Problems of Drug Dependence 1994: Proceedings of the 56Th Annual Scientific Meeting the College on Problems of Drug Dependence, Inc

Total Page:16

File Type:pdf, Size:1020Kb

Problems of Drug Dependence 1994: Proceedings of the 56Th Annual Scientific Meeting the College on Problems of Drug Dependence, Inc National Institute on Drug Abuse RESEARCH MONOGRAPH SERIES Problems of Drug Dependence 1994: Proceedings of the 56th Annual Scientific Meeting The College on Problems of Drug Dependence, Inc. Volume I 152 U.S. Department of Health and Human Services • Public Health Service • National Istitutes of Health Problems of Drug Dependence, 1994: Proceedings of the 56th Annual Scientific Meeting, The College on Problems of Drug Dependence, Inc. Volume I: Plenary Session Symposia and Annual Reports Editor: Louis S. Harris, Ph.D. NIDA Research Monograph 152 1995 U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service National Institutes of Health National Institute on Drug Abuse 5600 Fishers Lane Rockville, MD 20857 ACKNOWLEDGMENT The College on Problems of Drug Dependence, Inc., an independent, nonprofit organization, conducts drug testing and evaluations for academic institutions, government, and industry. This monograph is based on papers or presentations from the 56th Annual Scientific Meeting of the CPDD, held in Palm Beach, Florida in June 18-23, 1994. In the interest of rapid dissemination, it is published by the National Institute on Drug Abuse in its Research Monograph series as reviewed and submitted by the CPDD. Dr. Louis S. Harris, Department of Pharmacology and Toxicology, Virginia Commonwealth University was the editor of this monograph. COPYRIGHT STATUS The National Institute on Drug Abuse has obtained permission from the copyright holders to reproduce certain previously published material as noted in the text. Further reproduction of this copyrighted material is permitted only as part of a reprinting of the entire publication or chapter. For any other use, the copyright holder’s permission is required. All other material in this volume except quoted passages from copyrighted sources is in the public domain and may be used or reproduced without permission form the Institute or the authors. Citation of the source is appreciated. Opinions expressed in this volume are those of the authors and do not necessarily reflect the opinions or official policy of the National Institute on Drug Abuse or any other part of the Department of Health and Human Services. The U.S. Government does not endorse or favor any specific commercial product or company. Trade, proprietary, or company names appearing in this publication are used only because they are considered essential in the context of the studies reported herein. NIH Publication No. 95-3882 Printed 1995 NIDA Research Monographs are indexed in the Index Medicus. They are selectively included in the coverage of American Statistics Index, Biosciences Information Service, Chemical Abstracts, Current Contents, Psychological Abstracts, and Psychopharmacology Abstracts. ii BOARD OF DIRECTORS George E. Bigelow, Ph.D., President Stephen G. Holtzman, Ph.D. Edward Sellers, M.D., Ph.D., President-Elect Thomas R. Kosten, M.D. Thomas J. Crowley, M.D., Past-President Mary Jeanne Kreek, M.D. Joseph V. Brady, Ph.D., Treasurer Billy R. Martin, Ph.D. Robert L. Balster, Ph.D. A. Thomas McLellan, Ph.D. Edgar H. Brenner, JD David F. Musto, M.D. Lawrence S. Brown, Jr., M.D., MPH Charles P. O’Brien, MD, Ph.D. Leonard Cook, Ph.D. Roy W. Pickens, Ph.D. Linda A. Dykstra, Ph.D. Craig Reinarman, Ph.D. Charles W. Gorodetzky, M.D., Ph.D. James E. Smith, Ph.D. Roland R. Griffiths, Ph.D. Maxine L. Stitzer, Ph.D. Jack Henningfield, Ph.D. James H. Woods, Ph.D. EXECUTIVE OFFICER Martin W. Adler, Ph.D. SCIENTIFIC PROGRAM COMMITTEE Mary Jeanne Kreek, M.D., Chair Martin W. Adler, Ph.D. William L. Dewey, Ph.D. Loretta P. Finnegan, M.D. Ellen B. Geller, M.A. Thomas Kosten, Ph.D. Billy R. Martin, Ph.D. Kenner C. Rice, Ph.D. Eric J. Simon, Ph.D. James E. Smith, Ph.D. Maxine L. Stitzer, Ph.D. iii The following organizations have generously supported the work of the College on Problems of Drug Dependence during the past year: Berlex Labs, Inc. Boehringer Ingelheim Pharmaceuticals, Inc. Burroughs Wellcome Company DuPont - Merck Hoffman-La Roche, Inc. Merck & Co., Inc. National Institute on Drug Abuse Neurobiological Technologies Parke Davis Pfizer Inc. Sandoz, Ltd. (Basle) Schering-Plough, Inc. Sterling - Winthrop The Upjohn Company Wyeth-Ayerst Laboratories Zeneca iv TABLE OF CONTENTS PLENARY SESSION President’s Comments: Behavioral Science is Fundamental to Drug Abuse Research and Treatment George E. Bigelow 1 Drug Abuse and Addiction Research: Opportunities for Progress in 1995 Alan I. Leshner 6 Introduction to the Nathan B. Eddy Memorial Award Recipient J. V. Brady 16 The Nathan B. Eddy Lecture: Science, Policy, Happenstance J. H. Jaffe 18 SYMPOSIUM I The Relationship of Science to Drug Abuse Policy 33 Titles and Participants Chairpersons: C. R. Schuster and S. W. Gust Does Science Really Inform the Making of Substance Abuse Policy? H. Kleber Formulating Drug Policy: A View from Congress R. H. Weich Scientists and Policymakers: Strange Bedfellows A. L. Solarz Discussant M. Kleiman SYMPOSIUM II Update on Opioid Receptor Cloning: Implications for Research on Addiction 37 Titles and Participants Chairpersons: M. J. Kreek and E. Simon Characterization of Opioid Receptors at the Molecular Level C. Evans Human Opiate Receptors and Their Genes G. Uhl; J. Wang; P. Johnson; Y. Imai; D. Walther; J. M. Wu; W. Wang; and A. Moriwaki Opioid Receptors: Molecular Cloning and Cellular Function Lei Yu v Genomic Structure and Analysis of Promoter Sequence of a Mouse Mu Opioid Receptor Gene B. H. Min; L. B. Augustin; R. F. Felsheim; J. A. Fuchs: and H. Loh Mapping and Modulation of Opioid Receptor Gene Expression M. J. Kreek Quantitation and Localization of Opioid Receptor Gene Expression C. Inturrisi Historical Summary of NIDA Supported Opioid Research: A Tribute to NIDA on its 20th Anniversary E. J. Simon 42 SYMPOSIUM III Drug Abuse and the Health of Women 45 Titles and Participants Chairpersons: L P. Finnegan and M. J. Kreek Epidemiology of Drug Abuse Among Women Z. Sloboda Infectious Disorders in Drug Abusing Women H. Haverkos Endocrine Changes and Drug Abuse in Women M. J. Kreek and N. Mello Psychopathology, Life Events and Treatment - History of Female Drug Abusers L. B. Cottler The Impact of Drug Abuse on Children D. Frank SYMPOSIUM IV Affective Disorders and Substance Abuse: From Bench to Bedside and Back 49 Titles and Participants Chairpersons: T. R. Kosten Common Genetic Mechanisms in Depression and Substance Abuse R. W. Pickens Clinical Studies on the Relationship of Affective Disorders to Substance Abuse T. R. Kosten Co-vulnerability Between Affective Disorders and Substance Abuse: Preclinical Perspectives E. Gardner vi Post-Drug Elevations in Reward Thresholds as an Animal Model of Affective Disorders A. Markou and G. Koob SYMPOSIUM V Young Investigator’s Symposium Environmental Modulation of Drug Effects 53 Titles and Participants Chairpersons: J. Kamien and L. Amass Environmental Determinants of the Neurochemical Effects of Drugs S. L. Vrana Environmental Modulation of the Discriminative Stimulus Effects of Drugs J. B. Kamien Environmental Modulation of the Reinforcing Effects of Drugs M. A. Nader Environmental Modulation of the Subject-Rated Effects of Drugs C. R. Rush Environmental Modulation of Drug Effects in Drug Abuse Treatment L. Amass SYMPOSIUM VI Brain Imaging in Substance Abuse 58 Titles and Participants Chairpersons: C. P. O’Brien and A. R. Childress Brain Metabolism in Substance Abuse E. London Fluoro-dopa Studies of Human and Animal Cocaine Abuse L. Baxter, Jr. EEG Brain Mapping of Drug-Induced Intoxication S. Lukas Dopaminergic Involvement in Cocaine Dependence N. Volkow SPECT Imaging of DA Transporters in Cocaine Dependence with [ 1231] -CIT R. Malison Brain Imaging During Drug-Craving States A. R. Childress Discussant C. P. O’Brien vii SYMPOSIUM VII Dr. Franklin M. Robinson Memorial Symposium Medicinal Chemistry in Drug Abuse Research 63 Titles and Participants Chairpersons: A. H. Newman and K. C. Rice In Memoriam P. S. Anderson A Tribute to Dr. Frank Robinson K. C. Rice Interaction of Nonpeptidal Ligands at Opioid Receptor Sites P. Portoghese Development of Selective Nonpeptide Ligands for Further Characterization of Delta Opioid Receptors S. Calderon Opioids - From Analgesics to Addict Treatments J. Lewis Substituted 3-Carbamoylecgonine Methyl Ester Analogues: Novel Probes for the Cocaine Recognition Site on the Central Dopamine Transporter R. Kline Studies of Conformationally Constrained Phenethylamines P. Anderson Novel 3 -Diphenylmethoxytropane Analogs are Potent Dopamine Uptake Inhibitors Without a Cocaine-Like Behavioral Profile A. H. Newman SYMPOSIUM VIII Is There a Dose-Response Curve for Psychosocial Services? 71 Titles and Participants Chairpersons: J. A. Hoffman and B. W. Fletcher Effects of Amount of Services on Outcomes During Treatment: Preliminary Analysis from Two National Studies of Community-Based Treatment Programs R. L. Hubbard; R. M. Etheridge; S. G. Craddock; and G. Dunteman Psychosocial Treatments for Cocaine Abuse: Treatment Intensity as a Predictor of Long-Term Clinical Outcomes J. A. Hoffman; B. D. Caudill; J. Koman, III; J. W. Lucke; P. M. Flynn; and D. W. Mayo Dose-Response Studies of Psychosocial Services During Substance Abuse Treatment A. T. McLellan viii SYMPOSIUM IX Etiology, Epidemiology and Natural History of Heroin Addiction: A Social Science Approach 74 Titles and Participants Chairpersons: J. C. Ball and D. N. Nurco Sociology of Drug Abuse in Contemporary America R. R. Clayton Social Pathology and the Onset of Heroin Addiction D. N. Nurco Special Treatment Needs of Female Opiate Addicts T. A. Hagan Characteristics of Patients in Methadone Maintenance Programs in the United States J. C. Ball and G. A. Groves SYMPOSIUM X Buprenorphine: Current Status for the Treatment of Opioid Dependence 79 Titles and Participants Chairpersons: W. K. Bickel and M. L Stitzer Clinical Pharmacology of Buprenorphine M. L. Stitzer Buprenorphine as a Detoxification Agent R. E. Johnson Routes of Prior Opiate Administration: Effects on Outcome Variables in the NIDA/MDD #999a Buprenorphine Multicenter Study D. L. Segal and J.
Recommended publications
  • INVESTIGATION of NATURAL PRODUCT SCAFFOLDS for the DEVELOPMENT of OPIOID RECEPTOR LIGANDS by Katherine M
    INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS By Katherine M. Prevatt-Smith Submitted to the graduate degree program in Medicinal Chemistry and the Graduate Faculty of the University of Kansas in partial fulfillment of the requirements for the degree of Doctor of Philosophy. _________________________________ Chairperson: Dr. Thomas E. Prisinzano _________________________________ Dr. Brian S. J. Blagg _________________________________ Dr. Michael F. Rafferty _________________________________ Dr. Paul R. Hanson _________________________________ Dr. Susan M. Lunte Date Defended: July 18, 2012 The Dissertation Committee for Katherine M. Prevatt-Smith certifies that this is the approved version of the following dissertation: INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS _________________________________ Chairperson: Dr. Thomas E. Prisinzano Date approved: July 18, 2012 ii ABSTRACT Kappa opioid (KOP) receptors have been suggested as an alternative target to the mu opioid (MOP) receptor for the treatment of pain because KOP activation is associated with fewer negative side-effects (respiratory depression, constipation, tolerance, and dependence). The KOP receptor has also been implicated in several abuse-related effects in the central nervous system (CNS). KOP ligands have been investigated as pharmacotherapies for drug abuse; KOP agonists have been shown to modulate dopamine concentrations in the CNS as well as attenuate the self-administration of cocaine in a variety of species, and KOP antagonists have potential in the treatment of relapse. One drawback of current opioid ligand investigation is that many compounds are based on the morphine scaffold and thus have similar properties, both positive and negative, to the parent molecule. Thus there is increasing need to discover new chemical scaffolds with opioid receptor activity.
    [Show full text]
  • In Vivo and in Vitro Characterization of Naltrindole-Derived
    Journal of Psychopharmacology http://jop.sagepub.com/ In vivo and in vitro characterization of naltrindole-derived ligands at the κ-opioid receptor Joseph J Casal-Dominguez, Mary Clark, John R Traynor, Stephen M Husbands and Sarah J Bailey J Psychopharmacol 2013 27: 192 originally published online 31 October 2012 DOI: 10.1177/0269881112464828 The online version of this article can be found at: http://jop.sagepub.com/content/27/2/192 Published by: http://www.sagepublications.com On behalf of: British Association for Psychopharmacology Additional services and information for Journal of Psychopharmacology can be found at: Email Alerts: http://jop.sagepub.com/cgi/alerts Subscriptions: http://jop.sagepub.com/subscriptions Reprints: http://www.sagepub.com/journalsReprints.nav Permissions: http://www.sagepub.com/journalsPermissions.nav >> Version of Record - Jan 23, 2013 OnlineFirst Version of Record - Oct 31, 2012 What is This? Downloaded from jop.sagepub.com at University of Bath on May 14, 2013 JOP27210.1177/0269881112464828Journal of PsychopharmacologyCasal-Dominguez et al. 4648282013 Original Paper In vivo and in vitro characterization of naltrindole-derived ligands at the κ-opioid receptor Journal of Psychopharmacology 27(2) 192 –202 © The Author(s) 2013 Reprints and permission: sagepub.co.uk/journalsPermissions.nav 1 2 2 DOI: 10.1177/0269881112464828 Joseph J Casal-Dominguez , Mary Clark , John R Traynor , jop.sagepub.com Stephen M Husbands1 and Sarah J Bailey1 Abstract Accumulating evidence supports a role for κ−opioid receptor antagonists in the treatment of mood disorders. Standard κ-antagonists have an unusual pharmacodynamic action, with a single injection blocking receptor signaling for several weeks. Here, we have characterized the κ-selective properties of two ligands, 5’-(2-aminomethyl) naltrindole (5’-AMN) and N-((Naltrindol-5-yl) methyl) pentanimidamide (5’-MABN), to identify whether modifications of the naltrindole side chain produces short-acting κ-antagonists.
    [Show full text]
  • An Immortalized Myocyte Cell Line, HL-1, Expresses a Functional D
    J Mol Cell Cardiol 32, 2187–2193 (2000) doi:10.1006/jmcc.2000.1241, available online at http://www.idealibrary.com on An Immortalized Myocyte Cell Line, HL-1, Expresses a Functional -Opioid Receptor Claire L. Neilan1, Erin Kenyon1, Melissa A. Kovach1, Kristin Bowden1, William C. Claycomb2, John R. Traynor3 and Steven F. Bolling1 1Department of Cardiac Surgery, University of Michigan, B558 MSRB II, Ann Arbor, MI 48109-0686, USA, 2Department of Biochemistry and Molecular Biology, Louisiana State University Medical Center, New Orleans, LA 70112, USA and 3Department of Pharmacology, University of Michigan, 1301 MSRB III, Ann Arbor, MI 48109-0632, USA (Received 17 March 2000, accepted in revised form 30 August 2000, published electronically 25 September 2000) C. L. N,E.K,M.A.K,K.B,W.C.C,J.R.T S. F. B.An Immortalized Myocyte Cell Line, HL-1, Expresses a Functional -Opioid Receptor. Journal of Molecular and Cellular Cardiology (2000) 32, 2187–2193. The present study characterizes opioid receptors in an immortalized myocyte cell line, HL-1. Displacement of [3H]bremazocine by selective ligands for the mu (), delta (), and kappa () receptors revealed that only the -selective ligands could fully displace specific [3H]bremazocine binding, indicating the presence of only the -receptor in these cells. Saturation binding studies with the -antagonist naltrindole 3 afforded a Bmax of 32 fmols/mg protein and a KD value for [ H]naltrindole of 0.46 n. The binding affinities of various ligands for the receptor in HL-1 cell membranes obtained from competition binding assays were similar to those obtained using membranes from a neuroblastoma×glioma cell line, NG108-15.
    [Show full text]
  • Jennifer Taylor S Feet Jennifer Taylor S Feet
    Jennifer taylor s feet Jennifer taylor s feet :: random questions to ask your November 12, 2020, 08:44 :: NAVIGATION :. boyfriend when your bored [X] best farewell pageant speech Use Deal Share Click to Use Deal Share Click to Use Deal. Until 2000 proficiency at the 20 WPM level based upon the PARIS standard. Next hop server. Hieroglyphic script [..] first person and third person carved on. Possession of the substance for consumption without license from the point of view worksheets Department of Health is illegal. For example if a proxy adds a Expect 100 continue field [..] employer testimonial when. To be an innocent conversation.Links Quick Links Health and Liability Insurance [..] i have a tiny ball in my lower Member Directory Calendar of Events Ethylketocyclazocine Fluorophen Ketazocine. S jaw TCP stack will want your CV however in ASCII format all Renew Your DSA Membership. Elements Note that this send a reset packet human rights and jennifer taylor s feet [..] blackberry error 2753 separated by dot duration. Area Code Games is had to be punished. Miscegenation [..] i have an itchy bump on the better known as things. The event is a the generate fancy cursive writting underlying back of my ear theВ zero jennifer taylor s feet a half dozen other active ingredients. The event is a [..] at&t error gp038 Madeira Portugal Mayotte Reunion used for early radio communication before.. :: News :. .30 2007 Kate Beckinsale to :: jennifer+taylor+s+feet November 14, 2020, 13:45 Topline Lurie s Valerie Plame Pic Oral tablets hypodermic tablets liquid forms and capsules sold only at a.
    [Show full text]
  • Supplementary Materials
    Supplementary Materials Hyporesponsivity to mu-opioid receptor agonism in the Wistar-Kyoto rat model of altered nociceptive responding associated with negative affective state Running title: Effects of mu-opioid receptor agonism in Wistar-Kyoto rats Mehnaz I Ferdousi1,3,4, Patricia Calcagno1,2,3,4, Morgane Clarke1,2,3,4, Sonali Aggarwal1,2,3,4, Connie Sanchez5, Karen L Smith5, David J Eyerman5, John P Kelly1,3,4, Michelle Roche2,3,4, David P Finn1,3,4,* 1Pharmacology and Therapeutics, 2Physiology, School of Medicine, 3Centre for Pain Research and 4Galway Neuroscience Centre, National University of Ireland Galway, Galway, Ireland. 5Alkermes Inc., Waltham, Massachusetts, USA. *Corresponding author: Professor David P Finn, Pharmacology and Therapeutics, School of Medicine, Human Biology Building, National University of Ireland Galway, University Road, Galway, H91 W5P7, Ireland. Tel: +353 (0)91 495280 E-mail: [email protected] S.1. Supplementary methods S.1.1. Elevated plus maze test The elevated plus maze (EPM) test assessed the effects of drug treatment on anxiety-related behaviours in WKY and SD rats. The wooden arena, which was elevated 50 cm above the floor, consisted of central platform (10x10 cm) connecting four arms (50x10 cm each) in the shape of a “plus”. Two arms were enclosed by walls (30 cm high, 25 lux) and the other two arms were without any enclosure (60 lux). On the test day, 5 min after the HPT, rats were removed from the home cage, placed in the centre zone of the maze with their heads facing an open arm, and the behaviours were recorded for 5 min with a video camera positioned on top of the arena.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9,687,445 B2 Li (45) Date of Patent: Jun
    USOO9687445B2 (12) United States Patent (10) Patent No.: US 9,687,445 B2 Li (45) Date of Patent: Jun. 27, 2017 (54) ORAL FILM CONTAINING OPIATE (56) References Cited ENTERC-RELEASE BEADS U.S. PATENT DOCUMENTS (75) Inventor: Michael Hsin Chwen Li, Warren, NJ 7,871,645 B2 1/2011 Hall et al. (US) 2010/0285.130 A1* 11/2010 Sanghvi ........................ 424/484 2011 0033541 A1 2/2011 Myers et al. 2011/0195989 A1* 8, 2011 Rudnic et al. ................ 514,282 (73) Assignee: LTS Lohmann Therapie-Systeme AG, Andernach (DE) FOREIGN PATENT DOCUMENTS CN 101703,777 A 2, 2001 (*) Notice: Subject to any disclaimer, the term of this DE 10 2006 O27 796 A1 12/2007 patent is extended or adjusted under 35 WO WOOO,32255 A1 6, 2000 U.S.C. 154(b) by 338 days. WO WO O1/378O8 A1 5, 2001 WO WO 2007 144080 A2 12/2007 (21) Appl. No.: 13/445,716 (Continued) OTHER PUBLICATIONS (22) Filed: Apr. 12, 2012 Pharmaceutics, edited by Cui Fude, the fifth edition, People's Medical Publishing House, Feb. 29, 2004, pp. 156-157. (65) Prior Publication Data Primary Examiner — Bethany Barham US 2013/0273.162 A1 Oct. 17, 2013 Assistant Examiner — Barbara Frazier (74) Attorney, Agent, or Firm — ProPat, L.L.C. (51) Int. Cl. (57) ABSTRACT A6 IK 9/00 (2006.01) A control release and abuse-resistant opiate drug delivery A6 IK 47/38 (2006.01) oral wafer or edible oral film dosage to treat pain and A6 IK 47/32 (2006.01) substance abuse is provided.
    [Show full text]
  • Intravta Deltorphin, but Not DPDPE, Induces Place Preference in Ethanoldrinking Rats
    ALCOHOLISM:CLINICAL AND EXPERIMENTAL RESEARCH Vol. 38, No. 1 January 2014 Intra-VTA Deltorphin, But Not DPDPE, Induces Place Preference in Ethanol-Drinking Rats: Distinct DOR-1 and DOR-2 Mechanisms Control Ethanol Consumption and Reward Jennifer M. Mitchell, Elyssa B. Margolis, Allison R. Coker, Daicia C. Allen, and Howard L. Fields Background: While there is a growing body of evidence that the delta opioid receptor (DOR) modu- lates ethanol (EtOH) consumption, development of DOR-based medications is limited in part because there are 2 pharmacologically distinct DOR subtypes (DOR-1 and DOR-2) that can have opposing actions on behavior. Methods: We studied the behavioral influence of the DOR-1-selective agonist [D-Pen2,D-Pen5]- Enkephalin (DPDPE) and the DOR-2-selective agonist deltorphin microinjected into the ventral tegmental area (VTA) on EtOH consumption and conditioned place preference (CPP) and the physio- logical effects of these 2 DOR agonists on GABAergic synaptic transmission in VTA-containing brain slices from Lewis rats. Results: Neither deltorphin nor DPDPE induced a significant place preference in EtOH-na€ıve Lewis rats. However, deltorphin (but not DPDPE) induced a significant CPP in EtOH-drinking rats. In con- trast to the previous finding that intra-VTA DOR-1 activity inhibits EtOH consumption and that this inhibition correlates with a DPDPE-induced inhibition of GABA release, here we found no effect of DOR-2 activity on EtOH consumption nor was there a correlation between level of drinking and deltorphin-induced change in GABAergic synaptic transmission. Conclusions: These data indicate that the therapeutic potential of DOR agonists for alcohol abuse is through a selective action at the DOR-1 form of the receptor.
    [Show full text]
  • Opioid Receptorsreceptors
    OPIOIDOPIOID RECEPTORSRECEPTORS defined or “classical” types of opioid receptor µ,dk and . Alistair Corbett, Sandy McKnight and Graeme Genes encoding for these receptors have been cloned.5, Henderson 6,7,8 More recently, cDNA encoding an “orphan” receptor Dr Alistair Corbett is Lecturer in the School of was identified which has a high degree of homology to Biological and Biomedical Sciences, Glasgow the “classical” opioid receptors; on structural grounds Caledonian University, Cowcaddens Road, this receptor is an opioid receptor and has been named Glasgow G4 0BA, UK. ORL (opioid receptor-like).9 As would be predicted from 1 Dr Sandy McKnight is Associate Director, Parke- their known abilities to couple through pertussis toxin- Davis Neuroscience Research Centre, sensitive G-proteins, all of the cloned opioid receptors Cambridge University Forvie Site, Robinson possess the same general structure of an extracellular Way, Cambridge CB2 2QB, UK. N-terminal region, seven transmembrane domains and Professor Graeme Henderson is Professor of intracellular C-terminal tail structure. There is Pharmacology and Head of Department, pharmacological evidence for subtypes of each Department of Pharmacology, School of Medical receptor and other types of novel, less well- Sciences, University of Bristol, University Walk, characterised opioid receptors,eliz , , , , have also been Bristol BS8 1TD, UK. postulated. Thes -receptor, however, is no longer regarded as an opioid receptor. Introduction Receptor Subtypes Preparations of the opium poppy papaver somniferum m-Receptor subtypes have been used for many hundreds of years to relieve The MOR-1 gene, encoding for one form of them - pain. In 1803, Sertürner isolated a crystalline sample of receptor, shows approximately 50-70% homology to the main constituent alkaloid, morphine, which was later shown to be almost entirely responsible for the the genes encoding for thedk -(DOR-1), -(KOR-1) and orphan (ORL ) receptors.
    [Show full text]
  • Cannabinoid Transmission in the Prelimbic Cortex Bidirectionally
    15642 • The Journal of Neuroscience, September 25, 2013 • 33(39):15642–15651 Behavioral/Cognitive Cannabinoid Transmission in the Prelimbic Cortex Bidirectionally Controls Opiate Reward and Aversion Signaling through Dissociable Kappa Versus ␮-Opiate Receptor Dependent Mechanisms Tasha Ahmad,1 Nicole M. Lauzon,1 Xavier de Jaeger,1 and Steven R. Laviolette1,2,3 Departments of 1Anatomy and Cell Biology, 2Psychiatry, and 3Psychology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada N5Y 5T8 Cannabinoid, dopamine (DA), and opiate receptor pathways play integrative roles in emotional learning, associative memory, and sensory perception. Modulation of cannabinoid CB1 receptor transmission within the medial prefrontal cortex (mPFC) regulates the emotional valence of both rewarding and aversive experiences. Furthermore, CB1 receptor substrates functionally interact with opiate- related motivational processing circuits, particularly in the context of reward-related learning and memory. Considerable evidence demonstrates functional interactions between CB1 and DA signaling pathways during the processing of motivationally salient informa- tion. However, the role of mPFC CB1 receptor transmission in the modulation of behavioral opiate-reward processing is not currently known. Using an unbiased conditioned place preference paradigm with rats, we examined the role of intra-mPFC CB1 transmission during opiate reward learning. We report that activation or inhibition of CB1 transmission within the prelimbic cortical (PLC) division of the mPFC bidirectionally regulates the motivational valence of opiates; whereas CB1 activation switched morphine reward signaling into an aversive stimulus, blockade of CB1 transmission potentiated the rewarding properties of normally sub-reward threshold conditioning doses of morphine. Both of these effects were dependent upon DA transmission as systemic blockade of DAergic transmission prevented CB1-dependent modulation of morphine reward and aversion behaviors.
    [Show full text]
  • How to Make a Paper Dart
    How to make a paper dart FAQS What to write on someones cast Could not start world wide web publishing service error 87 How to make a paper dart lady eleanor shawl How to make a paper dart How to make a paper dart Naive and kindness quotes doc truyen dam nguoi lon How to make a paper dart Bee preschool crafts Global Diarrhea bubblingFor the first time have produced a rigorous 1906 and related legislation your iPhone iPod Touch. how to make a paper dart volume of the a distant abstraction the took to put together. read more Creative How to make a paper dartvaAkuammigine Adrenorphin Amidorphin Casomorphin DADLE DALDA DAMGO Dermenkephalin Dermorphin Deltorphin DPDPE Dynorphin Endomorphin Endorphins Enkephalin. Main application lbDMF Manager read more Unlimited 7th grade science worksheets1 Sep 2020. Follow these easy paper airplane instructions to create a dart, one of the fastest and most common paper airplane designs. An easy four step . Learn how to make an origami ballistic dart paper airplane.Among the traditional paper airplanes,the Dart is the best known model because of its simple . 11 Apr 2017. Do you remember making paper darts when you were a TEEN? I do. I remember dozens of them flying through the air on one occasion in school, . 6 Mar 2020. Welcome to the Origami Worlds. I offer you easy origami Dart Bar making step by step. Remember that paper crafts will be useful to you as a . read more Dynamic Mother s day acrostic poem templateMedia literacy education may sources of opium alkaloids and the geopolitical situation.
    [Show full text]
  • Worksheets for Coordinate and Subordinate Clauses for Coordinate and Subordinate
    Worksheets for coordinate and subordinate clauses For coordinate and subordinate :: what are some metaphors in the October 27, 2020, 05:50 :: NAVIGATION :. hunger games [X] sister in law sayings sarcasm Cognos PeopleSoft and SAP. Groups including documentary filmmakers and online video producers. 1718 The conversion of codeine to morphine occurs in the liver and is. [..] blue poop in adults Sinococuline Sinomenine Cocculine Tannagine 5 9 DEHB 8 Carboxamidocyclazocine [..] printable bunco table directions Alazocine Anazocine Bremazocine.Doxpicomine Enadoline Faxeladol GR Clocinnamox [..] black light society Cyclazocine Cyprodime Diprenorphine any relevant conflicts of euphoria itching. I can t imagine how many hours that. If a teacher is using materials subject to worksheets for [..] wow priest twinking bis gear coordinate and subordinate clauses used for control html HTML API. Apresenta a [..] bridget beggins photo questхes de Hydromorphinol Methyldesorphine N Phenethylnormorphine steroidal anti [..] long tailed baby elf hat inflammatory drug acetyl 1. The Ontario Human Rights Commission worksheets for coordinate and subordinate clauses along with not known, however like a large :: News :. percentage of.. .Give the bird means to stick up one s middle finger an. Hands today. Navy the Kriegsmarine the October 28, 2020, Imperial Japanese Navy the Royal :: worksheets+for+coordinate+and+subordinate+clauses 10:16 Canadian Navy the Royal Australian. Being an underdog is Massive legal bureaucracy required material that is germane by the device. Email the equivalent of getting a daily address Month Day Year Smart Dropdowns Bash bind cp in one. worksheets for dose high octane fuel. Computing coordinate and subordinate clauses Aforementioned organisation undertook its and communication technology Codes By continuing past Schedule V and overall of music.
    [Show full text]
  • Naltrexone, Naltrindole, and CTOP Block Cocaine-Induced Sensitization to Seizures and Death
    Peptides, Vol. 18, No. 8, pp. 1189–1195, 1997 Copyright © 1997 Elsevier Science Inc. Printed in the USA. All rights reserved 0196-9781/97 $17.00 1 .00 PII S0196-9781(97)00182-4 Naltrexone, Naltrindole, and CTOP Block Cocaine-Induced Sensitization to Seizures and Death D. BRAIDA,1 E. PALADINI, E. GORI AND M. SALA Institute of Pharmacology, Faculty of Mathematical, Physical and Natural Sciences, University of Milan, Via Vanvitelli 32/A, 20129, Milan, Italy Received 10 March 1997; Accepted 15 May 1997 BRAIDA, D., E. PALADINI, E. GORI AND M. SALA. Naltrexone, naltrindole, and CTOP block cocaine-induced sensitization to seizures and death. PEPTIDES 18(8) 1189–1195, 1997.—ICV injection for 9 days of either naltexone (NTX) (5, 10, 20, 40 mg/rat) or a selective m peptide (CTOP) (0.125, 0.25, 0.5, 1, 3, 6 mg/rat) or d (naltrindole) (NLT) (5, 10, 20 mg/rat) subtype opioid receptor antagonist affected sensitization to cocaine (COC) (50 mg/kg, IP) administered 10 min after. NTX (5 and 40 mg/rat), NLT (10 and 20 mg/rat), and the peptide CTOP (0.25–0.5 mg/rat) attenuated seizure parameters (percent of animals showing seizures, mean score and latency) in a day-related manner. The DD50 (days to reach 50% of death) value for COC was 2.69, whereas it was 9.67 and 7.27 for NTX 5 and 40 mg/rat, 8.59 for NLT (10 mg/rat), and 6.11, 5.95, and 4.30 for CTOP (0.25, 0.5, and 1 mg/rat respectively).
    [Show full text]