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PRODUCT INFORMATION Piclamilast Item No. 29170 CAS Registry No.: 144035-83-6 Formal Name: 3-(cyclopentyloxy)-N-(3,5-dichloro- 4-pyridinyl)-4-methoxy-benzamide O Synonyms: RP 73401, RPR 73401 Cl H MF: C18H18Cl2N2O3 FW: 381.3 N O Purity: ≥98% O Supplied as: A solid N Storage: -20°C Cl Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Piclamilast is supplied as a solid. A stock solution may be made by dissolving the piclamilast in the solvent of choice, which should be purged with an inert gas. Piclamilast is soluble in organic solvents such as ethanol and DMSO. The solubility of piclamilast in ethanol is approximately 20 mM and approximately 100 mM in DMSO. Description 1 Piclamilast is a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 0.31 nM). It is selective for PDE4 over PDE1, 2,3 PDE2, PDE3, PDE5, and PDE7A in cell-free assays (IC50s = >100, 40, >100, 14, and >10 μM, respectively). Piclamilast inhibits superoxide production by guinea pig eosinophils and histamine-induced contraction 1,4 in isolated guinea pig trachea (IC50s = 24 and 2 nM, respectively). It inhibits eosinophil, neutrophil, lymphocyte, and TNF-α accumulation in bronchoalveolar lavage fluid (BALF) from ovalbumin-sensitized 5 rats (ED50s = 23.8, 14.1, 19.5, and 14.4 μmol/kg, respectively). Piclamilast also inhibits ovalbumin-induced 2 bronchoconstriction in a guinea pig model of asthma (ED50 = 0.033 mg/kg). References 1. Ashton, M.J., Cook, D.C., Fenton, G., et al. Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. -
[3H]-Piclamilast and [3H]-Rolipram
JPET Fast Forward. Published on January 24, 2003 as DOI: 10.1124/jpet.102.047407 JPET FastThis articleForward. has not Published been copyedited on and January formatted. 24,The final2003 version as DOI:10.1124/jpet.102.047407 may differ from this version. Inhibitor Binding to Type 4 Phosphodiesterase (PDE4) Assessed Using [3H]-Piclamilast and [3H]-Rolipram Yu Zhao, Han-Ting Zhang, and James M. O’Donnell Department of Pharmacology University of Tennessee Health Science Center Downloaded from Memphis, Tennessee jpet.aspetjournals.org at ASPET Journals on September 27, 2021 1 Copyright 2003 by the American Society for Pharmacology and Experimental Therapeutics. JPET Fast Forward. Published on January 24, 2003 as DOI: 10.1124/jpet.102.047407 This article has not been copyedited and formatted. The final version may differ from this version. Running title: Inhibitor binding to PDE4 Correspondence should be addressed to: James M. O’Donnell, Ph.D. Department of Pharmacology University of Tennessee Health Science Center 874 Union Avenue Downloaded from Memphis, TN 38163 jpet.aspetjournals.org Phone: 901-448-3621 Fax: 901-448-3849 Email: [email protected] at ASPET Journals on September 27, 2021 Number of text page: 31 Number of tables: 3 Number of figures: 7 Number of references: 50 Number of words: Abstract (241); Introduction (716); Discussion (1544) Abbreviations: EHNA, erythro-9-(2-hydroxy-3-nonyl)adenine; HARBS, high-affinity rolipram binding site; LARBS, low-affinity rolipram binding site; IBMX, 3-isobutyl-1- methylxanthine; PDE, phosphodiesterase Section: Neuropharmacology 2 JPET Fast Forward. Published on January 24, 2003 as DOI: 10.1124/jpet.102.047407 This article has not been copyedited and formatted. -
Chapter Introduction
VU Research Portal Trypanosoma brucei phosphodiesterase B1 as a drug target for Human African Trypanosomiasis Jansen, C.J.W. 2015 document version Publisher's PDF, also known as Version of record Link to publication in VU Research Portal citation for published version (APA) Jansen, C. J. W. (2015). Trypanosoma brucei phosphodiesterase B1 as a drug target for Human African Trypanosomiasis. General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights. • Users may download and print one copy of any publication from the public portal for the purpose of private study or research. • You may not further distribute the material or use it for any profit-making activity or commercial gain • You may freely distribute the URL identifying the publication in the public portal ? Take down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. E-mail address: [email protected] Download date: 05. Oct. 2021 An introduction into phosphodiesterases and their potential role as drug targets for neglected diseases Chapter 1 4 CHAPTER 1 1.1 Human African Trypanosomiasis Human African Trypanomiasis (HAT), also known as African sleeping sickness, is a deadly infectious disease caused by the kinetoplastid Trypanosoma -
Stems for Nonproprietary Drug Names
USAN STEM LIST STEM DEFINITION EXAMPLES -abine (see -arabine, -citabine) -ac anti-inflammatory agents (acetic acid derivatives) bromfenac dexpemedolac -acetam (see -racetam) -adol or analgesics (mixed opiate receptor agonists/ tazadolene -adol- antagonists) spiradolene levonantradol -adox antibacterials (quinoline dioxide derivatives) carbadox -afenone antiarrhythmics (propafenone derivatives) alprafenone diprafenonex -afil PDE5 inhibitors tadalafil -aj- antiarrhythmics (ajmaline derivatives) lorajmine -aldrate antacid aluminum salts magaldrate -algron alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol combined alpha and beta blockers labetalol medroxalol -amidis antimyloidotics tafamidis -amivir (see -vir) -ampa ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) subgroup: -ampanel antagonists becampanel -ampator modulators forampator -anib angiogenesis inhibitors pegaptanib cediranib 1 subgroup: -siranib siRNA bevasiranib -andr- androgens nandrolone -anserin serotonin 5-HT2 receptor antagonists altanserin tropanserin adatanserin -antel anthelmintics (undefined group) carbantel subgroup: -quantel 2-deoxoparaherquamide A derivatives derquantel -antrone antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine antineoplastics (arabinofuranosyl derivatives) fazarabine fludarabine aril-, -aril, -aril- antiviral (arildone derivatives) pleconaril arildone fosarilate -arit antirheumatics (lobenzarit type) lobenzarit clobuzarit -arol anticoagulants (dicumarol type) dicumarol -
Phosphodiesterase (PDE)
Phosphodiesterase (PDE) Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules. www.MedChemExpress.com 1 Phosphodiesterase (PDE) Inhibitors, Activators & Modulators (+)-Medioresinol Di-O-β-D-glucopyranoside (R)-(-)-Rolipram Cat. No.: HY-N8209 ((R)-Rolipram; (-)-Rolipram) Cat. No.: HY-16900A (+)-Medioresinol Di-O-β-D-glucopyranoside is a (R)-(-)-Rolipram is the R-enantiomer of Rolipram. lignan glucoside with strong inhibitory activity Rolipram is a selective inhibitor of of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM phosphodiesterase. and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg (R)-DNMDP (S)-(+)-Rolipram Cat. No.: HY-122751 ((+)-Rolipram; (S)-Rolipram) Cat. No.: HY-B0392 (R)-DNMDP is a potent and selective cancer cell (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, AMP(cAMP)-specific phosphodiesterase (PDE) binds PDE3A directly. -
Inhibition of Phosphodiesterase 4 Modulates Cytokine Induction From
University of Groningen Inhibition of phosphodiesterase 4 modulates cytokine induction from toll like receptor activated, but not rhinovirus infected, primary human airway smooth muscle Van Ly, David; De Pedro, Monique; James, Peter; Morgan, Lucy; Black, Judith L.; Burgess, Janette K.; Oliver, Brian G. G. Published in: Respiratory Research DOI: 10.1186/1465-9921-14-127 IMPORTANT NOTE: You are advised to consult the publisher's version (publisher's PDF) if you wish to cite from it. Please check the document version below. Document Version Publisher's PDF, also known as Version of record Publication date: 2013 Link to publication in University of Groningen/UMCG research database Citation for published version (APA): Van Ly, D., De Pedro, M., James, P., Morgan, L., Black, J. L., Burgess, J. K., & Oliver, B. G. G. (2013). Inhibition of phosphodiesterase 4 modulates cytokine induction from toll like receptor activated, but not rhinovirus infected, primary human airway smooth muscle. Respiratory Research, 14, [127]. https://doi.org/10.1186/1465-9921-14-127 Copyright Other than for strictly personal use, it is not permitted to download or to forward/distribute the text or part of it without the consent of the author(s) and/or copyright holder(s), unless the work is under an open content license (like Creative Commons). The publication may also be distributed here under the terms of Article 25fa of the Dutch Copyright Act, indicated by the “Taverne” license. More information can be found on the University of Groningen website: https://www.rug.nl/library/open-access/self-archiving-pure/taverne- amendment. Take-down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. -
Annual Report 2016
Annexes to the annual report of the European Medicines Agency 2016 Annex 1 – Members of the Management Board ............................................................... 2 Annex 2 - Members of the Committee for Medicinal Products for Human Use ...................... 4 Annex 3 – Members of the Pharmacovigilance Risk Assessment Committee ........................ 6 Annex 4 – Members of the Committee for Medicinal Products for Veterinary Use ................. 8 Annex 5 – Members of the Committee on Orphan Medicinal Products .............................. 10 Annex 6 – Members of the Committee on Herbal Medicinal Products ................................ 12 Annex 7 – Committee for Advanced Therapies .............................................................. 14 Annex 8 – Members of the Paediatric Committee .......................................................... 16 Annex 9 – Working parties and working groups ............................................................ 18 Annex 10 – CHMP opinions: initial evaluations and extensions of therapeutic indication ..... 24 Annex 10a – Guidelines and concept papers adopted by CHMP in 2016 ............................ 25 Annex 11 – CVMP opinions in 2016 on medicinal products for veterinary use .................... 33 Annex 11a – 2016 CVMP opinions on extensions of indication for medicinal products for veterinary use .......................................................................................................... 39 Annex 11b – Guidelines and concept papers adopted by CVMP in 2016 ........................... -
Effect of Ibudilast: a Novel Antiasthmatic Agent, on Airway Hypersensitivity in Bronchial Asthma
Journal of Asthma, 29(4), 245-252 (1992) Effect of Ibudilast: A Novel Antiasthmatic Agent, on Airway Hypersensitivity in Bronchial Asthma Akira Kawasaki, M.D., Kiyoshi Hoshino, M.D., Rokuo Osaki, M.D., Yutaka Mizushima, M.D., and Saburo Yano, M.D. First Department of Internal Medicine Toyania Medical and Pharmaceutical University 2630 Sugitani Toyama, Japan 930-01 ABSTRACT Ibudilast, a unique agent with vasodilating and anti- allergic actions, was studied in 13 asthmatics for its ef- fect on airway hypersensitivity to histamine inhalation. For personal use only. The PC20 values improved significantly from 355.6 to 620.5 &mi at 3 months and further to 731.4 pghl at 6 months following the initial treatment with ibudilast (20 mg twice daily orally). In addition, the severity of the at- tacks decreased significantly. Improvements in the PC2,, and asthmatic symptoms also were observed in the disodium c:hrornoglycate group, but these were equal to or lesser than those in the ibudilast group. No improve- ment was observed in the untreated control group. These J Asthma Downloaded from informahealthcare.com by Yeshiva University on 09/15/14 results suggest that ibudilast would be an effective agent for improving nonspecific airway hypersensitivity in asthmatics. INTRODUCTION and ibudilast have been developed in rapid succession in Japan and used for the treat- After the introduction of disodium cromo- ment of bronchial asthma. Among them, glycate (DSCG) (11, many so-called “anti- ibudilast seems to be especially unique, for allergic agents” such as tranilast (21, ketotifen vasodilating and antiallergic effects (7 3). (3), azelastine (4), amoxanox (51, repirinast (6), Therefore, this agent is used clinically for the 245 Copyright 0 1992 by Marcel Dekker, Inc. -
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. -
Suplementum 12/1 MAKETA 7/1 2/23/12 12:12 PM Stránka 16
suplementum 12/1 _MAKETA 7/1 2/23/12 12:12 PM Stránka 16 16 ACTA MEDICA MARTINIANA 2012 Suppl. 1 DOI: 10.2478/v10201-011-0023-7 SELECTIVE INHIBITION OF PHOSPHODIESTERASE 7 (PDE7) BY BRL50481 IN HEALTHY AND OVALBUMIN-SENSITIZED GUINEA PIGS Christensen I.1, Miskovicova H. 1, Porvaznik I.1,JoskovaM.1, Mokra D.2, Mokry J.1 1Department of Pharmacology Jessenius Faculty of Medicine, Comenius University, Martin 2Department of Physiology, Jessenius Faculty of Medicine, Comenius University, Martin, Slovak Republic A b stract Phosphodiesterase (PDE) inhibitors may have significant clinical benefit in respiratory diseases associated with inflammation. The aim was to evaluate effects of selective PDE7 inhibitor (BRL50481) on citric acid induced cough, in vivo and in vitro airway smooth muscle reactivity in both healthy and ovalbumin sensitized guinea pigs, as well as its effectiveness in changes of blood cells count. Tested drugs were administered intraperitoneally to male guinea pigs once daily for 7 days either vehicle 10% DMSO (dimethyl sulfoxide) 3 ml/kg (as control) or BRL50481 1 mg/kg. Double chamber whole body plethysmo- graph was used for evaluation of citric acid (0.6 M) induced cough and specific airway resistance. Organ bath method was used for measurement of tracheal and lung tissue strips contractions evoked by cumulative doses (10- 8 – 10-3 mol/L) of acetylcholine (ACH) and histamine (HIS). In healthy guinea pigs we did not observe significant effect of tested drug BRL50481 on in vitro contractions (sim- ilarly to in vivo conditions). The effect on cough was in healthy animals negligible. In ovalbumin-sensitized ani- mals, more pronounced in vitro relaxing effect of BRL50481 in HIS induced contractions was observed with simi- lar results in vivo and no significant change in number of cough efforts. -
New Therapeutic Options in the Management of COPD – Focus on Roflumilast
International Journal of COPD Dovepress open access to scientific and medical research Open Access Full Text Article REVIEW New therapeutic options in the management of COPD – focus on roflumilast Sabina Antonela Antoniu Abstract: In chronic obstructive pulmonary disease (COPD) the inflammation occurring in the University of Medicine and Pharmacy, airways and in other lung tissues is complex and is orchestrated by various mediators including the Pulmonary Disease Division, isoenzyme 4 of the phosphodiesterases family (PDE4), which contributes to bronchoconstriction Pulmonary Disease University and inflammation. Various PDE4 inhibitors have been evaluated as potential therapies in asthma Hospital, Iasi, Romania or COPD but among these only roflumilast have been authorized in Europe to be used in patients with severe COPD as an add-on to the bronchodilator therapy. This review discusses the existing preclinical and clinical data supporting the use of roflumilast for this therapeutic indication and tackles some of the pending issues related to PDE4 in general and to roflumilast in particular. Keywords: COPD, roflumilast, PDE4, efficacy, safety Introduction COPD is an inflammatory disease of the airways related mainly to smoking and char- acterized by airflow limitation, which manifests clinically with dsypnea, cough, and sputum production, symptoms that aggravate disease severity and disease exacerbation. Chronic airways inflammation leads to their progressive obstruction, lung paren- chyma damage, and mucus hypersecretion. Subsequently these result in abnormalities in gas exchange at the pulmonary level and respiratory failure. Currently COPD is classified in 4 stages of severity depending on the degree of airways obstruction measured by FEV1 and with FEV1/FVC% ratio (Table 1). In COPD the therapeutic approach is aimed at treating disease exacerbation when this occurs and at slowing disease progression in the stable state. -
Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
US 20190192440A1 (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2019 /0192440 A1 LI (43 ) Pub . Date : Jun . 27 , 2019 ( 54 ) ORAL DRUG DOSAGE FORM COMPRISING Publication Classification DRUG IN THE FORM OF NANOPARTICLES (51 ) Int . CI. A61K 9 / 20 (2006 .01 ) ( 71 ) Applicant: Triastek , Inc. , Nanjing ( CN ) A61K 9 /00 ( 2006 . 01) A61K 31/ 192 ( 2006 .01 ) (72 ) Inventor : Xiaoling LI , Dublin , CA (US ) A61K 9 / 24 ( 2006 .01 ) ( 52 ) U . S . CI. ( 21 ) Appl. No. : 16 /289 ,499 CPC . .. .. A61K 9 /2031 (2013 . 01 ) ; A61K 9 /0065 ( 22 ) Filed : Feb . 28 , 2019 (2013 .01 ) ; A61K 9 / 209 ( 2013 .01 ) ; A61K 9 /2027 ( 2013 .01 ) ; A61K 31/ 192 ( 2013. 01 ) ; Related U . S . Application Data A61K 9 /2072 ( 2013 .01 ) (63 ) Continuation of application No. 16 /028 ,305 , filed on Jul. 5 , 2018 , now Pat . No . 10 , 258 ,575 , which is a (57 ) ABSTRACT continuation of application No . 15 / 173 ,596 , filed on The present disclosure provides a stable solid pharmaceuti Jun . 3 , 2016 . cal dosage form for oral administration . The dosage form (60 ) Provisional application No . 62 /313 ,092 , filed on Mar. includes a substrate that forms at least one compartment and 24 , 2016 , provisional application No . 62 / 296 , 087 , a drug content loaded into the compartment. The dosage filed on Feb . 17 , 2016 , provisional application No . form is so designed that the active pharmaceutical ingredient 62 / 170, 645 , filed on Jun . 3 , 2015 . of the drug content is released in a controlled manner. Patent Application Publication Jun . 27 , 2019 Sheet 1 of 20 US 2019 /0192440 A1 FIG .