cortical cultures using microelectrode arrays (MEA) Anne Zwartsen a,b, Laura Hondebrink b, Remco HS Westerink a,* a Neurotoxicology Research Group, Division Toxicology, Institute for Risk Assessment Sciences (IRAS), Faculty of Veterinary Medicine, Utrecht University, Utrecht, The Netherlands. b Dutch Poisons Information Center (DPIC), University Medical Center Utrecht, Utrecht University, Utrecht, The Netherlands. * Corresponding author: Dr. Remco HS Westerink. Neurotoxicology Research Group, Division Toxicology, Institute for Risk Assessment Sciences (IRAS), Faculty of Veterinary Medicine, Utrecht University, P.O.
    [Show full text]
  • The Designer Methcathinone Analogs, Mephedrone and Methylone, Are Substrates for Monoamine Transporters in Brain Tissue
    Neuropsychopharmacology (2012) 37, 1192–1203 & 2012 American College of Neuropsychopharmacology. All rights reserved 0893-133X/12 www.neuropsychopharmacology.org The Designer Methcathinone Analogs, Mephedrone and Methylone, are Substrates for Monoamine Transporters in Brain Tissue ,1 1 1 1 2 Michael H Baumann* , Mario A Ayestas Jr , John S Partilla , Jacqueline R Sink , Alexander T Shulgin , 2 3 1 4 5 Paul F Daley , Simon D Brandt , Richard B Rothman , Arnold E Ruoho and Nicholas V Cozzi 1 Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, 2 3 MD, USA; Alexander Shulgin Research Institute, Lafayette, CA, USA; School of Pharmacy and Biomolecular Sciences, Liverpool John Moores 4 University, Liverpool, UK; Department of Neuroscience and the UW Eye Research Institute, University of Wisconsin School of Medicine and 5 Public Health, Madison, WI, USA; Neuropharmacology Laboratory, Department of Cell and Regenerative Biology, University of Wisconsin School of Medicine and Public Health, Madison, WI, USA The nonmedical use of ‘designer’ cathinone analogs, such as 4-methylmethcathinone (mephedrone) and 3,4-methylenedioxymethcathi- none (methylone), is increasing worldwide, yet little information is available regarding the mechanism of action for these drugs. Here, we employed in vitro and in vivo methods to compare neurobiological effects of mephedrone and methylone with those produced by the structurally related compounds, 3,4-methylenedioxymethamphetamine (MDMA) and methamphetamine. In vitro release assays using rat brain synaptosomes revealed that mephedrone and methylone are nonselective substrates for plasma membrane monoamine transporters, similar to MDMA in potency and selectivity. In vivo microdialysis in rat nucleus accumbens showed that i.v.
    [Show full text]