Genomics and Proteomics Studies of Zolpidem
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Withdrawing Benzodiazepines in Primary Care
PC\/ICU/ ADTiriC • CNS Drugs 2009,-23(1): 19-34 KtVltW MKIIWLC 1172-7047/I»/O(X)1«119/S4W5/C1 © 2009 Adis Dato Intocmation BV. All rights reserved. Withdrawing Benzodiazepines in Primary Care Malcolm Luder} Andre Tylee^ and ]ohn Donoghue^ 1 Institute of Psychiatry, King's College London, London, England 2 John Moores University, Liverpool, Scotland Contents Abstract ' 19 1. Benzodiazepine Usage 22 2. Interventions 23 2.1 Simple interventions 23 2.2 Piiarmacoiogicai interventions 25 2.3 Psychoiogical Interventions 26 2.4 Meta-Anaiysis ot Various interventions 27 3. Outcomes 28 4. Practicai Issues 29 5. Otiier Medications 30 5.1 Antidepressants 30 5.2 Symptomatic Treatments 30 6. Conciusions 31 Abstract The use of benzodiazepine anxiolytics and hypnotics continues to excite controversy. Views differ from expert to expert and from country to country as to the extent of the problem, or even whether long-term benzodiazepine use actually constitutes a problem. The adverse effects of these drugs have been extensively documented and their effectiveness is being increasingly questioned. Discontinua- tion is usually beneficial as it is followed by improved psychomotor and cognitive functioning, particularly in the elderly. The potential for dependence and addic- tion have also become more apparent. The licensing of SSRIs for anxiety disorders has widened the prescdbers' therapeutic choices (although this group of medications also have their own adverse effects). Melatonin agonists show promise in some forms of insomnia. Accordingly, it is now even more imperative that long-term benzodiazepine users be reviewed with respect to possible discon- tinuation. Strategies for discontinuation start with primary-care practitioners, who are still the main prescdbers. -
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. -
Pharmacological Properties of GABAA- Receptors Containing Gamma1
Molecular Pharmacology Fast Forward. Published on November 4, 2005 as DOI: 10.1124/mol.105.017236 Molecular PharmacologyThis article hasFast not Forward.been copyedited Published and formatted. on The November final version 7, may 2005 differ as from doi:10.1124/mol.105.017236 this version. MOLPHARM/2005/017236 Pharmacological properties of GABAA- receptors containing gamma1- subunits Khom S.1, Baburin I.1, Timin EN, Hohaus A., Sieghart W., Hering S. Downloaded from Department of Pharmacology and Toxicology, University of Vienna Center of Brain Research , Medical University of Vienna, Division of Biochemistry and molpharm.aspetjournals.org Molecular Biology at ASPET Journals on September 27, 2021 1 Copyright 2005 by the American Society for Pharmacology and Experimental Therapeutics. Molecular Pharmacology Fast Forward. Published on November 4, 2005 as DOI: 10.1124/mol.105.017236 This article has not been copyedited and formatted. The final version may differ from this version. MOLPHARM/2005/017236 Running Title: GABAA- receptors containing gamma1- subunits Corresponding author: Steffen Hering Department of Pharmacology and Toxicology University of Vienna Althanstrasse 14 Downloaded from A-1090 Vienna Telephone number: +43-1-4277-55301 Fax number: +43-1-4277-9553 molpharm.aspetjournals.org [email protected] Text pages: 29 at ASPET Journals on September 27, 2021 Tables: 2 Figures: 7 References: 26 Abstract: 236 words Introduction:575 words Discussion:1383 words 2 Molecular Pharmacology Fast Forward. Published on November 4, 2005 as DOI: 10.1124/mol.105.017236 This article has not been copyedited and formatted. The final version may differ from this version. MOLPHARM/2005/017236 Abstract GABAA receptors composed of α1, β2, γ1-subunits are expressed in only a few areas of the brain and thus represent interesting drug targets. -
A One Pot Synthesis of Novel Bioactive Tri-Substitute-Condensed
RESEARCH ARTICLE A One Pot Synthesis of Novel Bioactive Tri- Substitute-Condensed-Imidazopyridines that Targets Snake Venom Phospholipase A2 Nirvanappa C. Anilkumar1, Mahalingam S. Sundaram2, Chakrabhavi Dhananjaya Mohan3, Shobith Rangappa4, Krishna C. Bulusu5, Julian E. Fuchs5, Kesturu S. Girish2,6, Andreas Bender5, Basappa1*, Kanchugarakoppal S. Rangappa3* 1 Laboratory of Chemical Biology, Department of Chemistry, Bangalore University, Central College campus, Palace Road, Bangalore-560 001, Karnataka, India, 2 Department of Studies in Biochemistry, University of Mysore, Mysore-570 006, Karnataka, India, 3 Department of Studies in Chemistry, University of Mysore, Mysore-570 006, Karnataka, India, 4 Frontier Research Center for Post-genome Science and Technology Hokkaido University, Sapporo, 060–0808, Japan, 5 Centre for Molecular Science Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, United Kingdom, 6 Department of Studies and Research in Biochemistry, Tumkur University, Tumkur-572 103, Karnataka, India * [email protected] (KSR); [email protected] (B) OPEN ACCESS Citation: Anilkumar NC, Sundaram MS, Mohan CD, Abstract Rangappa S, Bulusu KC, Fuchs JE, et al. (2015) A One Pot Synthesis of Novel Bioactive Tri-Substitute- Drugs such as necopidem, saripidem, alpidem, zolpidem, and olprinone contain nitrogen- Condensed-Imidazopyridines that Targets Snake containing bicyclic, condensed-imidazo[1,2-α]pyridines as bioactive scaffolds. In this work, Venom Phospholipase A2. PLoS ONE 10(7): e0131896. doi:10.1371/journal.pone.0131896 we report a high-yield one pot synthesis of 1-(2-methyl-8-aryl-substitued-imidazo[1,2-α] in silico Editor: Luis Eduardo M Quintas, Universidade pyridin-3-yl)ethan-1-onefor the first-time. -
Yasakli Maddeler
YASAKLI MADDELER Ülkemizde yarış atlarında kullanılan/kullanılma ihtimali olan ilaçların/maddelerin belirlenmesinde; ilacın farmakolojisi (öncelikle etkisi, etki grubu), farmasötik şekli, kullanılma yolu, kullanılma alanı, yarış sonucunu etkileme durumu, ulusal mevzuata göre veteriner hekimlikte ve/veya yarış atlarında kullanmak için ruhsatlı/izinli olup-olmama durumu, etiket-dışı kullanılma gibi hususlar dikkate alınmıştır. Eşik değeri (Threshold level) olan maddelerin (vücutta şekillenirler, çevre ve yem kaynaklı olabilirler) miktarı, belirlenen miktarı aştığında yasaklı-madde kullanılması/doping ihlali olarak değerlendirilir. Tedavide kullanılan/tarama limiti (Screening level) olan maddelerle ilgili değerlendirmede; bu maddelerle ilgili olarak yapılan doping analizlerinde ölçülen miktar, idrarda/plazmada belirlenen tarama değerini aştığında yasaklı madde kullanılması/doping-ihlali olarakdeğerlendirilir. Ana madde yanında, izomeri, metaboliti, metabolit izomeri, tuzları, esterleri, eterleri, diğer türevleri, ön-ilaç da yasaklı-madde listesinde yer alır; doping analizinde ortaya konulmaları doping ihlali olarak değerlendirilir. Maddeler ve yasaklı uygulamalar 6 başlık altında toplanmıştır. Bu liste ilgili uluslararası kuruluşların mevzuat ve düzenlemeleri ile ilgili maddelerin Farmakolojik özellikleri ve etkileri dikkate alınarak hazırlanmıştır. 1. YasaklıMaddeler Yasaklı maddeler; yarış atlarında tıbbi olarak kullanım yeri olmayan, atın yarış performansını açık şekilde etkileyen maddelerdir. İllegal kullanılan maddeler (Türkiye’de veteriner -
In Silico Screening of Novel Α1-GABAA Receptor Pams Towards Schizophrenia Based on Combined Modeling Studies of Imidazo [1,2-A]-Pyridines
International Journal of Molecular Sciences Article In Silico Screening of Novel α1-GABAA Receptor PAMs towards Schizophrenia Based on Combined Modeling Studies of Imidazo [1,2-a]-Pyridines Xiaojiao Zheng 1, Chenchen Wang 1, Na Zhai 1, Xiaogang Luo 1,2, Genyan Liu 1,* and Xiulian Ju 1,* 1 Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430205, China; [email protected] (X.Z.); [email protected] (C.W.); [email protected] (N.Z.); [email protected] (X.L.) 2 School of Materials Science and Engineering, Zhengzhou University, No. 100 Science Avenue, Zhengzhou 450001, China * Correspondence: [email protected] (G.L.); [email protected] (X.J.) Abstract: The ionotropic GABAA receptor (GABAAR) has been proven to be an important target of atypical antipsychotics. A novel series of imidazo [1,2-a]-pyridine derivatives, as selective positive allosteric modulators (PAMs) of α1-containing GABAARs with potent antipsychotic activities, have been reported recently. To better clarify the pharmacological essentiality of these PAMs and explore novel antipsychotics hits, three-dimensional quantitative structure–activity relationships (3D-QSAR), molecular docking, pharmacophore modeling, and molecular dynamics (MD) were performed on 33 imidazo [1,2-a]-pyridines. The constructed 3D-QSAR models exhibited good predictive abilities. The dockings results and MD simulations demonstrated that hydrogen bonds, π–π stackings, and hydrophobic interactions play essential roles in the binding of these novel PAMs in the GABAAR Citation: Zheng, X.; Wang, C.; Zhai, binding pocket. Four hit compounds (DS01–04) were then screened out by the combination of N.; Luo, X.; Liu, G.; Ju, X. -
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. -
(12) Patent Application Publication (10) Pub. No.: US 2011/0158983 A1 Bascomb Et Al
US 2011 O158983A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0158983 A1 Bascomb et al. (43) Pub. Date: Jun. 30, 2011 (54) COMPOSITIONS AND METHODS FOR A63L/4045 (2006.01) MUCOSITIS AND ONCOLOGY THERAPES A638/00 (2006.01) A 6LX 3/57 (2006.01) (76) Inventors: Newell Bascomb, Chester Springs, A 6LX 3L/2197 (2006.01) PA (US); John Maki, Mendham, A63L/506 (2006.01) NJ (US); Fredric S. Young, Los A63L/454 (2006.01) Altos, CA (US) A6II 3/69 (2006.01) A63L/352 (2006.01) (21) Appl. No.: 12/921,145 A63L/382 (2006.01) A63L/337 (2006.01) (22) PCT Fled: Mar. 5, 2009 A6II 3/426 (2006.01) A63L/437 (2006.01) A63/675 (2006.01) S371 (c)(1), A63L/4375 2006.O1 (2), (4) Date: Mar. 14, 2011 A63L/435 308: Related U.S. Application Data 3. 7. 308: (60) Provisional application No. 61/034,122, filed on Mar. A638/02 (2006.01) 5, 2008, provisional application No. 61/079,768, filed A6IP35/00 (2006.01) on Jul. 10, 2008, provisional application No. 61/086, A6IPI/00 (2006.01) 437, filed on Aug. 5, 2008, provisional application No. B65D 69/00 (2006.01) 61/144,121, filed on Jan. 12, 2009. (52) U.S. Cl. ...................... 424/133.1: 514/423: 514/165; 514/567; 514/568: 514/411; 514/570; 514/420; Publication Classification 514/413: 514/226.5: 514/682: 514/569; 514/374; (51) Int. Cl. si...","...si...S. St. E. 30: 424/141.1; 514/19.3: 514/266.4: 514/252.18: A6 IK3I/60 (2006.01) 514/234.5; 514/.414: 514/252.19; 514/275; A6 IK3I/I96 (2006.01) 514/323: 514/64; 514/456; 514/437; 514/449; A6 IK3I/92 (2006.01) 514/365: 514/266.24; 514/285; 424/649; -
Drug and Medication Classification Schedule
KENTUCKY HORSE RACING COMMISSION UNIFORM DRUG, MEDICATION, AND SUBSTANCE CLASSIFICATION SCHEDULE KHRC 8-020-1 (11/2018) Class A drugs, medications, and substances are those (1) that have the highest potential to influence performance in the equine athlete, regardless of their approval by the United States Food and Drug Administration, or (2) that lack approval by the United States Food and Drug Administration but have pharmacologic effects similar to certain Class B drugs, medications, or substances that are approved by the United States Food and Drug Administration. Acecarbromal Bolasterone Cimaterol Divalproex Fluanisone Acetophenazine Boldione Citalopram Dixyrazine Fludiazepam Adinazolam Brimondine Cllibucaine Donepezil Flunitrazepam Alcuronium Bromazepam Clobazam Dopamine Fluopromazine Alfentanil Bromfenac Clocapramine Doxacurium Fluoresone Almotriptan Bromisovalum Clomethiazole Doxapram Fluoxetine Alphaprodine Bromocriptine Clomipramine Doxazosin Flupenthixol Alpidem Bromperidol Clonazepam Doxefazepam Flupirtine Alprazolam Brotizolam Clorazepate Doxepin Flurazepam Alprenolol Bufexamac Clormecaine Droperidol Fluspirilene Althesin Bupivacaine Clostebol Duloxetine Flutoprazepam Aminorex Buprenorphine Clothiapine Eletriptan Fluvoxamine Amisulpride Buspirone Clotiazepam Enalapril Formebolone Amitriptyline Bupropion Cloxazolam Enciprazine Fosinopril Amobarbital Butabartital Clozapine Endorphins Furzabol Amoxapine Butacaine Cobratoxin Enkephalins Galantamine Amperozide Butalbital Cocaine Ephedrine Gallamine Amphetamine Butanilicaine Codeine -
Marrakesh Agreement Establishing the World Trade Organization
No. 31874 Multilateral Marrakesh Agreement establishing the World Trade Organ ization (with final act, annexes and protocol). Concluded at Marrakesh on 15 April 1994 Authentic texts: English, French and Spanish. Registered by the Director-General of the World Trade Organization, acting on behalf of the Parties, on 1 June 1995. Multilat ral Accord de Marrakech instituant l©Organisation mondiale du commerce (avec acte final, annexes et protocole). Conclu Marrakech le 15 avril 1994 Textes authentiques : anglais, français et espagnol. Enregistré par le Directeur général de l'Organisation mondiale du com merce, agissant au nom des Parties, le 1er juin 1995. Vol. 1867, 1-31874 4_________United Nations — Treaty Series • Nations Unies — Recueil des Traités 1995 Table of contents Table des matières Indice [Volume 1867] FINAL ACT EMBODYING THE RESULTS OF THE URUGUAY ROUND OF MULTILATERAL TRADE NEGOTIATIONS ACTE FINAL REPRENANT LES RESULTATS DES NEGOCIATIONS COMMERCIALES MULTILATERALES DU CYCLE D©URUGUAY ACTA FINAL EN QUE SE INCORPOR N LOS RESULTADOS DE LA RONDA URUGUAY DE NEGOCIACIONES COMERCIALES MULTILATERALES SIGNATURES - SIGNATURES - FIRMAS MINISTERIAL DECISIONS, DECLARATIONS AND UNDERSTANDING DECISIONS, DECLARATIONS ET MEMORANDUM D©ACCORD MINISTERIELS DECISIONES, DECLARACIONES Y ENTEND MIENTO MINISTERIALES MARRAKESH AGREEMENT ESTABLISHING THE WORLD TRADE ORGANIZATION ACCORD DE MARRAKECH INSTITUANT L©ORGANISATION MONDIALE DU COMMERCE ACUERDO DE MARRAKECH POR EL QUE SE ESTABLECE LA ORGANIZACI N MUND1AL DEL COMERCIO ANNEX 1 ANNEXE 1 ANEXO 1 ANNEX -
An Inventory of Literature on the Relation Between Drug Use, Impaired Driving and Traffic Accidents
View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by National Documentation Centre on Drug Use E.M.C.D.D.A. DRUGS MISUSE RESEARCH DIVISION HEALTH RESEARCH BOARD An Inventory of Literature on the Relation between Drug Use, Impaired Driving and Traffic Accidents CT.97.EP.14 Research Team: Colin Gemmell Trinity College, Dublin Rosalyn Moran Drugs Misuse Research Division, Health Research Board James Crowley Professor, Transport Policy Research Institute, University College Dublin Richeal Courtney Medical Expert, for the Health Research Board EMCDDA: Lucas Wiessing February 1999 Please use the following citation: European Monitoring Centre for Drugs and Drug Addiction. An Inventory of Literature on the Relation betweenDrug Use, Impaired Driving and Traffic Accidents. (CT.97.EP.14) Lisbon: EMCDDA, February 1999. Contact Details Drugs Misuse Research Division Health Research Board 73 Lower Baggot Street Dublin 2 Ireland European Monitoring Centre for Drugs and Drug Addiction Rua Cruz de Santa Apolónia 23/25 1100, Lisboa Portugal. Further copies of this bibliography can be obtained from the EMCDDA at the above address. CREDITS Principal Researchers Ms Rosalyn Moran, Project Leader, Health Research Board Professor James Crowley, Professor, Transport Policy Research Institute, UCD Dr Richeal Courtney, Medical Expert, on behalf of the Health Research Board Research Assistants Colin Gemmell (Synthesis and Final Reports) Sarah Heywood (Literature Search and Collaborative Network) For the EMCDDA Lucas Wiessing -
Easy and Efficient Selenocyanation of Imidazoheterocycles Using Triselenodicyanide
Easy and efficient selenocyanation of imidazoheterocycles using triselenodicyanide Sébastien Redon, Anne Roly Obah Kosso, Julie Broggi, Patrice Vanelle To cite this version: Sébastien Redon, Anne Roly Obah Kosso, Julie Broggi, Patrice Vanelle. Easy and efficient selenocya- nation of imidazoheterocycles using triselenodicyanide. Tetrahedron Letters, Elsevier, 2017, 58 (28), pp.2771-2773. 10.1016/j.tetlet.2017.06.003. hal-01665068 HAL Id: hal-01665068 https://hal.archives-ouvertes.fr/hal-01665068 Submitted on 4 Jan 2018 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. Easy and efficient selenocyanation of imidazoheterocycles using triselenodicyanide Sébastien Redon,* Anne Roly Obah Kosso, Julie Broggi and Patrice Vanelle ∗ Aix Marseille Univ, CNRS, ICR Institut de Chimie Radicalaire, UMR 7273, Equipe Pharmaco-Chimie Radicalaire (LPCR), Faculté de Pharmacie, 27 Bd Jean Moulin CS–30064 13385 Marseille Cedex5, France ARTICLE INFO ABSTRACT Article history: The regioselective selenocyanation of imidazoheterocycles using triselenodicyanide at room Received temperature is reported. The electrophilic aromatic substitution of a broad range of substrates is Received in revised form promoted by the triselenodicyanide obtained by oxidative coupling of malononitrile and Accepted selenium dioxide, under an air atmosphere. The major advantages of the presented method are Available online an easy set-up, excellent yields, short reaction times, use of odorless and inexpensive reagents and easy purification of the final products.