DOCSLIB.ORG

Sodium Channel Na Channels; Na+ Channels

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text

Load more

Sodium Channel Na channels; Na+ channels Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's plasma membrane. They are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials. Voltage-gated Na+ channels can exist in any of three distinct states: deactivated (closed), activated (open), or inactivated (closed). Ligand-gated sodium channels are activated by binding of a ligand instead of a change in membrane potential. www.MedChemExpress.com 1 Sodium Channel Inhibitors, Agonists, Antagonists, Activators & Modulators (+)-Kavain (-)-Sparteine sulfate pentahydrate Cat. No.: HY-B1671 ((-)-Lupinidine sulfate pentahydrate) Cat. No.: HY-B1304 (+)-Kavain, a main kavalactone extracted from Piper (-)-Sparteine sulfate pentahydrate ((-)-Lupinidine methysticum, has anticonvulsive properties, sulfate pentahydrate) is a class 1a antiarrhythmic attenuating vascular smooth muscle contraction agent and a sodium channel blocker. It is an through interactions with voltage-dependent Na+ alkaloid, can chelate the bivalents calcium and and Ca2+ channels. magnesium. Purity: 99.98% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 50 mg (Rac)-AMG8379 20(S)-Ginsenoside Rg3 ((Rac)-AMG8380) Cat. No.: HY-108425B (20(S)-Propanaxadiol; S-ginsenoside Rg3) Cat. No.: HY-N0603 (Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of 20(S)-Ginsenoside Rg3 is the main component of Red AMG8379. AMG8379 is a potent, orally active and ginseng. Ginsenoside Rg3 inhibits Na+ and selective sulfonamide antagonist of NaV1.7, with hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, μM, respectively. 20(S)-Ginsenoside Rg3 also respectively . inhibits Aβ levels, NF-κB activity, and COX-2 expression. Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg 5-(N,N-Hexamethylene)-amiloride A-317567 (Hexamethylene amiloride; HMA) Cat. No.: HY-128067 Cat. No.: HY-122135 5-(N,N-Hexamethylene)-amiloride (Hexamethylene A-317567 is a potent acid-sensing ion channel 3 amiloride) derives from an amiloride and is a (ASIC-3) inhibitor with an IC50 of 1.025 μM. potent Na+/H+ exchanger inhibitor, which A-317567 has antidepressant and antinociception decreases the intracellular pH (pHi) and induces effects. apoptosis in leukemic cells. Purity: 98.42% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg A-803467 A-887826 Cat. No.: HY-11079 Cat. No.: HY-100080 A 803467 is a selective Nav1.8 sodium channel A-887826 is a potent, selective, oral bioavailable blocker with an IC50 of 8 nM; over 100-fold more and voltage-dependent Na(v)1.8 sodium channel selective vs. human Nav1.2, 1.3, 1.5 and 1.7. blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo. Purity: 98.51% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 1 mg, 5 mg Ajmaline AM-2099 (Cardiorythmine; (+)-Ajmaline) Cat. No.: HY-B1167 Cat. No.: HY-100727 Ajmaline (Cardiorythmine) is a sodium channel AM-2099 is a potent and selective inhibitor of blocking, class 1A anti-arrhythmic agent. Ajmaline voltage-gated sodium channel Nav1.7 with an IC50 blocks HERG currents with an IC50 of 1 μM in HEK of 0.16 μM for human Nav1.7. cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia. Purity: 99.84% Purity: 98.02% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] AMG8380 Amiloride Cat. No.: HY-108425A (MK-870) Cat. No.: HY-B0285 AMG8380, an orally active and less active Amiloride (MK-870) is an inhibitor of both enantiomer of AMG8379, can serves as a negative epithelial sodium channel (ENaC) and control. AMG8380 inhibits human and mouse urokinase-type plasminogen activator receptor voltage-gated sodium channel NaV1.7 with IC50s of (uTPA). Amiloride is a blocker of polycystin-2 0.907 and 0.387 μM, respectively. (PC2; TRPP2) channel. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg Amiloride hydrochloride Amiloride hydrochloride dihydrate (MK-870 hydrochloride) Cat. No.: HY-B0285A (MK-870 hydrochloride dihydrate) Cat. No.: HY-B0285B Amiloride hydrochloride (MK-870 hydrochloride) is Amiloride hydrochloride dihydrate (MK-870 an inhibitor of both epithelial sodium channel hydrochloride dihydrate) is an inhibitor of both (ENaC) and urokinase-type plasminogen activator epithelial sodium channel (ENaC) and receptor (uTPA). Amiloride hydrochloride is a urokinase-type plasminogen activator receptor blocker of polycystin-2 (PC2; TRPP2) channel. (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel. Purity: 99.71% Purity: 99.50% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg Amitriptyline hydrochloride Annonacin Cat. No.: HY-B0527A Cat. No.: HY-N2877 Amitriptyline hydrochloride is an inhibitor of Annonacin is an Acetogenin and promotes serotonin reuptake transporter (SERT) and cytotoxicity via a pathway inhibiting the noradrenaline reuptake transporter (NET), with Kis mitochondrial complex. Annonacin is the active of 3.45 nM and 13.3 nM for human SERT and NET, agent found in Graviola leaf extract to act as an respectively. inhibitor of sodium/potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pumps. Purity: 99.56% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 5 mg APETx2 APETx2 TFA Cat. No.: HY-P1346 Cat. No.: HY-P1346A APETx2, a sea anemone peptide from Anthopleura APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses its external side. APETx2 could reverses acidinduced and inflammatory pain. acidinduced and inflammatory pain. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg AZD-3161 Benzamil Cat. No.: HY-117714 (Benzylamiloride) Cat. No.: HY-B1546 AZD-3161 is a potent and selective blocker of Benzamil (Benzylamiloride), an Amiloride analogue, + 2+ NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can is a Na /Ca exchanger (NCX) inhibitor be used for the research of neuropathic and (IC50~100 nM). Benzamil also is a non-selective inflammatory pain. Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg www.MedChemExpress.com 3 Benzamil hydrochloride Benzocaine (Benzylamiloride hydrochloride) Cat. No.: HY-B1546A Cat. No.: HY-Y0258 Benzamil hydrochloride (Benzylamiloride Benzocaine shares a common receptor with all othe hydrochloride), an Amiloride analogue, is a rLAs in the voltage-gated Na+ channel, with an + 2+ Na /Ca exchanger (NCX) inhibitor (IC50~100 IC50 of 0.8 mM tested with a potential of +30 mV. nM). Purity: 99.60% Purity: 99.98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 500 mg BI 01383298 BI-9627 Cat. No.: HY-124738 Cat. No.: HY-18071 BI 01383298 is a potent inhibitor of the BI-9627 is potent sodium-hydrogen exchanger sodium-citrate co-transporter (SLC13A5) that isoform 1 (NHE1) inhibitor, with IC50s of 6 and is highly expressed in the liver. 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. Purity: 99.96% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg BI-9627 hydrochloride Bifenthrin Cat. No.: HY-18071A Cat. No.: HY-B0824 BI-9627 hydrochloride is potent sodium-hydrogen Bifenthrin is a synthetic pyrethroid insecticide exchanger isoform 1 (NHE1) inhibitor, with IC50s that prolongs opening of sodium channels resulting of 6 and 31 nM in intracellular pH recovery (pHi) in membrane depolarization and conductance block and human platelet swelling assays, respectively. in the insect nervous system. Purity: >98% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg Brevetoxin B Brevetoxin-3 (Brevetoxin-2; PbTx-2) Cat. No.: HY-12546 (PbTx-3) Cat. No.: HY-12545 Brevetoxin B (Brevetoxin-2; PbTx-2) is a Brevetoxin-3 (PbTx-3) is a potent allosteric polyketide neurotoxin produced by Karenia species voltage-gated Na+ channel activator and has and other dinoflagellates.
Recommended publications
  • Chapter 11 Local Anesthetics

    Chapter 11 Local Anesthetics

    Chapter LOCAL ANESTHETICS 11 Kenneth Drasner HISTORY MECHANISMS OF ACTION AND FACTORS ocal anesthesia can be defined as loss of sensation in AFFECTING BLOCK L a discrete region of the body caused by disruption of Nerve Conduction impulse generation or propagation. Local anesthesia can Anesthetic Effect and the Active Form of the be produced by various chemical and physical means. Local Anesthetic However, in routine clinical practice, local anesthesia is Sodium Ion Channel State, Anesthetic produced by a narrow class of compounds, and recovery Binding, and Use-Dependent Block is normally spontaneous, predictable, and complete. Critical Role of pH Lipid Solubility Differential Local Anesthetic Blockade Spread of Local Anesthesia after Injection HISTORY PHARMACOKINETICS Cocaine’s systemic toxicity, its irritant properties when Local Anesthetic Vasoactivity placed topically or around nerves, and its substantial Metabolism potential for physical and psychological dependence gene- Vasoconstrictors rated interest in identification of an alternative local 1 ADVERSE EFFECTS anesthetic. Because cocaine was known to be a benzoic Systemic Toxicity acid ester (Fig. 11-1), developmental strategies focused Allergic Reactions on this class of chemical compounds. Although benzo- caine was identified before the turn of the century, its SPECIFIC LOCAL ANESTHETICS poor water solubility restricted its use to topical anesthe- Amino-Esters sia, for which it still finds some limited application in Amino-Amide Local Anesthetics modern clinical practice. The
  • In Silico Methods for Drug Repositioning and Drug-Drug Interaction Prediction

    In Silico Methods for Drug Repositioning and Drug-Drug Interaction Prediction

    In silico Methods for Drug Repositioning and Drug-Drug Interaction Prediction Pathima Nusrath Hameed ORCID: 0000-0002-8118-9823 Submitted in total fulfilment of the requirements for the degree of Doctor of Philosophy Department of Mechanical Engineering THE UNIVERSITY OF MELBOURNE May 2018 Copyright © 2018 Pathima Nusrath Hameed All rights reserved. No part of the publication may be reproduced in any form by print, photoprint, microfilm or any other means without written permission from the author. Abstract Drug repositioning and drug-drug interaction (DDI) prediction are two fundamental ap- plications having a large impact on drug development and clinical care. Drug reposi- tioning aims to identify new uses for existing drugs. Moreover, understanding harmful DDIs is essential to enhance the effects of clinical care. Exploring both therapeutic uses and adverse effects of drugs or a pair of drugs have significant benefits in pharmacology. The use of computational methods to support drug repositioning and DDI prediction en- able improvements in the speed of drug development compared to in vivo and in vitro methods. This thesis investigates the consequences of employing a representative training sam- ple in achieving better performance for DDI classification. The Positive-Unlabeled Learn- ing method introduced in this thesis aims to employ representative positives as well as reliable negatives to train the binary classifier for inferring potential DDIs. Moreover, it explores the importance of a finer-grained similarity metric to represent the pairwise drug similarities. Drug repositioning can be approached by new indication detection. In this study, Anatomical Therapeutic Chemical (ATC) classification is used as the primary source to determine the indications/therapeutic uses of drugs for drug repositioning.
  • 3-Local-Anesthetics.Pdf

    3-Local-Anesthetics.Pdf

    Overview • Local anesthetics produce a transient and reversible loss of sensation (analgesia) in a circumscribed region of the body without loss of consciousness. • Normally, the process is completely reversible. • Local anesthetics are generally classified as either esters or amides and are usually linked to: – a lipophilic aromatic group – to a hydrophilic, ionizable tertiary (sometimes secondary) amine. • Most are weak bases with pKa ( 8 – 9), and at physiologic pH they are primarily in the charged, cationic form. • The potency of local anesthetics is positively correlated with their lipid solubility, which may vary 16-fold, and negatively correlated with their molecular size. • These anesthetics are selected for use on the basis of: 1. the duration of drug action • Short: 20 min • Intermediate: 1—1.5 hrs • Long: 2—4 hrs 2. effectiveness at the administration site 3. potential for toxicity Mechanism of action Local anesthetics act by blocking sodium channels and the conduction of action potentials along sensory nerves. • Blockade is voltage dependent and time dependent. a. At rest, the voltage-dependent sodium (Na+) channels of sensory nerves are in the resting (closed) state. • Following the action potential the Na+ channel becomes active (open) and then converts to an inactive (closed) state that is insensitive to depolarization. • Following repolarization of the plasma membrane there is a slow reversion of channels from the inactive to the resting state, which can again be activated by depolarization. • During excitation the cationic charged form of local anesthetics interacts preferentially with the inactivated state of the Na+ channels on the inner aspect of the sodium channel to block sodium current and increase the threshold for excitation.
  • Summary Analgesics Dec2019

    Summary Analgesics Dec2019

    Status as of December 31, 2019 UPDATE STATUS: N = New, A = Advanced, C = Changed, S = Same (No Change), D = Discontinued Update Emerging treatments for acute and chronic pain Development Status, Route, Contact information Status Agent Description / Mechanism of Opioid Function / Target Indication / Other Comments Sponsor / Originator Status Route URL Action (Y/No) 2019 UPDATES / CONTINUING PRODUCTS FROM 2018 Small molecule, inhibition of 1% diacerein TWi Biotechnology / caspase-1, block activation of 1 (AC-203 / caspase-1 inhibitor Inherited Epidermolysis Bullosa Castle Creek Phase 2 No Topical www.twibiotech.com NLRP3 inflamasomes; reduced CCP-020) Pharmaceuticals IL-1beta and IL-18 Small molecule; topical NSAID Frontier 2 AB001 NSAID formulation (nondisclosed active Chronic low back pain Phase 2 No Topical www.frontierbiotech.com/en/products/1.html Biotechnologies ingredient) Small molecule; oral uricosuric / anti-inflammatory agent + febuxostat (xanthine oxidase Gout in patients taking urate- Uricosuric + 3 AC-201 CR inhibitor); inhibition of NLRP3 lowering therapy; Gout; TWi Biotechnology Phase 2 No Oral www.twibiotech.com/rAndD_11 xanthine oxidase inflammasome assembly, reduced Epidermolysis Bullosa Simplex (EBS) production of caspase-1 and cytokine IL-1Beta www.arraybiopharma.com/our-science/our-pipeline AK-1830 Small molecule; tropomyosin Array BioPharma / 4 TrkA Pain, inflammation Phase 1 No Oral www.asahi- A (ARRY-954) receptor kinase A (TrkA) inhibitor Asahi Kasei Pharma kasei.co.jp/asahi/en/news/2016/e160401_2.html www.neurosmedical.com/clinical-research;
  • Proxymetacaine Hydrochloride Ropivacaine Hydrochloride

    Proxymetacaine Hydrochloride Ropivacaine Hydrochloride

    1870 Local Anaesthetics Preparations pore: Alcaine; Switz.: Alcaine; Turk.: Alcaine; Opticaine; USA: Ak-Taine; Alcaine; Ocu-Caine; Ophthetic; Parcaine; Venez.: Alcaine; Oftaine†; Poen- (details are given in Part 3) caina. Proprietary Preparations CH3 Multi-ingredient: Spain: Detraine. O Multi-ingredient: Canad.: Fluoracaine†; USA: Fluoracaine; Fluorocaine. N CH3 O Quinisocaine Hydrochloride (BANM, rINNM) H3C Propipocaine (rINN) O Chinisocainum Hydrochloride; Dimethisoquin Hydrochloride Propipocaína; Propipocaïne; Propipocainum; Propoxypipero- (USAN); Dimethisoquinium Chloride; Hidrocloruro de quinisocaí- NH2 caine. 3-Piperidino-4′-propoxypropiophenone. na; Quinisocaïne, Chlorhydrate de; Quinisocaini Hydrochlori- (proxymetacaine) dum. 2-(3-Butyl-1-isoquinolyloxy)-NN-dimethylethylamine hy- Пропипокаин drochloride. C17H25NO2 = 275.4. Хинизокаина Гидрохлорид CAS — 3670-68-6. NOTE. PROX is a code approved by the BP 2008 for use on single unit doses of eye drops containing proxymetacaine hydrochlo- C17H24N2O,HCl = 308.8. ride where the individual container may be too small to bear all CAS — 86-80-6 (quinisocaine); 2773-92-4 (quinisocaine the appropriate labelling information. PROXFLN is a similar hydrochloride). O code approved for eye drops containing proxymetacaine hydro- ATC — D04AB05. chloride and fluorescein sodium. ATC Vet — QD04AB05. N Pharmacopoeias. In Br. and US. BP 2008 (Proxymetacaine Hydrochloride). A white or almost H3C CH3 white, odourless or almost odourless, crystalline powder. Soluble O in water and in chloroform; very soluble in dehydrated alcohol; N practically insoluble in ether. A 1% solution in water has a pH of O CH Profile 5.7 to 6.4. Protect from light. 3 Propipocaine is a local anaesthetic (p.1850) that has been used USP 31 (Proparacaine Hydrochloride). A white to off-white, or for surface anaesthesia.
  • Pharmacology for Regional Anaesthesia

    Pharmacology for Regional Anaesthesia

    Sign up to receive ATOTW weekly - email [email protected] PHARMACOLOGY FOR REGIONAL ANAESTHESIA ANAESTHESIA TUTORIAL OF THE WEEK 49 26TH MARCH 2007 Dr J. Hyndman Questions 1) List the factors that determine the duration of a local anaesthetic nerve block. 2) How much more potent is bupivocaine when compared to lidocaine? 3) How does the addition of epinephrine increase the duration of a nerve block? 4) What is the maximum recommended dose of: a) Plain lidocaine? b) Lidocaine with epinephrine 1:200 000? 5) What is the recommended dose of a) Clonidine to be added to local anaesthetic solution? b) Sodium bicarbonate? In this section, I will discuss the pharmacology of local anaesthetic agents and then describe the various additives used with these agents. I will also briefly cover the pharmacology of the other drugs commonly used in regional anaesthesia practice. A great number of drugs are used in regional anaesthesia. I am sure no two anaesthetists use exactly the same combinations of drugs. I will emphasise the drugs I use in my own practice but the reader may select a different range of drugs according to his experience and drug availability. The important point is to use the drugs you are familiar with. For the purposes of this discussion, I am going to concentrate on the following drugs: Local anaesthetic agents Lidocaine Prilocaine Bupivacaine Levobupivacaine Ropivacaine Local anaesthetic additives Epinephrine Clonidine Felypressin Sodium bicarbonate Commonly used drugs Midazolam/Temazepam Fentanyl Ephedrine Phenylephrine Atropine Propofol ATOTW 49 Pharmacology for regional anaesthesia 29/03/2007 Page 1 of 6 Sign up to receive ATOTW weekly - email [email protected] Ketamine EMLA cream Ametop gel Naloxone Flumazenil PHARMACOLOGY OF LOCAL ANAESTHETIC DRUGS History In 1860, cocaine was extracted from the leaves of the Erythroxylon coca bush.
  • Pdf; Chi 2015 DPP Air in Cars.Pdf; Dodson 2014 DPP Dust CA.Pdf; Kasper-Sonnenberg 2014 Phth Metabolites.Pdf; EU Cosmetics Regs 2009.Pdf

    Pdf; Chi 2015 DPP Air in Cars.Pdf; Dodson 2014 DPP Dust CA.Pdf; Kasper-Sonnenberg 2014 Phth Metabolites.Pdf; EU Cosmetics Regs 2009.Pdf

    Bouge, Cathy (ECY) From: Nancy Uding <[email protected]> Sent: Friday, January 13, 2017 10:24 AM To: Steward, Kara (ECY) Cc: Erika Schreder Subject: Comments re. 2016 CSPA Rule Update - DPP Attachments: DPP 131-18-0 exposure.pdf; Chi 2015 DPP air in cars.pdf; Dodson 2014 DPP dust CA.pdf; Kasper-Sonnenberg 2014 phth metabolites.pdf; EU Cosmetics Regs 2009.pdf Please accept these comments from Toxic-Free Future concerning the exposure potential of DPP for consideration during the 2016 CSPA Rule update. Regards, Nancy Uding -- Nancy Uding Grants & Research Specialist Toxic-Free Future 206-632-1545 ext.123 http://toxicfreefuture.org 1 JES-00888; No of Pages 9 JOURNAL OF ENVIRONMENTAL SCIENCES XX (2016) XXX– XXX Available online at www.sciencedirect.com ScienceDirect www.elsevier.com/locate/jes Determination of 15 phthalate esters in air by gas-phase and particle-phase simultaneous sampling Chenchen Chi1, Meng Xia1, Chen Zhou1, Xueqing Wang1,2, Mili Weng1,3, Xueyou Shen1,4,⁎ 1. College of Environmental & Resource Sciences, Zhejiang University, Hangzhou 310058, China 2. Zhejiang National Radiation Environmental Technology Co., Ltd., Hangzhou 310011, China 3. School of Environmental and Resource Sciences, Zhejiang Agriculture and Forestry University, Hangzhou 310058, China 4. Zhejiang Provincial Key Laboratory of Organic Pollution Process and Control, Hangzhou 310058, China ARTICLE INFO ABSTRACT Article history: Based on previous research, the sampling and analysis methods for phthalate esters (PAEs) Received 24 December 2015 were improved by increasing the sampling flow of indoor air from 1 to 4 L/min, shortening the Revised 14 January 2016 sampling duration from 8 to 2 hr.
  • Rodgers 693..696

    Rodgers 693..696

    Copyright #ERS Journals Ltd 1999 Eur Respir J 1999; 14: 693±696 European Respiratory Journal Printed in UK ± all rights reserved ISSN 0903-1936 The effect of topical benzamil and amiloride on nasal potential difference in cystic fibrosis H.C. Rodgers, A.J. Knox The effect of topical benzamil and amiloride on nasal potential difference in cystic fibrosis. Respiratory Medicine Unit, City Hospital, H.C. Rodgers, A.J. Knox. #ERS Journals Ltd 1999. Hucknall Road, Nottingham, NG5 IPB. ABSTRACT: The electrochemical defect in the bronchial epithelium in cystic fibrosis (CF) consists of defective chloride secretion and excessive sodium reabsorption. The Correspondence: A.J. Knox Respiratory Medicine Unit sodium channel blocker, amiloride, has been shown to reversibly correct the sodium Clinical Sciences Building reabsorption in CF subjects, but long term studies of amiloride have been disap- City Hospital pointing due to its short duration of action. Benzamil, a benzyl substituted amiloride Hucknall Road analogue, has a longer duration of action than amiloride in cultured human nasal Nottingham NG5 lPB epithelium. The results of the first randomized, placebo controlled, double blind, UK crossover study are reported here comparing the effects of benzamil and amiloride on Fax: 0115 9602140 nasal potential difference (nasal PD) in CF. Ten adults with CF attended on three occasions. At each visit baseline nasal PD was Keywords: Amiloride -3 -3 benzamil recorded, the drug (amiloride 1610 M, benzamil 1.7610 M, or 0.9% sodium cystic fibrosis chloride) was administered topically via a nasal spray, and nasal PD was measured at nasal potential difference 15, 30 min, 1, 2, 4 and 8 h.
  • 4 Supplementary File

    4 Supplementary File

    Supplemental Material for High-throughput screening discovers anti-fibrotic properties of Haloperidol by hindering myofibroblast activation Michael Rehman1, Simone Vodret1, Luca Braga2, Corrado Guarnaccia3, Fulvio Celsi4, Giulia Rossetti5, Valentina Martinelli2, Tiziana Battini1, Carlin Long2, Kristina Vukusic1, Tea Kocijan1, Chiara Collesi2,6, Nadja Ring1, Natasa Skoko3, Mauro Giacca2,6, Giannino Del Sal7,8, Marco Confalonieri6, Marcello Raspa9, Alessandro Marcello10, Michael P. Myers11, Sergio Crovella3, Paolo Carloni5, Serena Zacchigna1,6 1Cardiovascular Biology, 2Molecular Medicine, 3Biotechnology Development, 10Molecular Virology, and 11Protein Networks Laboratories, International Centre for Genetic Engineering and Biotechnology (ICGEB), Padriciano, 34149, Trieste, Italy 4Institute for Maternal and Child Health, IRCCS "Burlo Garofolo", Trieste, Italy 5Computational Biomedicine Section, Institute of Advanced Simulation IAS-5 and Institute of Neuroscience and Medicine INM-9, Forschungszentrum Jülich GmbH, 52425, Jülich, Germany 6Department of Medical, Surgical and Health Sciences, University of Trieste, 34149 Trieste, Italy 7National Laboratory CIB, Area Science Park Padriciano, Trieste, 34149, Italy 8Department of Life Sciences, University of Trieste, Trieste, 34127, Italy 9Consiglio Nazionale delle Ricerche (IBCN), CNR-Campus International Development (EMMA- INFRAFRONTIER-IMPC), Rome, Italy This PDF file includes: Supplementary Methods Supplementary References Supplementary Figures with legends 1 – 18 Supplementary Tables with legends 1 – 5 Supplementary Movie legends 1, 2 Supplementary Methods Cell culture Primary murine fibroblasts were isolated from skin, lung, kidney and hearts of adult CD1, C57BL/6 or aSMA-RFP/COLL-EGFP mice (1) by mechanical and enzymatic tissue digestion. Briefly, tissue was chopped in small chunks that were digested using a mixture of enzymes (Miltenyi Biotec, 130- 098-305) for 1 hour at 37°C with mechanical dissociation followed by filtration through a 70 µm cell strainer and centrifugation.
  • (200731) Hypromellose Phthalate (220824) Ibudilast

    (200731) Hypromellose Phthalate (220824) Ibudilast

    21222122 Infrared Reference Spectra JP XVII Hypromellose Phthalate (200731) Hypromellose Phthalate (220824) Ibudilast The JP Drugs are to be tested according to the provisions given in the pertinent monographs, General Notices, General Rules for Crude Drugs, General Rules for Preparations, and General Tests for their conformity to the Japanese Pharmacopoeia. (See the General Notices 5.) JP XVII Infrared Reference Spectra 21232123 Ibuprofen Ibuprofen Piconol Ifenprodil Tartrate The JP Drugs are to be tested according to the provisions given in the pertinent monographs, General Notices, General Rules for Crude Drugs, General Rules for Preparations, and General Tests for their conformity to the Japanese Pharmacopoeia. (See the General Notices 5.) 21242124 Infrared Reference Spectra JP XVII Imidapril Hydrochloride Imipenem Hydrate Indapamide The JP Drugs are to be tested according to the provisions given in the pertinent monographs, General Notices, General Rules for Crude Drugs, General Rules for Preparations, and General Tests for their conformity to the Japanese Pharmacopoeia. (See the General Notices 5.) JP XVII Infrared Reference Spectra 21252125 Indenolol Hydrochloride Indometacin Iohexol The JP Drugs are to be tested according to the provisions given in the pertinent monographs, General Notices, General Rules for Crude Drugs, General Rules for Preparations, and General Tests for their conformity to the Japanese Pharmacopoeia. (See the General Notices 5.) 21262126 Infrared Reference Spectra JP XVII Iopamidol Iotalamic Acid Iotroxic Acid The JP Drugs are to be tested according to the provisions given in the pertinent monographs, General Notices, General Rules for Crude Drugs, General Rules for Preparations, and General Tests for their conformity to the Japanese Pharmacopoeia.
  • 8–16–01 Vol. 66 No. 159 Thursday Aug. 16, 2001 Pages 42929

    8–16–01 Vol. 66 No. 159 Thursday Aug. 16, 2001 Pages 42929

    8–16–01 Thursday Vol. 66 No. 159 Aug. 16, 2001 Pages 42929–43064 VerDate 11-MAY-2000 19:13 Aug 15, 2001 Jkt 194001 PO 00000 Frm 00001 Fmt 4710 Sfmt 4710 E:\FR\FM\16AUWS.LOC pfrm11 PsN: 16AUWS 1 II Federal Register / Vol. 66, No. 159 / Thursday, August 16, 2001 The FEDERAL REGISTER is published daily, Monday through SUBSCRIPTIONS AND COPIES Friday, except official holidays, by the Office of the Federal Register, National Archives and Records Administration, PUBLIC Washington, DC 20408, under the Federal Register Act (44 U.S.C. Subscriptions: Ch. 15) and the regulations of the Administrative Committee of Paper or fiche 202–512–1800 the Federal Register (1 CFR Ch. I). The Superintendent of Assistance with public subscriptions 512–1806 Documents, U.S. Government Printing Office, Washington, DC 20402 is the exclusive distributor of the official edition. General online information 202–512–1530; 1–888–293–6498 Single copies/back copies: The Federal Register provides a uniform system for making available to the public regulations and legal notices issued by Paper or fiche 512–1800 Federal agencies. These include Presidential proclamations and Assistance with public single copies 512–1803 Executive Orders, Federal agency documents having general FEDERAL AGENCIES applicability and legal effect, documents required to be published Subscriptions: by act of Congress, and other Federal agency documents of public interest. Paper or fiche 523–5243 Assistance with Federal agency subscriptions 523–5243 Documents are on file for public inspection in the Office of the Federal Register the day before they are published, unless the issuing agency requests earlier filing.
  • An Ultra Fast and Sensitive Detection of 165 Drugs of Abuse in Human Urine Using Polarity Switching Ultra Performance Liquid Chromatog- Raphy Tandem Mass Spectrometry

    An Ultra Fast and Sensitive Detection of 165 Drugs of Abuse in Human Urine Using Polarity Switching Ultra Performance Liquid Chromatog- Raphy Tandem Mass Spectrometry

    id15306796 pdfMachine by Broadgun Software - a great PDF writer! - a great PDF creator! - http://www.pdfmachine.com http://www.broadgun.com AAnnaallyyttiiccaaIlSlS N : 0974-7419 Volume 15 Issue 8 CCHHEEAMMn InIdIiSSanTT JoRuRrnYaYl Full Paper ACAIJ, 15(8) 2015 [319-338] An ultra fast and sensitive detection of 165 drugs of abuse in human urine using polarity switching ultra performance liquid chromatog- raphy tandem mass spectrometry Sachin Dubey, Shobha Ahi, Alka Beotra*, Tejinder Kaur, Shila Jain National Dope Testing Laboratory, Ministry of Youth Affairs and Sports, CGO Complex, Lodhi Road, New Delhi, 110003, (INDIA) E-mail : [email protected] ABSTRACT KEYWORDS The screening of wide variety of prohibited substances in a time bound Bioanalytical method; manner by adhering to latest World Anti-Doping Agency (WADA) guide- Sports drug testing; lines is a challenging task for doping control laboratories. The revised crite- UPLC-MS/MS; rion of detection limits (WADATD2013MRPL) has further required the doping Polarity switching; laboratories to review their testing procedures. The present work was aimed WADA. at developing a fast, sensitive and robust analytical method based on solid phase cleanup (SPE) and ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) to achieve the required detection lev- els. The method development involved optimization of deconjugation of phase II metabolites, SPE using mixed-mode ion cartridges for extraction of analytes of wider chemistries; and fast polarity switching UPLC-MS/MS detection. The developed method was validated to detect approximately 165 compounds and/or metabolites prohibited by WADA. The eight min- utes runtime allowed testing of approximately 180 samples in 24 hours at the limit of detection (LOD) of 50% below required detection levels.