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Présentation HJ
Conflits d’intérêts Astra-Zeneca, Janssen, Abacus international, Laboratoire ETAP, Institut Pasteur. Dr Hervé JAVELOT Pharmacien PH Etablissement Public de Santé Alsace Nord Service Pharmacie 141 avenue de Strasbourg 67 170 BRUMATH Tél. : 03 88 64 61 70 Fax : 03 88 64 61 58 Mail : [email protected] Perspectives dans la psychopharmacologie de l’anxiété et de la dépression Hervé JAVELOT Etablissement Public de Santé Alsace Nord Perspectives dans la psychopharmacologie de l’anxiété et de la dépression Traitements des troubles anxio-dépressifs. Les perspectives. ◦ L’axe GABAergique…éternellement prometteur ? ◦ L’incontournable théorie « monoaminergique »… ◦ Des théories alternatives à suivre … Traitements des troubles anxio-dépressifs. Contexte : ◦ XXI ème siècle : Le « siècle de la dépression » s’installe ? (Hardeveld et al., 2010) L’« ère de l’angoisse » s’affirme ? (Auden, 1947) ◦ Prévalence au cours de la vie : 16 à 17% pour la dépression, 17 à 18% pour les troubles anxieux Co-morbidité des 2 troubles dans 20 à 40% des cas (Antony, 2011 ; Depping et al., 2010 ; Hardeveld et al., 2010 ; Huppert, 2009) Auden WH (1947). The Age of Anxiety: A Baroque Eclogue. Random House: New York. Hardeveld F, Spijker J, De Graaf R, Nolen WA, Beekman AT. Prevalence and predictors of recurrence of major depressive disorder in the adult population. Acta Psychiatr Scand. 2010;122(3):184-91. Antony MM. Recent advances in the treatment of anxiety disorders. Canadian Psychology 2011;52(1), 10-19. Depping AM, Komossa K, Kissling W, Leucht S. Second-generation antipsychotics for anxiety disorders. Cochrane Database Syst Rev. 2010;(12):CD008120. Huppert JD. Anxiety disorders and depression comorbidity. -
BMC Pharmacology Biomed Central
CORE Metadata, citation and similar papers at core.ac.uk Provided by Springer - Publisher Connector BMC Pharmacology BioMed Central Research article Open Access Pharmacological Properties of DOV 315,090, an ocinaplon metabolite Dmytro Berezhnoy†1, Maria C Gravielle†1, Scott Downing1, Emmanuel Kostakis1, Anthony S Basile2, Phil Skolnick2, Terrell T Gibbs1 and David H Farb*1 Address: 1Laboratory of Molecular Neurobiology, Department of Pharmacology & Experimental Therapeutics, Boston University School of Medicine, 715 Albany St., Boston, MA 02118, USA and 2DOV Pharmaceutical, Inc, 150 Pierce St., Somerset, NJ 08873-4185, USA Email: Dmytro Berezhnoy - [email protected]; Maria C Gravielle - [email protected]; Scott Downing - [email protected]; Emmanuel Kostakis - [email protected]; Anthony S Basile - [email protected]; Phil Skolnick - [email protected]; Terrell T Gibbs - [email protected]; David H Farb* - [email protected] * Corresponding author †Equal contributors Published: 13 June 2008 Received: 20 December 2007 Accepted: 13 June 2008 BMC Pharmacology 2008, 8:11 doi:10.1186/1471-2210-8-11 This article is available from: http://www.biomedcentral.com/1471-2210/8/11 © 2008 Berezhnoy et al; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Background: Compounds targeting the benzodiazepine binding site of the GABAA-R are widely prescribed for the treatment of anxiety disorders, epilepsy, and insomnia as well as for pre- anesthetic sedation and muscle relaxation. It has been hypothesized that these various pharmacological effects are mediated by different GABAA-R subtypes. -
Guaiana, G., Barbui, C., Caldwell, DM, Davies, SJC, Furukawa, TA
View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Explore Bristol Research Guaiana, G., Barbui, C., Caldwell, D. M., Davies, S. J. C., Furukawa, T. A., Imai, H., ... Cipriani, A. (2017). Antidepressants, benzodiazepines and azapirones for panic disorder in adults: a network meta-analysis. Cochrane Database of Systematic Reviews, 2017(7), [CD012729]. https://doi.org/10.1002/14651858.CD012729 Publisher's PDF, also known as Version of record Link to published version (if available): 10.1002/14651858.CD012729 Link to publication record in Explore Bristol Research PDF-document This is the final published version of the article (version of record). It first appeared online via Cochrane Library at https://www.cochranelibrary.com/cdsr/doi/10.1002/14651858.CD012729/full . Please refer to any applicable terms of use of the publisher. University of Bristol - Explore Bristol Research General rights This document is made available in accordance with publisher policies. Please cite only the published version using the reference above. Full terms of use are available: http://www.bristol.ac.uk/pure/about/ebr-terms Cochrane Database of Systematic Reviews Antidepressants, benzodiazepines and azapirones for panic disorder in adults: a network meta-analysis (Protocol) Guaiana G, Barbui C, Caldwell DM, Davies SJC, Furukawa TA, Imai H, Koesters M, Tajika A, Bighelli I, Pompoli A, Cipriani A Guaiana G, Barbui C, Caldwell DM, Davies SJC, Furukawa TA, Imai H, Koesters M, Tajika A, Bighelli I, Pompoli A, Cipriani A. Antidepressants, benzodiazepines and azapirones for panic disorder in adults: a network meta-analysis. Cochrane Database of Systematic Reviews 2017, Issue 7. -
(12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig. -
(12) Patent Application Publication (10) Pub. No.: US 2004/0224012 A1 Suvanprakorn Et Al
US 2004O224012A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0224012 A1 Suvanprakorn et al. (43) Pub. Date: Nov. 11, 2004 (54) TOPICAL APPLICATION AND METHODS Related U.S. Application Data FOR ADMINISTRATION OF ACTIVE AGENTS USING LIPOSOME MACRO-BEADS (63) Continuation-in-part of application No. 10/264,205, filed on Oct. 3, 2002. (76) Inventors: Pichit Suvanprakorn, Bangkok (TH); (60) Provisional application No. 60/327,643, filed on Oct. Tanusin Ploysangam, Bangkok (TH); 5, 2001. Lerson Tanasugarn, Bangkok (TH); Suwalee Chandrkrachang, Bangkok Publication Classification (TH); Nardo Zaias, Miami Beach, FL (US) (51) Int. CI.7. A61K 9/127; A61K 9/14 (52) U.S. Cl. ............................................ 424/450; 424/489 Correspondence Address: (57) ABSTRACT Eric G. Masamori 6520 Ridgewood Drive A topical application and methods for administration of Castro Valley, CA 94.552 (US) active agents encapsulated within non-permeable macro beads to enable a wider range of delivery vehicles, to provide longer product shelf-life, to allow multiple active (21) Appl. No.: 10/864,149 agents within the composition, to allow the controlled use of the active agents, to provide protected and designable release features and to provide visual inspection for damage (22) Filed: Jun. 9, 2004 and inconsistency. US 2004/0224012 A1 Nov. 11, 2004 TOPCAL APPLICATION AND METHODS FOR 0006 Various limitations on the shelf-life and use of ADMINISTRATION OF ACTIVE AGENTS USING liposome compounds exist due to the relatively fragile LPOSOME MACRO-BEADS nature of liposomes. Major problems encountered during liposome drug Storage in vesicular Suspension are the chemi CROSS REFERENCE TO OTHER cal alterations of the lipoSome compounds, Such as phos APPLICATIONS pholipids, cholesterols, ceramides, leading to potentially toxic degradation of the products, leakage of the drug from 0001) This application claims the benefit of U.S. -
Understanding Benzodiazephine Use, Abuse, and Detection
Siemens Healthcare Diagnostics, the leading clinical diagnostics company, is committed to providing clinicians with the vital information they need for the accurate diagnosis, treatment and monitoring of patients. Our comprehensive portfolio of performance-driven systems, unmatched menu offering and IT solutions, in conjunction with highly responsive service, is designed to streamline workflow, enhance operational efficiency and support improved patient care. Syva, EMIT, EMIT II, EMIT d.a.u., and all associated marks are trademarks of General Siemens Healthcare Diagnostics Inc. All Drugs other trademarks and brands are the Global Division property of their respective owners. of Abuse Siemens Healthcare Product availability may vary from Diagnostics Inc. country to country and is subject 1717 Deerfield Road to varying regulatory requirements. Deerfield, IL 60015-0778 Please contact your local USA representative for availability. www.siemens.com/diagnostics Siemens Global Headquarters Global Siemens Healthcare Headquarters Siemens AG Understanding Wittelsbacherplatz 2 Siemens AG 80333 Muenchen Healthcare Sector Germany Henkestrasse 127 Benzodiazephine Use, 91052 Erlangen Germany Abuse, and Detection Telephone: +49 9131 84 - 0 www.siemens.com/healthcare www.usa.siemens.com/diagnostics Answers for life. Order No. A91DX-0701526-UC1-4A00 | Printed in USA | © 2009 Siemens Healthcare Diagnostics Inc. Syva has been R1 R2 a leading developer N and manufacturer of AB R3 X N drugs-of-abuse tests R4 for more than 30 years. R2 C Now part of Siemens Healthcare ® Diagnostics, Syva boasts a long and Benzodiazepines have as their basic chemical structure successful track record in drugs-of-abuse a benzene ring fused to a seven-membered diazepine ring. testing, and leads the industry in the All important benzodiazepines contain a 5-aryl substituent ring (ring C) and a 1,4–diazepine ring. -
Efficient Synthesis of Pyrazolopyridines Containing a Chromane Backbone Through Domino Reaction
Efficient synthesis of pyrazolopyridines containing a chromane backbone through domino reaction Razieh Navari1, Saeed Balalaie*1,2, Saber Mehrparvar1, Fatemeh Darvish1, Frank Rominger3, Fatima Hamdan1 and Sattar Mirzaie1 Full Research Paper Open Access Address: Beilstein J. Org. Chem. 2019, 15, 874–880. 1Peptide Chemistry Research Center, K. N. Toosi University of doi:10.3762/bjoc.15.85 Technology, P. O. Box 15875-4416, Tehran, Iran, Tel: +98-21-23064226, Fax: +98-21-22889403, 2Medical Biology Received: 07 February 2019 Research Center, Kermanshah University of Medical Sciences, Accepted: 29 March 2019 Kermanshah, Iran and 3Organisch-Chemisches Institut der Published: 11 April 2019 Universitaet Heidelberg, Im Neuenheimer Feld 270, D-69120 Heidelberg, Germany Associate Editor: T. J. J. Müller Email: © 2019 Navari et al.; licensee Beilstein-Institut. Saeed Balalaie* - [email protected] License and terms: see end of document. * Corresponding author Keywords: chromane; domino reaction; fused heterocyclic skeletons; pyrazolopyridines Abstract An efficient approach for the synthesis of pyrazolopyridines containing the aminochromane motif through a base-catalyzed cycliza- tion reaction is reported. The synthesis was carried out through a three-component reaction of (arylhydrazono)methyl-4H-chromen- 4-one, malononitrile, primary amines in the presence of Et3N at room temperature. However, carrying out the reaction under the same conditions without base led to a fused chromanyl-cyanopyridine. High selectivity, high atom economy, and good to high yields in addition to mild reaction conditions are the advantages of this approach. Introduction The synthesis of new fused heterocyclic backbones has always Chromone derivatives have been found to exhibit a broad range been a major challenge in the field of organic synthesis [1-3]. -
Anaesthesia for Castration of Piglets: Comparison Between Intranasal and Intramuscular Application of Ketamine, Climazolam and Azaperone
Originalarbeiten Anaesthesia for castration of piglets: Comparison between intranasal and intramuscular application of ketamine, climazolam and azaperone S. M. Axiak1, N. Jäggin1, S. Wenger1, M. G. Doherr2, U. Schatzmann1 1Division of Anaesthesiology and 2Division of Clinical Veterinary Research, Department of Clinical Veterinary Medicine, University of Bern Summary Kurznarkose zur Kastration von neugeborenen Ferkeln: Vergleich zwischen intranasaler und intramuskulärer Applikation von Ketamin, Climazolam und Azaperon The aim of this study was to compare the effect of Ziel dieser Studie war es, eine Kombination aus an anaesthetic combination given either intramus- Ketamin, Azaperon and Climazolam intranasal oder cularly (IM) or intranasally (IN) for castration of intramuskulär Kastrationsferkeln zur Narkoseein- piglets. Forty piglets aged 4 to 7 days were ran- leitung zu verabreichen und ihre Wirkung verglei- domly assigned to receive a mixture of ketamine 15 chen. 40 Ferkel im Alter zwischen 4–7 Tagen er- mg kg-1, climazolam 1.5 mg kg-1 and azaperone hielten 15 mg/kg KGW Ketamine, 1.5 mg/kg 1.0 mg kg-1, IN or IM, 10 minutes prior to castra- KGW Climazolam und 1 mg/kg KGW Azaperon tion. Physiological parameters were measured. Cas- intranasal (IN) oder intramuskulär (IM) zehn Mi- tration was videotaped for evaluation by 3 inde- nuten vor der Kastration. Physiologische Parameter pendent observers using a scoring system. Reaction wurden aufgezeichnet. and vocalization to the skin incision and cutting of Die Kastration wurde gefilmt und von drei unab- spermatic cord was evaluated and scored (0 = no hängigen Beobachtern mittels einem Punktesys- reaction, 16 = strong reaction). The IN group had tem (Kastrationsscore) beurteilt, wobei bei den a significantly higher (P < 0.01) castration score, Hautschnitten und der Durchtrennung der Samen- compared to the IM group. -
Crystal Structure Analysis of Ethyl 6-(4-Methoxyphenyl)-1-Methyl-4-Methyl- Sulfanyl-3-Phenyl-1H-Pyrazolo[3,4-B]Pyridine-5-Carboxylate
research communications Crystal structure analysis of ethyl 6-(4-methoxy- phenyl)-1-methyl-4-methylsulfanyl-3-phenyl-1H- pyrazolo[3,4-b]pyridine-5-carboxylate ISSN 2056-9890 H. Surya Prakash Rao,a,b* Ramalingam Gunasundarib and Jayaraman Muthukumaranc‡ Received 4 June 2020 aDepartment of Chemistry and Biochemistry, School of Basic Sciences and Research, Sharda University, Greater Noida Accepted 30 June 2020 201306, India, bDepartment of Chemistry, Pondicherry University, Puducherry 605 014, India, and cDepartment of Biotechnology, School of Engineering and Technology, Sharda University, Greater Noida 201306, India. *Correspon- dence e-mail: [email protected] Edited by D. Chopra, Indian Institute of Science Education and Research Bhopal, India In the title compound, C24H23N3O3S, the dihedral angle between the fused ‡ Additional correspondence author, e-mail: pyrazole and pyridine rings is 1.76 (7) . The benzene and methoxy phenyl rings [email protected]. make dihedral angles of 44.8 (5) and 63.86 (5) , respectively, with the pyrazolo[3,4-b] pyridine moiety. An intramolecular short SÁÁÁO contact Keywords: crystal structure; pyrazolopyridine; [3.215 (2) A˚ ] is observed. The crystal packing features C—HÁÁÁ interactions. pyrazolo[3,4-b]pyridine; C—HÁÁÁ interactions. CCDC reference: 2005976 Supporting information: this article has 1. Chemical context supporting information at journals.iucr.org/e Pyrazolopyridines, in which a group of three nitrogen atoms is incorporated into a bicyclic heterocycle, are privileged medicinal scaffolds, often utilized in drug design and discovery regimes (Kumar et al., 2019). Owing to the possibilities of the easy synthesis of a literally unlimited number of a combina- torial library of small organic molecules with a pyrazolo- pyridine scaffold, there has been enormous interest in these molecules among medicinal chemists (Kumar et al. -
GABA Receptors
D Reviews • BIOTREND Reviews • BIOTREND Reviews • BIOTREND Reviews • BIOTREND Reviews Review No.7 / 1-2011 GABA receptors Wolfgang Froestl , CNS & Chemistry Expert, AC Immune SA, PSE Building B - EPFL, CH-1015 Lausanne, Phone: +41 21 693 91 43, FAX: +41 21 693 91 20, E-mail: [email protected] GABA Activation of the GABA A receptor leads to an influx of chloride GABA ( -aminobutyric acid; Figure 1) is the most important and ions and to a hyperpolarization of the membrane. 16 subunits with γ most abundant inhibitory neurotransmitter in the mammalian molecular weights between 50 and 65 kD have been identified brain 1,2 , where it was first discovered in 1950 3-5 . It is a small achiral so far, 6 subunits, 3 subunits, 3 subunits, and the , , α β γ δ ε θ molecule with molecular weight of 103 g/mol and high water solu - and subunits 8,9 . π bility. At 25°C one gram of water can dissolve 1.3 grams of GABA. 2 Such a hydrophilic molecule (log P = -2.13, PSA = 63.3 Å ) cannot In the meantime all GABA A receptor binding sites have been eluci - cross the blood brain barrier. It is produced in the brain by decarb- dated in great detail. The GABA site is located at the interface oxylation of L-glutamic acid by the enzyme glutamic acid decarb- between and subunits. Benzodiazepines interact with subunit α β oxylase (GAD, EC 4.1.1.15). It is a neutral amino acid with pK = combinations ( ) ( ) , which is the most abundant combi - 1 α1 2 β2 2 γ2 4.23 and pK = 10.43. -
Neurobiological and Neurobehavioral Mechanisms of Chronic Alcohol Drinking
Neurobiological and Neurobehavioral Mechanisms of Chronic Alcohol Drinking Neurobiological and Neurobehavioral Mechanisms of Chronic Alcohol Drinking Alcoholism comprises a set of complex behaviors seeking behaviors, have been developed. These in which an individual becomes increasingly models, which remain an integral part of the preoccupied with obtaining alcohol. These study of alcoholism, include animals that pref- behaviors ultimately lead to a loss of control over erentially drink solutions containing alcohol, consumption of the drug and to the development animals that self-administer alcohol during of tolerance, dependence, and impaired social and withdrawal, animals with a history of dependence occupational functioning. that self-administer alcohol, and animals that self- administer alcohol after a period of abstinence Although valuable information regarding toler- from the drug. Genetic models for alcoholism ance and dependence has been, and continues to also exist and include animals that have been bred be, gathered through human studies, much of the selectively for high alcohol consumption. Studies detailed understanding of the impact of exposure using such models are uncovering the systemic, to alcohol on behavior and on the biological cellular, and molecular neurobiological mech- mechanisms underlying those behaviors has been anisms that appear to contribute to chronic obtained through the use of animal models for alcohol consumption. The challenge of current alcoholism and a variety of in vitro, or cellular, and future studies is to understand which specific systems. Through the use of cellular systems and cellular and subcellular systems undergo mole- animal models, researchers can control the genetic cular changes to influence tolerance and depen- background and experimental conditions under dence in motivational systems that lead to which a specific alcohol-related behavior or chronic drinking. -
Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix
United States International Trade Commission Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix USITC Publication 4208 December 2010 U.S. International Trade Commission COMMISSIONERS Deanna Tanner Okun, Chairman Irving A. Williamson, Vice Chairman Charlotte R. Lane Daniel R. Pearson Shara L. Aranoff Dean A. Pinkert Address all communications to Secretary to the Commission United States International Trade Commission Washington, DC 20436 U.S. International Trade Commission Washington, DC 20436 www.usitc.gov Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix Publication 4208 December 2010 (This page is intentionally blank) Pursuant to the letter of request from the United States Trade Representative of December 15, 2010, set forth at the end of this publication, and pursuant to section 1207(a) of the Omnibus Trade and Competitiveness Act, the United States International Trade Commission is publishing the following modifications to the Harmonized Tariff Schedule of the United States (HTS) to implement changes to the Pharmaceutical Appendix, effective on January 1, 2011. Table 1 International Nonproprietary Name (INN) products proposed for addition to the Pharmaceutical Appendix to the Harmonized Tariff Schedule INN CAS Number Abagovomab 792921-10-9 Aclidinium Bromide 320345-99-1 Aderbasib 791828-58-5 Adipiplon 840486-93-3 Adoprazine 222551-17-9 Afimoxifene 68392-35-8 Aflibercept 862111-32-8 Agatolimod