Known Bioactives Library: Biomol ICCBL - 2012
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Biomol Average and SD Table S1.Xlsx
Compound GliNS1 G179NS G166NS average, n=5 STD average, n=3 STD average, n=3 STD INTRACELLULAR CALCIUM Antibiotic A-23187 0.00 0.00 0.10 0.07 0.15 0.14 INTRACELLULAR CALCIUM Ryanodine 1.04 0.14 1.03 0.03 1.03 0.03 INTRACELLULAR CALCIUM Cyclopiazonic acid 1.01 0.06 0.88 0.05 0.92 0.06 INTRACELLULAR CALCIUM Gingerol 1.00 0.06 0.91 0.01 1.01 0.06 INTRACELLULAR CALCIUM Thapsigargin 0.00 0.01 0.00 0.00 0.10 0.12 INTRACELLULAR CALCIUM TMB-8 0.89 0.07 0.91 0.05 0.94 0.03 INTRACELLULAR CALCIUM Dantrolene 0.91 0.08 0.98 0.05 0.94 0.01 CALCIUM CHANNELS Amiloride 1.01 0.07 1.01 0.04 1.03 0.05 CALCIUM CHANNELS Benzamil 0.83 0.08 0.83 0.12 0.96 0.04 CALCIUM CHANNELS BAY K-8644 0.93 0.13 0.93 0.09 1.07 0.14 CALCIUM CHANNELS Diltiazem 0.96 0.07 0.99 0.12 0.94 0.14 CALCIUM CHANNELS L-cis-Diltiazem 0.91 0.17 1.01 0.12 0.95 0.12 CALCIUM CHANNELS Flunarizine 0.85 0.08 1.00 0.06 0.85 0.05 CALCIUM CHANNELS FPL-64176 0.99 0.11 0.95 0.07 1.05 0.05 CALCIUM CHANNELS Nifedipine 1.06 0.17 0.95 0.12 1.03 0.09 CALCIUM CHANNELS Nimodipine 1.05 0.06 0.95 0.03 1.06 0.17 CALCIUM CHANNELS Nitrendipine 0.99 0.07 0.96 0.10 1.04 0.09 CALCIUM CHANNELS SDZ-202791 R(-) 1.01 0.08 0.92 0.06 1.01 0.08 CALCIUM CHANNELS SKF-96365 0.73 0.05 0.70 0.11 0.69 0.04 CALCIUM CHANNELS Tetrandrine 0.47 0.07 0.76 0.16 0.87 0.20 CALCIUM CHANNELS Verapamil 1.01 0.02 0.89 0.07 1.06 0.20 CALCIUM CHANNELS Methoxy Verapamil 0.93 0.14 0.96 0.07 0.93 0.13 CALCIUM CHANNELS Bepridil 0.70 0.16 0.92 0.15 0.84 0.14 CALCIUM CHANNELS Amiodarone 0.32 0.12 0.58 0.07 0.48 0.23 CALCIUM CHANNELS YS035 1.00 0.16 -
Central Valley Toxicology Drug List
Chloroform ~F~ Lithium ~A~ Chlorpheniramine Loratadine Famotidine Acebutolol Chlorpromazine Lorazepam Fenoprofen Acetaminophen Cimetidine Loxapine Fentanyl Acetone Citalopram LSD (Lysergide) Fexofenadine 6-mono- Clomipramine acetylmorphine Flecainide ~M~ Clonazepam a-Hydroxyalprazolam Fluconazole Maprotiline Clonidine a-Hydroxytriazolam Flunitrazepam MDA Clorazepate Albuterol Fluoxetine MDMA Clozapine Alprazolam Fluphenazine Medazepam Cocaethylene Amantadine Flurazepam Meperidine Cocaine 7-Aminoflunitrazepam Fluvoxamine Mephobarbital Codeine Amiodarone Fosinopril Meprobamate Conine Amitriptyline Furosemide Mesoridazine Cotinine Amlodipine Methadone Cyanide ~G~ Amobarbital Methanol Cyclobenzaprine Gabapentin Amoxapine d-Methamphetamine Cyclosporine GHB d-Amphetamine l-Methamphetamine Glutethamide l-Amphetamine ~D~ Methapyrilene Guaifenesin Aprobarbital Demoxepam Methaqualone Atenolol Desalkylfurazepam ~H~ Methocarbamol Atropine Desipramine Halazepam Methylphenidate ~B~ Desmethyldoxepin Haloperidol Methyprylon Dextromethoraphan Heroin Metoclopramide Baclofen Diazepam Hexobarbital Metoprolol Barbital Digoxin Hydrocodone Mexiletine Benzoylecgonine Dihydrocodein Hydromorphone Midazolam Benzphetamine Dihydrokevain Hydroxychloroquine Mirtazapine Benztropine Diltiazem Hydroxyzine Morphine (Total/Free) Brodificoum Dimenhydrinate Bromazepam ~N~ Diphenhydramine ~I~ Bupivacaine Nafcillin Disopyramide Ibuprofen Buprenorphine Naloxone Doxapram Imipramine Bupropion Naltrexone Doxazosin Indomethacin Buspirone NAPA Doxepin Isoniazid Butabarbital Naproxen -
CAS Number Index
2334 CAS Number Index CAS # Page Name CAS # Page Name CAS # Page Name 50-00-0 905 Formaldehyde 56-81-5 967 Glycerol 61-90-5 1135 Leucine 50-02-2 596 Dexamethasone 56-85-9 963 Glutamine 62-44-2 1640 Phenacetin 50-06-6 1654 Phenobarbital 57-00-1 514 Creatine 62-46-4 1166 α-Lipoic acid 50-11-3 1288 Metharbital 57-22-7 2229 Vincristine 62-53-3 131 Aniline 50-12-4 1245 Mephenytoin 57-24-9 1950 Strychnine 62-73-7 626 Dichlorvos 50-23-7 1017 Hydrocortisone 57-27-2 1428 Morphine 63-05-8 127 Androstenedione 50-24-8 1739 Prednisolone 57-41-0 1672 Phenytoin 63-25-2 335 Carbaryl 50-29-3 569 DDT 57-42-1 1239 Meperidine 63-75-2 142 Arecoline 50-33-9 1666 Phenylbutazone 57-43-2 108 Amobarbital 64-04-0 1648 Phenethylamine 50-34-0 1770 Propantheline bromide 57-44-3 191 Barbital 64-13-1 1308 p-Methoxyamphetamine 50-35-1 2054 Thalidomide 57-47-6 1683 Physostigmine 64-17-5 784 Ethanol 50-36-2 497 Cocaine 57-53-4 1249 Meprobamate 64-18-6 909 Formic acid 50-37-3 1197 Lysergic acid diethylamide 57-55-6 1782 Propylene glycol 64-77-7 2104 Tolbutamide 50-44-2 1253 6-Mercaptopurine 57-66-9 1751 Probenecid 64-86-8 506 Colchicine 50-47-5 589 Desipramine 57-74-9 398 Chlordane 65-23-6 1802 Pyridoxine 50-48-6 103 Amitriptyline 57-92-1 1947 Streptomycin 65-29-2 931 Gallamine 50-49-7 1053 Imipramine 57-94-3 2179 Tubocurarine chloride 65-45-2 1888 Salicylamide 50-52-2 2071 Thioridazine 57-96-5 1966 Sulfinpyrazone 65-49-6 98 p-Aminosalicylic acid 50-53-3 426 Chlorpromazine 58-00-4 138 Apomorphine 66-76-2 632 Dicumarol 50-55-5 1841 Reserpine 58-05-9 1136 Leucovorin 66-79-5 -
Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Cr
Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Crizotinib (PF-02341066) 1 4 55 Docetaxel 1 5 98 Anastrozole 1 6 25 Cladribine 1 7 23 Methotrexate 1 8 -187 Letrozole 1 9 65 Entecavir Hydrate 1 10 48 Roxadustat (FG-4592) 1 11 19 Imatinib Mesylate (STI571) 1 12 0 Sunitinib Malate 1 13 34 Vismodegib (GDC-0449) 1 14 64 Paclitaxel 1 15 89 Aprepitant 1 16 94 Decitabine 1 17 -79 Bendamustine HCl 1 18 19 Temozolomide 1 19 -111 Nepafenac 1 20 24 Nintedanib (BIBF 1120) 1 21 -43 Lapatinib (GW-572016) Ditosylate 1 22 88 Temsirolimus (CCI-779, NSC 683864) 1 23 96 Belinostat (PXD101) 1 24 46 Capecitabine 1 25 19 Bicalutamide 1 26 83 Dutasteride 1 27 68 Epirubicin HCl 1 28 -59 Tamoxifen 1 29 30 Rufinamide 1 30 96 Afatinib (BIBW2992) 1 31 -54 Lenalidomide (CC-5013) 1 32 19 Vorinostat (SAHA, MK0683) 1 33 38 Rucaparib (AG-014699,PF-01367338) phosphate1 34 14 Lenvatinib (E7080) 1 35 80 Fulvestrant 1 36 76 Melatonin 1 37 15 Etoposide 1 38 -69 Vincristine sulfate 1 39 61 Posaconazole 1 40 97 Bortezomib (PS-341) 1 41 71 Panobinostat (LBH589) 1 42 41 Entinostat (MS-275) 1 43 26 Cabozantinib (XL184, BMS-907351) 1 44 79 Valproic acid sodium salt (Sodium valproate) 1 45 7 Raltitrexed 1 46 39 Bisoprolol fumarate 1 47 -23 Raloxifene HCl 1 48 97 Agomelatine 1 49 35 Prasugrel 1 50 -24 Bosutinib (SKI-606) 1 51 85 Nilotinib (AMN-107) 1 52 99 Enzastaurin (LY317615) 1 53 -12 Everolimus (RAD001) 1 54 94 Regorafenib (BAY 73-4506) 1 55 24 Thalidomide 1 56 40 Tivozanib (AV-951) 1 57 86 Fludarabine -
Kava - the Unfolding Story: Report on a Work-In-Progress
Article Kava - the unfolding story: Report on a work-in-progress. Denham, Alison, McIntyre, Michael and Whitehouse, Jule Available at http://clok.uclan.ac.uk/9455/ Denham, Alison, McIntyre, Michael and Whitehouse, Jule Kava - the unfolding story: Report on a work-in-progress. Journal of Alternative and Complementary Medicine, 8 (3). pp. 237-263. It is advisable to refer to the publisher’s version if you intend to cite from the work. For more information about UCLan’s research in this area go to http://www.uclan.ac.uk/researchgroups/ and search for <name of research Group>. For information about Research generally at UCLan please go to http://www.uclan.ac.uk/research/ All outputs in CLoK are protected by Intellectual Property Rights law, including Copyright law. Copyright, IPR and Moral Rights for the works on this site are retained by the individual authors and/or other copyright owners. Terms and conditions for use of this material are defined in the policies page. CLoK Central Lancashire online Knowledge www.clok.uclan.ac.uk THE JOURNAL OF ALTERNATIVE AND COMPLEMENTARY MEDICINE Volume 8, Number 3, 2002, pp. 237–263 © Mary Ann Liebert, Inc. SPECIAL REPORT Kava—the Unfolding Story: Report on a Work-in-Progress ALISON DENHAM, B.A. (Soc.), M.N.I.M.H., 1 MICHAEL McINTYRE, M.A., F.N.I.M.H., F.R.C.H.M., M.B.Ac.C., 2 and JULIE WHITEHOUSE, Ph.D., M.N.I.M.H. 3 ABSTRACT This paper, originated as a submission (now updated) to the U.K. Medicines Control Agency and Committee of Safety of Medicines (CSM) on January 11, 2002, in response to a report circu- lated by the German Federal Institute for Drugs and Medical Products (German initials are BfArM), a compilation of which is summarized in Appendix 2. -
Letters to the Editor
Letters to the Editor Internet Pharmacy Prescription complete the medication database. Of course, patients can abuse and Phentermine Overdose any medications, so collaboration between pharmacies and physicians is essential to minimize this risk. Sir: The Internet is now widely used by patients for both Dr. Takeshita reports no financial or other relationship relevant to the health information and prescription services. Yet, a MEDLINE subject matter of this letter. search in January 2002 using the phrase “Internet pharmacy” showed a total of 99 articles; nearly all were geared toward REFERENCES health care management or the general public. There are only a few published reports of bad outcome resulting from medical 1 1. Crocco AG, Villasis-Keever M, Jadad AR. Analysis of cases of information obtained from the Internet. The U.S. Food and harm associated with use of health information on the Internet. Drug Administration noted 326 Internet sites selling pharma- JAMA 2002;287:2867–2871 ceutical products.2 The exact numbers are difficult to quantify 2. Henney JE. Cyberpharmacies and the role of the US Food and Drug as Web sites are constantly changing. I report a case of overdose Administration. J Med Internet Res 2001;3:E3 with phentermine that was obtained through an Internet 3. Gardin JM, Schumacher D, Constantine G, et al. Valvular abnormali- pharmacy. ties and cardiovascular status following exposure to dexfenfluramine or phentermine/fenfluramine. JAMA 2000;283:1703–1709 4. Koury E, Stone CK, Stapczynski JS, et al. Sympathetic overactivity Case report. Ms. A, a 20-year-old woman with a prior from fenfluramine-phentermine overdose. -
Please Check Desired Specimen Type & Drugs/Drug Classes for Testing
PATIENT INFORMATION PRACTICE INFORMATION ____________________________________ _____________________________________ _______ ________________________ __________________ Last Name First Name MI Facility/Group Referring Physician ________/________/________ Social Security: _________-_________-________ ☐ Male ☐ Female ___________________________________________ Date of Birth Address NPI Provider Nr. __________________________________________________________________ Address DIAGNOSTIC CODES (ICD-10 codes): _____________________________ ☐ Self-Pay (attach Information) ☐ Commercial Insurance (attach copy) ☐ W/C (Date of Injury): ____________ ☐ Medicare (attach copy of Insurance) I certify that I have voluntarily provided a fresh unadulterated urine/dried blood/oral fluid specimen for analytical testing. The information provided on this form and on the label affixed to the specimen is accurate. I authorize lab to release the results of this testing to the ordering physician. I also authorize lab to bill my insurance provider and to receive payment of benefits for the tests ordered by my physician. I further authorize lab and the ordering physician to release to my insurance provider any medical information necessary to process this claim. I acknowledge that lab may be an out-of-network facility with my insurance provider. Patient Signature (or Legal Guardian): ___________________________________________________________________________ Date: _______________ TEST PANELS (please check desired specimen type & drugs/drug classes for testing): ☐ URINE -
Kava Kava Extract Is Available from Ashland Chemical Co., Mini Star International, Inc., and QBI (Quality Botanical Ingredients, Inc.)
SUMMARY OF DATA FOR CHEMICAL SELECTION Kava Kava 9000-38-8; 84696-40-2 November 1998 TABLE OF CONTENTS Basis for Nomination Chemical Identification Production Information Use Pattern Human Exposure Regulatory Status Evidence for Possible Carcinogenic Activity Human Data Animal Data Metabolism Other Biological Effects Structure-Activity Relationships References BASIS OF NOMINATION TO THE CSWG Kava kava is brought to the attention of the CSWG because it is a rapidly growing, highly used dietary supplement introduced into the mainstream U.S. market relatively recently. Through this use, millions of consumers using antianxiety preparations are potentially exposed to kava kava. A traditional beverage of various Pacific Basin countries, kava clearly has psychoactive properties. The effects of its long-term consumption have not been documented adequately; preliminary studies suggest possibly serious organ system effects. The potential carcinogenicity of kava and its principal constituents are unknown. INPUT FROM GOVERNMENT AGENCIES/INDUSTRY The U.S. Pharmacopeia is in the process of reviewing kava kava. No decision on preparation of a monograph has been made. SELECTION STATUS ACTION BY CSWG: 12/14/98 Studies requested: - Toxicological evaluation, to include studies of reproductive toxicity and neurotoxicity - Genotoxicity Priority: High Rationale/Remarks: - Significant human exposure - Leading dietary supplement with rapidly growing use - Concern that kava has been promoted as a substitute for ritilin in children - Test extract standardized to 30 percent kavalactones - NCI is conducting studies in Salmonella typhimurium CHEMICAL IDENTIFICATION CAS Registry Number: 9000-38-8 Kava-kava resin (8CI) Chemical Abstract Service Name: 84696-40-2 CAS Registry Number: Pepper (Piper), P. methysticum, ext. Chemical Abstract Service Name: Extract of kava; kava extract; Piper Synonyms and Trade Names: methisticum extract Description: The tropical shrub Piper methysticum is widely cultivated in the South Pacific. -
Kavain, the Major Constituent of the Anxiolytic Kava
RESEARCH ARTICLE Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism Han Chow Chua1, Emilie T. H. Christensen1,2, Kirsten Hoestgaard-Jensen2, Leonny Y. Hartiadi1, Iqbal Ramzan1, Anders A. Jensen2, Nathan L. Absalom1, Mary Chebib1* 1 Faculty of Pharmacy, The University of Sydney, Sydney, New South Wales, Australia, 2 Department of a11111 Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark * [email protected] Abstract OPEN ACCESS Extracts of the pepper plant kava (Piper methysticum) are effective in alleviating anxiety in Citation: Chua HC, Christensen ETH, Hoestgaard- Jensen K, Hartiadi LY, Ramzan I, Jensen AA, et al. clinical trials. Despite the long-standing therapeutic interest in kava, the molecular target(s) (2016) Kavain, the Major Constituent of the Anxiolytic of the pharmacologically active constituents, kavalactones have not been established. γ- Kava Extract, Potentiates GABAA Receptors: Aminobutyric acid type A receptors (GABAARs) are assumed to be the in vivo molecular tar- Functional Characteristics and Molecular Mechanism. PLoS ONE 11(6): e0157700. doi:10.1371/journal. get of kavalactones based on data from binding assays, but evidence in support of a direct pone.0157700 interaction between kavalactones and GABAARs is scarce and equivocal. In this study, we Editor: Steven Barnes, Dalhousie University, characterised the functional properties of the major anxiolytic kavalactone, kavain at human CANADA recombinant α1β2, β2γ2L, αxβ2γ2L (x = 1, 2, 3 and 5), α1βxγ2L (x = 1, 2 and 3) and α4β2δ Received: March 24, 2016 GABAARs expressed in Xenopus oocytes using the two-electrode voltage clamp technique. -
Un Novedoso Enfoque Para El Diseño De Fármacos Antimicrobianos Asistido Por Computadora
TOMOCOMD-CARDD: Un Novedoso Enfoque para el Diseño de Fármacos Antimicrobianos Asistido por Computadora Autora: Yasnay Valdés Rodríguez. Tutores: Prof. Dr. Yovani Marrero Ponce. Prof. MSc. Ricardo Medina Marrero. 2005-2006 La ignorancia afirma o niega rotundamente; la ciencia duda… Voltaire (1694-1778) Quiero dedicar este trabajo a todas aquellas personas que me aprecian y desean lo mejor para mi, especialmente a mis padres. A mi padre Dedico este trabajo con mucho amor, por hacerme comprender que siempre se puede llegar mas lejos, y que no hay nada imposible, solamente hay que luchar... A mi madre Por su infinita bondad, por su sacrificio inigualable. A mis familiares Por todo su apoyo y ayuda que me han mostrado incondicionalmente. A mi hermano Por ser mi fuente de inspiración. A la humanidad “...porque si supiera que el mundo se acaba mañana, yo, hoy todavía, plantaría un árbol” Quiero agradecer a todas aquellas personas que me han ayudado a realizar este sueño: A mis padres por todo el sacrificio realizado, y aún parecerles poco, los amo mucho. A mi madre por estar siempre a mi lado en los buenos y malos momentos ayudándome a levantarme en cualquier recaída. A mi padre por guiarme en la vida y brindarme sus consejos siempre útiles, por darme fuerza y vitalidad. A mi mayor tesoro, mi hermano, que me alumbra de esperanza día a día. A mis tías y primos que me ayudaron mucho, aún estando lejos. A mi novio que me apoyo en todas mis decisiones y con paciencia supo ayudarme. A mis tutores y cotutores que siempre me dieron la mano; especialmente a Yovani por su paciencia, a quien debo gran parte de mi formación como profesional por sus exigencias. -
Big Conductance Calcium-Activated Potassium Channel Openers Control Spasticity Without Sedation
British Journal of British Journal of Pharmacology (2017) 174 2662–2681 2662 BJP Pharmacology RESEARCH PAPER Big conductance calcium-activated potassium channel openers control spasticity without sedation Correspondence Professor David Baker, Neuroimmunology Unit, Blizard Institute, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, 4 Newark Street, Whitechapel, London E1 4AT, UK. E-mail: [email protected] Received 5 January 2017; Revised 27 April 2017; Accepted 17 May 2017 David Baker1,2,* ,GarethPryce1,2,*, Cristina Visintin2,3,SofiaSisay1, Alexander I Bondarenko4,5, WSVanessaHo6, Samuel J Jackson1, Thomas E Williams1, Sarah Al-Izki1, Ioanna Sevastou3, Masahiro Okuyama3, Wolfgang F Graier4, Lesley A Stevenson6,CarolynTanner7,RuthRoss7, Roger G Pertwee7, Christopher M Henstridge8,AndrewJIrving8, Jesse Schulman9,KeithPowell9,MarkDBaker1, Gavin Giovannoni1,2 and David L Selwood3,* 1Neuroimmunology Unit, Blizard Institute, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, London, UK, 2Department of Neuroinflammation, UCL Institute of Neurology, University College London, London, UK, 3Department of Medicinal Chemistry, UCL Wolfson Institute for Biomedical Research, University College London, London, UK, 4Institute of Molecular Biology and Biochemistry, Medical University of Graz, Graz, Austria, 5A.A. Bogomoletz Institute of Physiology, Kiev, Ukraine, 6Vascular Biology Research Centre. St. George’s, University of London, London, UK, 7Department of Biomedical Sciences, -
Functional Analysis of Penicillium Paxilli Genes Required for Biosynthesis of Paxilline
Copyright is owned by the Author of the thesis. Permission is given for a copy to be downloaded by an individual for the purpose of research and private study only. The thesis may not be reproduced elsewhere without the permission of the Author. Functional analysis of Penicillium paxilli genes required for biosynthesis of paxilline This thesis is presented in partial fulfilment of the requirements for the degree of Doctor of Philosophy (PhD) In Biochemistry at Massey University, Palmerston North, New Zealand Sanjay Saikia 2006 ABSTRACT Paxilline belongs to a large, structurally and functionally diverse group of indole-diterpenes and is synthesised by the filamentous fungus Penicillium paxilli. A gene cluster for paxilline biosynthesis in P. paxilli has been identified and characterised. However, none of the steps proposed in the biosynthesis of paxilline or paxilline-like indole-diterpenes have been validated . In some diterpene-producing fi lamentous fungi, including P. paxilli, two distinct copies of geranylgeranyl diphosphate (GGPP) synthase, that catalyses the committed step in diterpene biosynthesis, have been identified . However, the biological significance of the presence of two distinct GGPP synthases is not known. In this study, biochemical analysis of the paxilline gene products in P. paxilli and subcellular localisation of the two P. paxilli GGPP synthases, Ggs1 and PaxG, were carried out. Transfer of constructs containing different combinations of pax genes into a pax cluster negative deletion derivative of P. paxilli identified four Pax proteins that are required for the biosynthesis of a paxilline intermediate, paspaline. These proteins are PaxG, a GGPP synthase, PaxM, a FAD-dependent monooxygenase, PaxB, a putative membrane protein, and PaxC, a prenyltransferase.