Design and Synthesis of Functionally Selective Kappa Opioid Receptor Ligands
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Red Panda Biotic Factors Biotic Factors
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52Nd Annual Meeting
ACNP 52nd Annual Meeting Final Program December 8-12, 2013 The Westin Diplomat Resort & Spa Hollywood, Florida President: David A. Lewis, M.D. Program Committee Chair: Randy D. Blakely, Ph.D. Program Committee Co-Chair: Pat R. Levitt, Ph.D. This meeting is jointly sponsored by the Vanderbilt University School of Medicine Department of Psychiatry and the American College of Neuropsychopharmacology. Dear ACNP Members and Guests, It is a distinct pleasure to welcome you to the 2014 meeting of the American College of Neuropsychopharmacology! This 52nd annual meeting will again provide opportunities for the exercise of the College’s core values: the spirit of Collegiality, promoting in each other the best in science, training and service; participation in Community, pursuing together the goals of understanding the neurobiology of brain diseases and eliminating their burden on individuals and our society; and engaging in Celebration, taking the time to recognize and enjoy the contributions and accomplishments of our members and guests. Under the excellent leadership of Randy Blakely and Pat Levitt, the Program Committee has done a superb job in assembling an outstanding slate of scientific presentations. Based on membership feedback, the meeting schedule has been designed with the goals of achieving an optimal mix of topics and types of sessions, increasing the diversity of participating scientists and creating more time for informal interactions. The presentations will highlight both the breadth of the investigative interests of ACNP membership -
Behavioral and Brain Sciences Plasticity: Implications for Opioid
Behavioral and Brain Sciences http://journals.cambridge.org/BBS Additional services for Behavioral and Brain Sciences: Email alerts: Click here Subscriptions: Click here Commercial reprints: Click here Terms of use : Click here Plasticity: Implications for opioid and other pharmacological interventions in specific pain states Anthony H. Dickenson Behavioral and Brain Sciences / Volume 20 / Issue 03 / September 1997, pp 392 403 DOI: null, Published online: 08 September 2000 Link to this article: http://journals.cambridge.org/abstract_S0140525X97241488 How to cite this article: Anthony H. Dickenson (1997). Plasticity: Implications for opioid and other pharmacological interventions in specific pain states. Behavioral and Brain Sciences,20, pp 392403 Request Permissions : Click here Downloaded from http://journals.cambridge.org/BBS, IP address: 144.82.107.43 on 10 Aug 2012 BEHAVIORAL AND BRAIN SCIENCES (1997) 20, 392±403 Printed in the United States of America Plasticity: Implications for opioid and other pharmacological interventions in specific pain states Anthony H. Dickenson Department of Pharmacology, University College London, London WC1E 6BT, United Kingdom Electronic mail: anthony.dickenson6ucl.ac.uk Abstract: The spinal mechanisms of action of opioids under normal conditions are reasonably well understood. The spinal effects of opioids can be enhanced or reduced depending on pathology and activity in other segmental and nonsegmental pathways. This plasticity will be considered in relation to the control of different pain states using opioids. The complex and contradictory findings on the supraspinal actions of opioids are explicable in terms of heterogeneous descending pathways to different spinal targets using multiple transmitters and receptors ± therefore opioids can both increase and decrease activity in descending pathways. -
A Global Review on Short Peptides: Frontiers and Perspectives †
molecules Review A Global Review on Short Peptides: Frontiers and Perspectives † Vasso Apostolopoulos 1 , Joanna Bojarska 2,* , Tsun-Thai Chai 3 , Sherif Elnagdy 4 , Krzysztof Kaczmarek 5 , John Matsoukas 1,6,7, Roger New 8,9, Keykavous Parang 10 , Octavio Paredes Lopez 11 , Hamideh Parhiz 12, Conrad O. Perera 13, Monica Pickholz 14,15, Milan Remko 16, Michele Saviano 17, Mariusz Skwarczynski 18, Yefeng Tang 19, Wojciech M. Wolf 2,*, Taku Yoshiya 20 , Janusz Zabrocki 5, Piotr Zielenkiewicz 21,22 , Maha AlKhazindar 4 , Vanessa Barriga 1, Konstantinos Kelaidonis 6, Elham Mousavinezhad Sarasia 9 and Istvan Toth 18,23,24 1 Institute for Health and Sport, Victoria University, Melbourne, VIC 3030, Australia; [email protected] (V.A.); [email protected] (J.M.); [email protected] (V.B.) 2 Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Zeromskiego˙ 116, 90-924 Lodz, Poland 3 Department of Chemical Science, Faculty of Science, Universiti Tunku Abdul Rahman, Kampar 31900, Malaysia; [email protected] 4 Botany and Microbiology Department, Faculty of Science, Cairo University, Gamaa St., Giza 12613, Egypt; [email protected] (S.E.); [email protected] (M.A.) 5 Institute of Organic Chemistry, Faculty of Chemistry, Lodz University of Technology, Zeromskiego˙ 116, 90-924 Lodz, Poland; [email protected] (K.K.); [email protected] (J.Z.) 6 NewDrug, Patras Science Park, 26500 Patras, Greece; [email protected] 7 Department of Physiology and Pharmacology, -
The Oxytocin/Vasopressin Receptor Family Has at Least Five Members in the Gnathostome Lineage, Including Two Distinct V2 Subtypes
The oxytocin/vasopressin receptor family has at least five members in the gnathostome lineage, including two distinct V2 subtypes General and Comparative Endocrinology 175(1): 135-143 doi:10.1016/j.ygcen.2011.10.011 Accepted October 20, 2011 E-pub October 28, 2012 Published January 1, 2012 Figshare doi:10.6084/m9.figshare.811860. Shared October 1, 2013 Daniel Ocampo Daza*, Michalina Lewicka¹, Dan Larhammar Department of Neuroscience, Science for Life Laboratory, Uppsala Universitet, Box 593, SE-751 24 Uppsala, Sweden * Corresponding author. E-mail address: [email protected] ¹ Current address: Department of Neuroscience, Karolinska Institutet, SE-171 77 Stockholm, Sweden Cite as D. Ocampo Daza, M. Lewicka and D. Larhammar. The oxytocin/vasopressin family has at least five members in the gnathostome lineage, including two distinct V2 subtypes. General and Comparative Endocrinology, 175 (1) (2012) 135-143. This document corresponds to the article as it appeared upon acceptance. You are free to download, print and distribute it for any purposes under a Creative Commons Attribution 3.0 Unported License (http://creativecommons.org/licenses/by/3.0/), provided the original work is cited as specified. Errata: The introduction incorrectly states that “the V2 receptor inhibits adenylyl cyclase, thereby reducing the production of cAMP” on page 3. In fact the V2-type vasopressin receptors stimulate adenylyl cyclase and increase the cytosolic cyclic AMP release, see for instance Schöneberg et al., Molecular aspects of vasopressin receptor function, Advances in experimental medicine and biology 449 (1998) 347–58. This mistake was reported in the proofreading phase of pre-publication, but the correction was not carried to the final version of the article. -
ESI-MS Method for the Simultaneous Detection of Five Major Opium Alkaloids
Development and evaluation of an LC- ESI-MS method for the simultaneous detection of five major opium alkaloids M.G. Carlin PhD 2015 Development and evaluation of an LC-ESI- MS method for the simultaneous detection of five major opium alkaloids Michelle Groves Carlin A thesis submitted in partial fulfilment of the requirements of the University of Northumbria at Newcastle for the degree of Doctor of Philosophy Research undertaken in the Department of Applied Sciences, Faculty of Health & Life Sciences August 2015 Abstract The aim of this work was to establish an analytical method for the simultaneous detection of five major opium alkaloids in poppy seeds by liquid chromatography-electrospray ionisation-mass spectrometry (LC- ESI-MS). Once opium alkaloids were detected in poppy seeds, toxicological studies were carried out to establish if these compounds were detected in oral fluid (OF) of participants who ingested muffins containing poppy seeds. It is known that the ingestion of poppy seeds has caused positive opiate drug test results and much work has been reported in the scientific literature in the last 20 years. Researchers in the field have investigated alternatives to differentiate between heroin administration and that of other opiate drugs versus poppy seed ingestion. Most of the work which has been carried out relates to establishing illicit heroin use by examining biological matrices for the presence of acetylcodeine, thebaine, papaverine, noscapine and their associated metabolites. The research methodology consisted of establishing an LC-ESI-MS method for the simultaneous detection of five major opium alkaloids (morphine, codeine, thebaine, papaverine and noscapine). A deuterated internal standard (morphine-d3) was used for the quantitation of alkaloids in harvested poppy seeds and oral fluid samples. -
G Protein-Coupled Receptors: What a Difference a ‘Partner’ Makes
Int. J. Mol. Sci. 2014, 15, 1112-1142; doi:10.3390/ijms15011112 OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 www.mdpi.com/journal/ijms Review G Protein-Coupled Receptors: What a Difference a ‘Partner’ Makes Benoît T. Roux 1 and Graeme S. Cottrell 2,* 1 Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK; E-Mail: [email protected] 2 Reading School of Pharmacy, University of Reading, Reading RG6 6UB, UK * Author to whom correspondence should be addressed; E-Mail: [email protected]; Tel.: +44-118-378-7027; Fax: +44-118-378-4703. Received: 4 December 2013; in revised form: 20 December 2013 / Accepted: 8 January 2014 / Published: 16 January 2014 Abstract: G protein-coupled receptors (GPCRs) are important cell signaling mediators, involved in essential physiological processes. GPCRs respond to a wide variety of ligands from light to large macromolecules, including hormones and small peptides. Unfortunately, mutations and dysregulation of GPCRs that induce a loss of function or alter expression can lead to disorders that are sometimes lethal. Therefore, the expression, trafficking, signaling and desensitization of GPCRs must be tightly regulated by different cellular systems to prevent disease. Although there is substantial knowledge regarding the mechanisms that regulate the desensitization and down-regulation of GPCRs, less is known about the mechanisms that regulate the trafficking and cell-surface expression of newly synthesized GPCRs. More recently, there is accumulating evidence that suggests certain GPCRs are able to interact with specific proteins that can completely change their fate and function. These interactions add on another level of regulation and flexibility between different tissue/cell-types. -
Opioids Regulate Cgmp Formationin Cloned Neuroblastoma Cells
Proc. NatL. Acad. Sci. USA Vol. 79, pp. 690-694, January 1982 Neurobiology Opioids regulate cGMP formation in cloned neuroblastoma cells (cyclic nucleotides/opiate receptor/desensitization) GERMAINE J. GWYNN AND ERMINIO COSTA* Laboratory of Preclinical Pharmacology, National Institute of Mental Health, Saint Elizabeths Hospital, Washington, D.C. 20032 Communicated by Floyd E. Bloom, October 8, 1981 ABSTRACT Opioid agonists caused a rapid dose-related el- cumulation in rat striatal slices with characteristics that fulfill evation of the cGMP content of N4TG1 murine neuroblastoma the criteria for a specific narcotic action (6). In contrast, the cells. An excellent correlation was found between the rank order decrements in the cGMP content ofcerebellar tissue observed of potency of agonists in stimulating cGMP accumulation and in after morphine administration are probably indirect effects of displacing [3H]etorphine ([H]ETP) bound to intact cells. The nar- opioid receptor stimulation mediated by the modulation of y- cotic antagonists naloxone and diprenorphine failed to increase aminobutyric acid or acetylcholine collateral neuronal loops (7, cGMP content; moreover, in the presence of 5 ,IM naloxone, the 8). A functional role for cGMP in opioid action is further sug- EC50 of ETP increased from w9 nM to >1 ,uM. N4TG1 cells that had been incubated for 20 min with 0.32 ItM ETP and thoroughly gested by the pivotal role that calcium ions play both in regu- washed displayed a marked loss in sensitivity to subsequent ETP lating cGMP formation (for review, see refs. 9, 10) and in me- challenge. This desensitization was characterized by a 40-50% diating the acute and chronic effects ofopioids (for review, see decrease in maximal response and an increase in the apparent Ka refs. -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. -
Neurones Ofguinea-Pig Caecum by Activating 3-Receptors Satoshi Mihara & R
Br. J. Pharmac. (1986), 88, 315-322 Opioids increase potassium conductance in submucous neurones ofguinea-pig caecum by activating 3-receptors Satoshi Mihara & R. Alan North Neuropharmacology Laboratory, 56-245 Massachusetts Institute ofTechnology, Cambridge MA 02139, U.S.A. 1 Intracellular records were made from neurones in the submucous plexus ofthe guinea-pig caecum. 2 [Met5Jenkephalin, [Leu5]enkephalin, [D-Ala2,D-Leu5]enkephalin (DADLE) and [D-Ser9,Leu5Jenke- phalin-Thr (DSLET) hyperpolarized the membrane when applied in concentrations of 30 nM- 10 gM. Normorphine, [D-Ala2, MePhe4,Gly5]enkephalin-ol (DAGO), [D-Ala2,MePhe4,Met(0)5]enkephalin-ol (FK33824), dynorphin A and tifluadom had no effect at concentrations up to M. 3 The hyperpolarization resulted from an increase in the membrane potassium conductance. 4 Hyperpolarizations induced by [Met5]enkephalin were antagonized competitively by naloxone and by N-bisallyl[aminoisobutyrate2 3, Leu5]enkephalin (ICI 174864). The Schild plots for these antagon- isms had slopes not different from one, and the dissociation equilibrium constants among individual neurones were 5-50 nM for naloxone and 5-60 nM for ICI 174864. 5 The results indicate that the opioid receptors on guinea-pig submucous neurones which are coupled to potassium channels are of the 6-type. Introduction Opioid receptors of the 6-type were discovered as a ors to conclude that the 6-receptor was on the nerves result of their relative insensitivity to blockade by the rather than the mucosal cells themselves. In keeping antagonist naloxone (Lord et al., 1977). They have a with this is the failure to detect any binding of [3HJ- characteristic distribution throughout the nervous [Met5]enkephalin on enterocytes of the rabbit ileum system which is distinct from that of the p- or ic-type (Binder et al., 1984). -
Osteoblast Regulation Via Ligand-Activated Nuclear Trafficking of the Oxytocin Receptor
Osteoblast regulation via ligand-activated nuclear trafficking of the oxytocin receptor Adriana Di Benedettoa,b, Li Sunc,d, Carlo G. Zambonine, Roberto Tammaa, Beatrice Nicoa, Cosima D. Calvanoe, Graziana Colaiannia, Yaoting Jic,d, Giorgio Morib, Maria Granoa, Ping Luc,d, Silvia Coluccia, Tony Yuenc,d, Maria I. Newf,1, Alberta Zallonea,2, and Mone Zaidic,d,g,1,2 aDepartment of Basic Medical Science, Neurosciences and Sensory Organs, University of Bari Aldo Moro Medical School, Bari 70126, Italy; bDepartment of Clinical and Experimental Medicine, University of Foggia, Foggia 71122, Italy; cMount Sinai Bone Program and dDepartment of Medicine, Mount Sinai School of Medicine, New York, NY 10029; eDepartment of Chemistry, University of Bari Aldo Moro, Bari 70126, Italy; and Departments of fPediatrics and gStructural and Chemical Biology, Mount Sinai School of Medicine, New York, NY 10029 Contributed by Maria I. New, October 8, 2014 (sent for review August 27, 2014); reviewed by Xu Cao, Christopher Huang, and Carlos Isales We report that oxytocin (Oxt) receptors (Oxtrs), on stimulation by bisphosphate 3-kinase (Akt/PI3K) (9, 10). Such mechanisms can the ligand Oxt, translocate into the nucleus of osteoblasts, impli- elicit delayed genomic responses. cating this process in the action of Oxt on osteoblast maturation. After being internalized, GPCRs are either recycled back to Sequential immunocytochemistry of intact cells or isolated nucleo- the plasma membrane to resensitize the cell to ligand action or plasts stripped of the outer nuclear membrane showed progressive transported to lysosomes for degradation. Although G proteins nuclear localization of the Oxtr; this nuclear translocation was con- have been found in the Golgi body, endoplasmic reticulum, and firmed by monitoring the movement of Oxtr–EGFP as well as by cytoskeleton (11–13), GPCRs can localize to the nucleus or nuclear immunogold labeling. -
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