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Effects of the Putative Antipsychotic Alstonine on Glutamate Uptake in Acute Hippocampal Slices ⇑ Ana P
Neurochemistry International 61 (2012) 1144–1150 Contents lists available at SciVerse ScienceDirect Neurochemistry International journal homepage: www.elsevier.com/locate/nci Effects of the putative antipsychotic alstonine on glutamate uptake in acute hippocampal slices ⇑ Ana P. Herrmann a,b, , Paula Lunardi b, Luísa Klaus Pilz a, Ana C. Tramontina b, Viviane M. Linck a,b, Christopher O. Okunji c, Carlos A. Gonçalves b, Elaine Elisabetsky a,b a Laboratório de Etnofarmacologia, Departamento de Farmacologia, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Rua Sarmento Leite, 500, 90050-170 Porto Alegre, RS, Brazil b Programa de Pós-graduação em Ciências Biológicas: Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Rua Ramiro Barcelos, 2600, 90035-000 Porto Alegre, RS, Brazil c International Centre for Ethnomedicine and Drug Development (InterCEDD), Nsukka, Enugu State, Nigeria article info abstract Article history: A dysfunctional glutamatergic system is thought to be central to the negative symptoms and cognitive Received 8 March 2012 deficits recognized as determinant to the poor quality of life of people with schizophrenia. Modulating Received in revised form 13 August 2012 glutamate uptake has, thus, been suggested as a novel target for antipsychotics. Alstonine is an indole Accepted 15 August 2012 alkaloid sharing with atypical antipsychotics the profile in animal models relevant to schizophrenia, Available online 25 August 2012 though divergent in its mechanism of action. The aim of this study was to evaluate the effects of alstonine on glutamate uptake. Additionally, the effects on glutathione content and extracellular S100B levels were Keywords: assessed. -
(12) United States Patent (10) Patent No.: US 9,687,864 B2 Fulton Et Al
USOO9687864B2 (12) United States Patent (10) Patent No.: US 9,687,864 B2 Fulton et al. (45) Date of Patent: Jun. 27, 2017 (54) SYSTEMAND METHOD FOR ENHANCED 428/25 (2015.01); Y10T 428/31504 (2015.04); ELECTROSTATIC DEPOSITION AND Y10T 428/31507 (2015.04); SURFACE COATINGS (Continued) (58) Field of Classification Search (71) Applicant: Battelle Memorial Institute, USPC .......... 118/620–640; 23.9/690 708; 427/458, Columbus, OH (US) 427/475 4.86 (72) Inventors: John L. Fulton, Richland, WA (US); See application file for complete search history. George S. Deverman, Richland, WA (US); Dean W. Matson, Kennewick, (56) References Cited CA (US); Clement R. Yonker, Kennewick, WA (US); C. Douglas U.S. PATENT DOCUMENTS Taylor, Franklinton, NC (US); James 3,087,860 A 4, 1963 Endicott B. McClain, Raleigh, NC (US); Joseph 3,123,077 A 3, 1964 Alcamo M. Crowley, Cambria, CA (US) (Continued) (73) Assignee: Battelle Memorial Institute, Columbus, OH (US) FOREIGN PATENT DOCUMENTS CA 2589761 12, 2004 (*) Notice: Subject to any disclaimer, the term of this CN 1465410 1, 2004 patent is extended or adjusted under 35 (Continued) U.S.C. 154(b) by 0 days. (21) Appl. No.: 14/310,960 OTHER PUBLICATIONS Abreu Filho et al., “Influence of metal alloy and the profile of (22) Filed: Jun. 20, 2014 coronary stents in patients with multi-vessel coronary disease.” Clinics 66(6):985-989 (2011). (65) Prior Publication Data (Continued) US 2015/OO40827 A1 Feb. 12, 2015 Related U.S. Application Data Primary Examiner — Yewebdar Tadesse (74) Attorney, Agent, or Firm — Lerner, David, (62) Division of application No. -
Fused Tricyclic Dual Inhibitors of Cdk 4/6 and Flt3
(19) TZZ ¥¥_T (11) EP 2 937 349 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 28.10.2015 Bulletin 2015/44 C07D 471/14 (2006.01) C07D 519/00 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) (2006.01) (21) Application number: 15161337.9 A61P 35/02 (22) Date of filing: 21.03.2012 (84) Designated Contracting States: • Keegan, Kathleen S. AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Bainbridge Island, WA Washington 98110 (US) GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO • LI, Zhihong PL PT RO RS SE SI SK SM TR Millbrae, CA California 94030 (US) Designated Extension States: • Lively, Sarah E. BA ME San Carlos, CA California 94070 (US) • McGee, Lawrence R. (30) Priority: 23.03.2011 US 201161466841 P Pacifica, CA California 94044 (US) •Ragains,Mark L. (62) Document number(s) of the earlier application(s) in Fort Worth, TX Texas 76109 (US) accordance with Art. 76 EPC: • Wang, Xianghong 12711738.0 / 2 688 887 Dublin, CA California 94568 (US) • Weidner, Margaret F. (71) Applicant: AMGEN INC. Woodinville, WA Washington 98072 (US) Thousand Oaks, CA 91320-1799 (US) • Zhang, Jian Foster City, CA California 94404 (US) (72) Inventors: • Chen, Xiaoqi (74) Representative: Hoffmann Eitle Palo Alto, CA California 94303 (US) Patent- und Rechtsanwälte PartmbB •Dai,Kang Arabellastraße 30 Albany, CA California 94706 (US) 81925 München (DE) • Duquette, Jason A. Millbrae, CA California 94030 (US) Remarks: • Gribble, Michael W., Jr. This application was filed on 12-05-2015 as a San Francisco, CA California 94110 (US) divisional application to the application mentioned • Huard, Justin N. -
Exploring New Pharmacology and Toxicological Screening and Safety
Zaman et al. BMC Complementary and Alternative Medicine (2015) 15:121 DOI 10.1186/s12906-015-0635-2 RESEARCH ARTICLE Open Access Exploring new pharmacology and toxicological screening and safety evaluation of one widely used formulation of Nidrakar Bati from South Asia region Afria Zaman1, Md Shamsuddin Sultan Khan2*, Lucky Akter1, Sharif Hossain Syeed3, Jakia Akter4, Abdullah Al Mamun5, Md Ershad Alam5, Md Ahsan Habib5 and Md Abdul Jalil5 Abstract Background: Nidrakar Bati (NKB) is an herbal remedy consisted with seven medicinal herbs widely used to cure Somnifacient (sleeping aid) in South Asia as Ayurvedic medicinal system. In the present study, pharmacological and toxicological effects of this medicine was investigated in mice to validate the safety and efficacy of the herb. Methods: Organic solvent extracts NKB were prepared using maceration method. Effect of extracts on the central nervous system was evaluated using hypnotic activity assay. Effect of the extracts on metabolic activity, assessing involvement of thyroid was conducted using hypoxia test. analgesic and anti-inflammatory activities were assessed in mice using acetic acid induced writhing, formalin induced paw edema, xylene induced ear edema assays. Anxiolytic activity was performed using plus maze, climbing out and forced swimming tests. Effect of the extracts on psychopharmacological effect was carried out using locomotor activity tests (open field, Hole-board and Hole-cross tests). Neuropharmacological effect of the extracts was performed using motor coordination (rotarod test). Toxicological potential of the extract was evaluated using gastro-intestinal activity (gastric emptying and gastrointestinal motility tests). Results: The studied formulation reduced the CNS stimulant effects dose independently. In the hypoxia test, only a dose of 100 mg/kg of NKB decreased the survival time. -
Rethinking Psychiatric Care(2)
Rethinking Psychiatric Care: If We Follow the Scientific Evidence, What Must We Do To Better Promote Long- term Recovery? The Common Wisdom The introduction of Thorazine into asylum medicine in 1955 “initiated a revolution in psychiatry, comparable to the introduction of penicillin in general medicine.” --Edward Shorter, A History of Psychiatry The Disabled Mentally Ill in the United States, 1955-2007 (under government care) Per 100,000 population 1500 1200 1315 900 600 543 300 213 0 1955 1987 2007 Source: Silverman, C. The Epidemiology of Depression (1968): 139. U.S. Social Security Administration Reports, 1987-2007. U.S. Disability in the Prozac Era Millions of adults, 18 to 66 years old 4 3 2 1 0 1987 1991 1995 1999 2003 2007 Source: U.S. Social Security Administration Reports, 1987-2007 Increased Treatment and Disability In U.S., 1990 to 2003 1990 2003 Number treated for psychiatric disorders 11.16 million 21.77 million Number on government disability 1.47 million 3.25 million due to mental illness Source: Surveys on prevalence of psychiatric disorders in 1990 and 2003, and percentage of those with disorders who were treated; SSI and SSDI disability data for 1990 to 2003. The Chemical Imbalance Theory of Mental Disorders • Arose from understanding of how drugs act on brain (1960s-1970s) • Investigations of dopamine theory of schizophrenia and serotonin theory of depression started in 1970s Findings re the Chemical Imbalance Theory of Mental Disorders A. Serotonin Theory of Depression • “Elevations or decrements in the functioning of serotonergic systems per se are not likely to be associated with depression.” --NIMH, 1984. -
The Rise and Fall of the Diagnosis of Functional Psychoses: an Essay Per Bergsholm
Bergsholm BMC Psychiatry (2016) 16:387 DOI 10.1186/s12888-016-1101-5 DEBATE Open Access Is schizophrenia disappearing? The rise and fall of the diagnosis of functional psychoses: an essay Per Bergsholm Abstract Background: The categories of functional psychoses build on views of influential professionals. There have long been four main categories – affective, schizophrenic, schizoaffective/cycloid/reactive/polymorphic, and delusional/ paranoid psychoses. The last three are included in “psychotic disorders”. However, this dichotomy and the distinctions between categories may have been over-estimated and contributed to lack of progress. Ten topics relevant for the diagnosis of functional psychoses: 1. The categories of functional psychoses have varied with time, place and professionals’ views, with moving boundaries, especially between schizophrenia and affective psychoses. 2. Catatonia is most often related to affective and organic psychoses, and paranoia is related to grandiosity and guilt, calling in question catatonic and paranoid schizophrenia. Arguments exist for schizophrenia being a “misdiagnosis”. 3. In some countries schizophrenia has been renamed, with positive consequences. 4. The doctrine of “unitary psychosis”, which included abnormal affect, was left in the second half of the 1800s. 5. This was followed by a dichotomy between schizophrenia and affective psychoses and broadening of the schizophrenia concept, whereas affective symptoms were strongly downgraded. 6. Many homogeneous psychoses with mixtures of schizophrenic and affective symptoms were described and related to “psychotic disorders”, although they might as well be affective disorders. 7. Critique of the extensive schizophrenia concept led to, in DSM-III and ICD-10, affective symptoms being exclusion criteria for schizophrenia and acceptance of mood-incongruent psychotic symptoms in affective psychoses. -
Antitumor Activities of Rauwolfia Vomitoria Extract and Potentiation Of
Current Therapeutic Research 75 (2013) 8–14 Contents lists available at ScienceDirect Current Therapeutic Research journal homepage: www.elsevier.com/locate/cuthre Antitumor Activities of Rauwolfia vomitoria Extract and Potentiation of Carboplatin Effects Against Ovarian Cancer☆ Jun Yu, PhD1,2, Yan Ma, PhD1,2, Jeanne Drisko, MD2, Qi Chen, PhD1,2,n 1 Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, Kansas City, Kansas 2 KU Integrative Medicine, University of Kansas Medical Center, Kansas City, Kansas article info abstract Article history: Background: Tumor resistance to platinum-based drugs has been an obstacle to the treatment of ovarian Accepted 26 April 2013 cancer. Extract of the plant Rauwolfia vomitoria has long been used by cancer patients. However, there have not been systematic studies of its anticancer activity. Key words: Objective: In an effort to enhance the effectiveness of platinum-based drugs, we investigated the carboplatin anticancer effect of a Rauwolfia vomitoria extract (Rau), both alone and in combination with ovarian cancer carboplatin (Cp). plant extract Methods: In vitro cytotoxicity and colony formation were evaluated in several ovarian cancer cell lines. fi Rauwol a vomitoria In vivo effects were evaluated in an intraperitoneal ovarian cancer mouse model. The combination of Rau synergy and Cp was assessed using Chou-Talalay’s constant ratio design and median effect analysis based on the isobologram principle to determine the combination index values. Results: Rau decreased cell growth in all 3 tested ovarian cancer cell lines dose dependently and completely inhibited formation of colonies in soft agar. Apoptosis was induced in a time- and dose- dependent manner and was the predominant form of Rau-induced cell death. -
Development of a Pharmacophore for Inhibition of Human Liver Cytochrome P-450 2D6: Molecular Modeling and Inhibition Studies
1136 J. Med. Chem. 1993,36, 1136-1145 Development of a Pharmacophore for Inhibition of Human Liver Cytochrome P-450 2D6: Molecular Modeling and Inhibition Studies Giinter R. Strob1,'J Stephanie von Kruedener,t Joachim Stockigt; F. Peter Guengerich,O and Thomas Wolfft Znstitut fur Toxikologie, GSF - Forschungszentrum fiir Umwelt und Gesundheit, 8042 Neuherberg, Germany, Znstitut fur Pharmazie, Johannes Gutenberg- Universitiit, 6500 Mainz, Germany, and Center in Molecular Toxicology, Vanderbilt University, Nashville, Tennessee 37232 Received December 31, 1991 To gain insight into the specificity of cytochrome P-450 2D6 toward inhibitors, a preliminary pharmacophore model was built up using strong competitive inhibitors. Ajmalicine (l),the strongest inhibitor known (Ki = 3 nM) was selected as template because of ita rigid structure. The preliminary pharmacophore model was validated by performing inhibition studies with derivatives of ajmalicine (1)and quinidine (9). Bufuralol(18) was chosen as substrate and the metabolite 1'-hydroxybufuralol (19) was separated by high performance liquid chromatography. All incubations were carried out using human liver microsomes after demonstration that the Ki values obtained with microsomes were in accordance with those obtained with a reconstituted monooxygenase system containing purified cytochrome P-4502D6. Large differences of Ki values ranging between 0.005 and 100 pM were observed. Low-energy conformers of tested compounds were fit within the preliminary pharmacophore model. The analysis of steric and electronic properties of these compounds led to the definition of a final pharmacophore model. Characteristic properties are a positive charge on a nitrogen atom and a flat hydrophobic region, the plane of which is almost perpendicular to the N-H axis and maximally extends up to a distance of 7.5 A from the nitrogen atom. -
GUIDELINES for the USE of PSYCHOTROPIC DRUGS a Clinical Handbook GUIDELINES for the USE of PSYCHOTROPIC DRUGS a Clinical Handbook
GUIDELINES FOR THE USE OF PSYCHOTROPIC DRUGS A Clinical Handbook GUIDELINES FOR THE USE OF PSYCHOTROPIC DRUGS A Clinical Handbook Edited by HARVEY C STANCER, Ph.D., M.D., F.R.CP.(C) Clarke Institute of Psychiatry University of Toronto PAUL E. GARFINKEL, M.S., M.D., F.R.C.P.(C) Toronto General Hospital University of Toronto VIVIAN M. RAKOFF, M.A., M.B., F.R.CP.(C) Clarke Institute of Psychiatry University of Toronto LIMITED InternationalMT~il Medical Publishers Published in the UK and Europe by MTP Press Limited Falcon House Lancaster, England Published in the US by SPECTRUM PUBLICA nONS, INC. 175-20 Wexford Terrace Jamaica, NY 11432 Copyright © 1984 by Spectrum Publications, Inc. Softcover reprint of the hardcover 1st edition 1984 All rights reserved. No part of this book may be reproduced in any form, by photostat, microfilm, retrieval system, or any other means without prior written permission of the copyright holder or his licensee. ISBN 978-94-011-7620-0 ISBN 978-94-011-7618-7 (eBook) DOl 10.1007/978-94-011-7618-7 This volume is dedicated to Magda, Dorothy, and Gina Contributors William H. Anderson, M.D .• Assistant Clinical Professor of Psychiatry, Harvard Medical School; Acute Psychiatry Service, Massachusetts General Hospital, Boston, Massachusetts Jack D. Barchas, M.D .• Nancy Pritzker Laboratory of Behavioral Neurochemistry and Stanford Mental Health Clinical Research Center, Department of Psychiatry and Behavioral Sciences, Stanford University School of Medicine, Stanford, California Philip A. Berger, M.D .• Department of Psychiatry and Behavioral Sciences, Stanford University School of Medicine, Stanford, California Janel S. -
Antipsychotics-2020.Pdf
© Mind 2020 Antipsychotics Explains what antipsychotics are used for, how the medication works, possible side effects and information about withdrawal. If you require this information in Word document format for compatibility with screen readers, please email: [email protected] Contents What are antipsychotics? ...................................................................................................................... 2 Could antipsychotics help me? .............................................................................................................. 5 How to take antipsychotics safely ......................................................................................................... 9 What dosage of antipsychotics should I be on? .................................................................................. 15 Antipsychotics during pregnancy and breastfeeding ........................................................................... 17 What side effects can antipsychotics cause? ....................................................................................... 20 What is a depot injection? ................................................................................................................... 30 How can I compare different antipsychotics? ..................................................................................... 31 Can I come off antipsychotics? ............................................................................................................ 41 Alternatives to antipsychotics -
Handbook of Experimental Pharmacology Volume
Handbook of Experimental Pharmacology Volume 212 Editor-in-Chief F.B. Hofmann, München Editorial Board J.A. Beavo, Seattle J.E. Barrett, Philadelphia D. Ganten, Berlin P. Geppetti, Florence M.C. Michel, Ingelheim C.P. Page, London W. Rosenthal, Berlin For further volumes: http://www.springer.com/series/164 . Gerhard Gross • Mark A. Geyer Editors Current Antipsychotics Editors Gerhard Gross Mark A. Geyer Abbott, Neuroscience Research, GPRD University of California San Diego Ludwigshafen, Germany Department of Psychiatry Institut fu¨r Pharmakologie La Jolla Universita¨t Duisburg-Essen California Universita¨tsklinikum Essen USA Essen Germany ISSN 0171-2004 ISSN 1865-0325 (electronic) ISBN 978-3-642-25760-5 ISBN 978-3-642-25761-2 (eBook) DOI 10.1007/978-3-642-25761-2 Springer Heidelberg New York Dordrecht London Library of Congress Control Number: 2012952465 # Springer-Verlag Berlin Heidelberg 2012 This work is subject to copyright. All rights are reserved by the Publisher, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfilms or in any other physical way, and transmission or information storage and retrieval, electronic adaptation, computer software, or by similar or dissimilar methodology now known or hereafter developed. Exempted from this legal reservation are brief excerpts in connection with reviews or scholarly analysis or material supplied specifically for the purpose of being entered and executed on a computer system, for exclusive use by the purchaser of the work. Duplication of this publication or parts thereof is permitted only under the provisions of the Copyright Law of the Publisher’s location, in its current version, and permission for use must always be obtained from Springer. -
Handbook of Schizophrenia Spectrum Disorders, Volume III
Handbook of Schizophrenia Spectrum Disorders, Volume III Michael S. Ritsner Editor Handbook of Schizophrenia Spectrum Disorders, Volume III Therapeutic Approaches, Comorbidity, and Outcomes 123 Editor Michael S. Ritsner Technion – Israel Institute of Technology Rappaport Faculty of Medicine Haifa Israel [email protected] ISBN 978-94-007-0833-4 e-ISBN 978-94-007-0834-1 DOI 10.1007/978-94-007-0834-1 Springer Dordrecht Heidelberg London New York Library of Congress Control Number: 2011924745 © Springer Science+Business Media B.V. 2011 No part of this work may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, microfilming, recording or otherwise, without written permission from the Publisher, with the exception of any material supplied specifically for the purpose of being entered and executed on a computer system, for exclusive use by the purchaser of the work. Printed on acid-free paper Springer is part of Springer Science+Business Media (www.springer.com) Foreword Schizophrenia Spectrum Disorders: Insights from Views Across 100 years Schizophrenia spectrum and related disorders such as schizoaffective and mood dis- orders, schizophreniform disorders, brief psychotic disorders, delusional and shared psychotic disorders, and personality (i.e., schizotypal, paranoid, and schizoid per- sonality) disorders are the most debilitating forms of mental illness, worldwide. There are 89,377 citations (including 10,760 reviews) related to “schizophrenia” and 2118 (including 296 reviews) related to “schizophrenia spectrum” in PubMed (accessed on August 12, 2010). The classification of these disorders, in particular, of schizophrenia, schizoaf- fective and mood disorders (referred to as functional psychoses), has been debated for decades, and its validity remains controversial.