Medchemexpress | Medchemexpress
Total Page：16
File Type：pdf, Size：1020Kb
Load more
Recommended publications
-
Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix
United States International Trade Commission Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix USITC Publication 4208 December 2010 U.S. International Trade Commission COMMISSIONERS Deanna Tanner Okun, Chairman Irving A. Williamson, Vice Chairman Charlotte R. Lane Daniel R. Pearson Shara L. Aranoff Dean A. Pinkert Address all communications to Secretary to the Commission United States International Trade Commission Washington, DC 20436 U.S. International Trade Commission Washington, DC 20436 www.usitc.gov Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix Publication 4208 December 2010 (This page is intentionally blank) Pursuant to the letter of request from the United States Trade Representative of December 15, 2010, set forth at the end of this publication, and pursuant to section 1207(a) of the Omnibus Trade and Competitiveness Act, the United States International Trade Commission is publishing the following modifications to the Harmonized Tariff Schedule of the United States (HTS) to implement changes to the Pharmaceutical Appendix, effective on January 1, 2011. Table 1 International Nonproprietary Name (INN) products proposed for addition to the Pharmaceutical Appendix to the Harmonized Tariff Schedule INN CAS Number Abagovomab 792921-10-9 Aclidinium Bromide 320345-99-1 Aderbasib 791828-58-5 Adipiplon 840486-93-3 Adoprazine 222551-17-9 Afimoxifene 68392-35-8 Aflibercept 862111-32-8 Agatolimod -
Human Surrogate Models of Central Sensitization
Human surrogate models of central sensitization: a critical review and practical guide Charles Quesada, Anna Kostenko, Idy Ho, Caterina Leone, Zahra Nochi, Alexandre Stouffs, Matthias Wittayer, Ombretta Caspani, Nanna Brix Finnerup, André Mouraux, et al. To cite this version: Charles Quesada, Anna Kostenko, Idy Ho, Caterina Leone, Zahra Nochi, et al.. Human surrogate models of central sensitization: a critical review and practical guide. European Journal of Pain, Wiley, In press, 10.1002/ejp.1768. hal-03196193 HAL Id: hal-03196193 https://hal.archives-ouvertes.fr/hal-03196193 Submitted on 12 Apr 2021 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. Human surrogate models of central sensitization: a critical review and practical guide Charles Quesada1,2, Anna Kostenko3, Idy Ho4, Caterina Leone5, Zahra Nochi6, Alexandre Stouffs7, Matthias Wittayer3, Ombretta Caspani3, Nanna Brix Finnerup6, André Mouraux7, Gisèle Pickering8, Irene Tracey4, Andrea Truini5, Rolf-Detlef Treede3, Luis Garcia-Larrea1,2* 1) NeuroPain lab, Lyon Centre for Neuroscience (Inserm -
WO 2013/169741 Al 14 November 2013 (14.11.2013) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2013/169741 Al 14 November 2013 (14.11.2013) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 31/401 (2006.01) A61P 9/12 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/405 (2006.01) A61P 25/00 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 31/7048 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, PCT/US20 13/039904 KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, (22) International Filing Date: ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, 7 May 2013 (07.05.2013) NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, (25) Filing Language: English TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, (26) Publication Language: English ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 61/644,134 8 May 2012 (08.05.2012) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (72) Inventors; and UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (71) Applicants : STEIN, Emily A. -
Potential Cannabis Antagonists for Marijuana Intoxication
Central Journal of Pharmacology & Clinical Toxicology Bringing Excellence in Open Access Review Article *Corresponding author Matthew Kagan, M.D., Cedars-Sinai Medical Center, 8730 Alden Drive, Los Angeles, CA 90048, USA, Tel: 310- Potential Cannabis Antagonists 423-3465; Fax: 310.423.8397; Email: Matthew.Kagan@ cshs.org Submitted: 11 October 2018 for Marijuana Intoxication Accepted: 23 October 2018 William W. Ishak, Jonathan Dang, Steven Clevenger, Shaina Published: 25 October 2018 Ganjian, Samantha Cohen, and Matthew Kagan* ISSN: 2333-7079 Cedars-Sinai Medical Center, USA Copyright © 2018 Kagan et al. Abstract OPEN ACCESS Keywords Cannabis use is on the rise leading to the need to address the medical, psychosocial, • Cannabis and economic effects of cannabis intoxication. While effective agents have not yet been • Cannabinoids implemented for the treatment of acute marijuana intoxication, a number of compounds • Antagonist continue to hold promise for treatment of cannabinoid intoxication. Potential therapeutic • Marijuana agents are reviewed with advantages and side effects. Three agents appear to merit • Intoxication further inquiry; most notably Cannabidiol with some evidence of antipsychotic activity • THC and in addition Virodhamine and Tetrahydrocannabivarin with a similar mixed receptor profile. Given the results of this research, continued development of agents acting on cannabinoid receptors with and without peripheral selectivity may lead to an effective treatment for acute cannabinoid intoxication. Much work still remains to develop strategies that will interrupt and reverse the effects of acute marijuana intoxication. ABBREVIATIONS Therapeutic uses of cannabis include chronic pain, loss of appetite, spasticity, and chemotherapy-associated nausea and CBD: Cannabidiol; CBG: Cannabigerol; THCV: vomiting [8]. Recreational cannabis use is on the rise with more Tetrahydrocannabivarin; THC: Tetrahydrocannabinol states approving its use and it is viewed as no different from INTRODUCTION recreational use of alcohol or tobacco [9]. -
Trkb Receptor Signalling: Implications in Neurodegenerative, Psychiatric and Proliferative Disorders
Int. J. Mol. Sci. 2013, 14, 10122-10142; doi:10.3390/ijms140510122 OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 www.mdpi.com/journal/ijms Review TrkB Receptor Signalling: Implications in Neurodegenerative, Psychiatric and Proliferative Disorders Vivek K. Gupta 1,*, Yuyi You 1, Veer Bala Gupta 2, Alexander Klistorner 1,3 and Stuart L. Graham 1,3 1 Australian School of Advanced Medicine, Macquarie University, F10A, 2 Technology Place, North Ryde, Sydney, NSW 2109, Australia; E-Mails: [email protected] (Y.Y.); [email protected] (A.K.); [email protected] (S.L.G.) 2 Centre of Excellence for Alzheimer’s Disease Research & Care, School of Medical Sciences, Edith Cowan University, Joondalup, WA 6027, Australia; E-Mail: [email protected] 3 Save Sight Institute, Sydney University, Sydney, NSW 2000, Australia * Author to whom correspondence should be addressed; E-Mail: [email protected]; Tel.: +61-2-98-123-537; Fax: +61-2-98-123-600. Received: 27 March 2013; in revised form: 27 April 2013 / Accepted: 28 April 2013 / Published: 13 May 2013 Abstract: The Trk family of receptors play a wide variety of roles in physiological and disease processes in both neuronal and non-neuronal tissues. Amongst these the TrkB receptor in particular has attracted major attention due to its critical role in signalling for brain derived neurotrophic factor (BDNF), neurotrophin-3 (NT3) and neurotrophin-4 (NT4). TrkB signalling is indispensable for the survival, development and synaptic plasticity of several subtypes of neurons in the nervous system. Substantial evidence has emerged over the last decade about the involvement of aberrant TrkB signalling and its compromise in various neuropsychiatric and degenerative conditions. -
Novel Approaches in Clinical Development of Cannabinoid Drugs
Novel approaches in clinical development of cannabinoid drugs Linda Klumpers novel approaches in clinical development of cannabinoid drugs Novel approaches in clinical development of cannabinoid drugs proefschrift ter verkrijging van de graad van Doctor aan de Universiteit Leiden, op gezag van de Rector Magnificus prof. mr. C.J.J.M. Stolker, volgens besluit van het College voor Promoties, te verdedigen op dinsdag 21 januari 2014, klokke 16:15 uur door Linda Elvira Klumpers, geboren te Rotterdam in 1980 Promotiecommissie chapter i 7 Introduction to the endocannabinoid system as a target for drug development promotores Prof. dr. J.M.A. van Gerven chapter ii 49 Professor of Clinical Neuropsychopharmacology, Leiden University Medical Center Novel ∆9-tetrahydrocannabinol formulation Namisol® has bene- and Centre for Human Drug Research ficial pharmacokinetics and promising pharmacodynamic effects Prof. dr. A.F. Cohen Professor of Clinical Pharmacology, Leiden University Medical Center and Centre chapter iii 79 for Human Drug Research Manipulating brain connectivity with ∆9-tetrahydrocannabinol: a pharmacological resting state fmri study overige leden chapter iv 115 Prof. dr. P.H. van der Graaf Surinabant, a selective cb¡ antagonist, inhibits thc-induced Professor of Bio-pharmaceutical Sciences, Leiden University central nervous system and heart rate effects in humans Dr. J.T. Tamsma Internist and Medical Director of the Leiden University Medical Center chapter v 145 Prof. dr. R.F. Witkamp Peripheral selectivity of the novel cannabinoid receptor -
Cannabinoid Receptor Cannabinoid Receptor
Cannabinoid Receptor Cannabinoid Receptor Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol. www.MedChemExpress.com 1 Cannabinoid Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators (S)-MRI-1867 (±)-Ibipinabant Cat. No.: HY-141411A ((±)-SLV319; (±)-BMS-646256) Cat. No.: HY-14791A (S)-MRI-1867 is a peripherally restricted, orally (±)-Ibipinabant ((±)-SLV319) is the racemate of bioavailable dual cannabinoid CB1 receptor and SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent inducible NOS (iNOS) antagonist. (S)-MRI-1867 and selective cannabinoid-1 (CB-1) receptor ameliorates obesity-induced chronic kidney disease antagonist with an IC50 of 22 nM. (CKD). Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg 2-Arachidonoylglycerol 2-Palmitoylglycerol Cat. No.: HY-W011051 (2-Palm-Gl) Cat. No.: HY-W013788 2-Arachidonoylglycerol is a second endogenous 2-Palmitoylglycerol (2-Palm-Gl), an congener of cannabinoid ligand in the central nervous system. 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119. -
284588417-Oa
fphar-09-01143 October 8, 2018 Time: 15:40 # 1 ORIGINAL RESEARCH published: 10 October 2018 doi: 10.3389/fphar.2018.01143 Burst-Like Subcutaneous Electrical Stimulation Induces BDNF-Mediated, Cyclotraxin B-Sensitive Central Sensitization in Rat Spinal Cord Jeffri Retamal1,2, Andrea Reyes1, Paulina Ramirez1,2, David Bravo1,2, Alejandro Hernandez1, Teresa Pelissier3, Luis Villanueva4 and Luis Constandil1,2* 1 Laboratory of Neurobiology, Department of Biology, Faculty of Chemistry and Biology, University of Santiago de Chile, Santiago, Chile, 2 Center for the Development of Nanoscience and Nanotechnology (CEDENNA), Santiago, Chile, 3 Program of Molecular and Clinical Pharmacology, Institute of Biomedical Sciences, Faculty of Medicine, University of Chile, Santiago, Chile, 4 Centre de Psychiatrie et Neurosciences, INSERM UMR 894, Paris, France Intrathecal administration of brain derived neurotrophic factor (BDNF) induces long- term potentiation (LTP) and generates long-lasting central sensitization in spinal cord thus mimicking chronic pain, but the relevance of these observations to chronic pain mechanisms is uncertain. Since C-fiber activation by a high-frequency subcutaneous electrical stimulation (SES) protocol causes spinal release of BDNF and induces spinal Edited by: cord LTP, we propose that application of such protocol would be a sufficient condition Ramón Sotomayor-Zárate, Universidad de Valparaíso, Chile for generating long-lasting BDNF-mediated central sensitization. Results showed that Reviewed by: application of burst-like SES to rat toes produced (i) rapid induction of hyperalgesia James W. Grau, that lasted for more than 3 weeks, (ii) early increase of C-reflex activity followed by Texas A&M University, United States Claudio Coddou, increased wind-up scores lasting for more than 1 week, and (iii) early increase followed Universidad Católica del Norte, Chile by late decrease in BDNF protein levels and phosphorylated TrkB that lasted for more *Correspondence: than 1 week. -
Mood Disorders in Huntington's Disease
REVIEW ARTICLE published: 23 April 2014 BEHAVIORAL NEUROSCIENCE doi: 10.3389/fnbeh.2014.00135 Mood disorders in Huntington’s disease: from behavior to cellular and molecular mechanisms Patrick Pla 1,2,3,4, Sophie Orvoen 5, Frédéric Saudou 1,2,3, Denis J. David 5 and Sandrine Humbert 1,2,3* 1 Institut Curie, Orsay, France 2 CNRS UMR3306, Orsay, France 3 INSERM U1005, Orsay, France 4 Faculté des Sciences, Université Paris-Sud, Orsay, France 5 EA3544, Faculté de Pharmacie, Université Paris-Sud, Châtenay-Malabry, France Edited by: Huntington’s disease (HD) is a neurodegenerative disorder that is best known for its Benjamin Adam Samuels, Columbia effect on motor control. Mood disturbances such as depression, anxiety, and irritability University, USA also have a high prevalence in patients with HD, and often start before the onset Reviewed by: of motor symptoms. Various rodent models of HD recapitulate the anxiety/depressive Catherine Belzung, Université Francois Rabelais, France behavior seen in patients. HD is caused by an expanded polyglutamine stretch in Emmanuel Brouillet, Commissariat à the N-terminal part of a 350 kDa protein called huntingtin (HTT). HTT is ubiquitously l’Energie Atomique and Centre expressed and is implicated in several cellular functions including control of transcription, National de la Recherche vesicular trafficking, ciliogenesis, and mitosis. This review summarizes progress in Scientifique, France efforts to understand the cellular and molecular mechanisms underlying behavioral *Correspondence: Sandrine Humbert, Institut Curie, disorders in patients with HD. Dysfunctional HTT affects cellular pathways that are Bâtiment 110, 91405 Orsay Cedex, involved in mood disorders or in the response to antidepressants, including BDNF/TrkB France and serotonergic signaling. -
Phd Thesis Distinto.Pdf
Università degli Studi di Cagliari Corso di Dottorato di Ricerca in Scienze e tecnologie Farmaceutiche Ciclo XXVII Progettazione e sintesi di nuovi antagonisti CB1 a struttura pirazolica come potenziali radiofarmaci per la PET imaging CHIM08 Presentata da: Dott.ssa Rita Distinto Coordinatore Dottorato: Prof. Elias Maccioni Tutor/Relatore Prof. Elias Maccioni Dott. Paolo Lazzari Esame finale anno accademico 2013 – 2014 A mia madre 2 Abstract Cannabinoid receptors are members of the large family of G-protein coupled receptors. Two types of cannabinoid receptor have been discovered: CB1 and CB2. CB1 receptors are localised predominantly in the brain whereas CB2 receptors are more abundant in peripheral nervous system cells. CB1 receptors have been related with a number of disorders, including depression, anxiety, stress, schizophrenia, chronic pain and obesity. For this reason, several cannabinoid ligands were developed as drug candidates. Among these ligands, a prominent position is occupied by SR141716 (Rimonabant), which is a pyrazole derivative with inverse agonist activity discovered by Sanofi-Synthelabo in 1994. This compound was marketed in Europe as an anti-obesity drug, but subsequently withdrawn due to its side-effects. Since the relationship between the CB1 receptors’ functional modification, density and distribution, and the beginning of a pathological state is still not well understood, the development of radio-ligands suitable for in vivo PET (Positron Emission Tomography) functional imaging of CB1 receptors remains an important area of research in medicine and drug development. To date, a few radiotracers have been synthesised and tested in vivo, but most of them afforded unsatisfactory brain imaging results. A handful of radiolabelled CB1 PET ligands have also been submitted to clinical trials in humans. -
(12) United States Patent (10) Patent No.: US 8,853,205 B2 Makriyannis Et Al
US008853205 B2 (12) United States Patent (10) Patent No.: US 8,853,205 B2 Makriyannis et al. (45) Date of Patent: *Oct. 7, 2014 (54) HETEROPYRROLE ANALOGSACTING ON 5,462,960 A * 10/1995 Barth et al. ................... 514,406 CANNABINOID RECEPTORS 6.432,984 B1 8, 2002 Barth et al. 6,509,367 B1 1/2003 Martin et al. 7,119, 108 B1 10/2006 Makriyannis et al. (75) Inventors: Alexandros Makriyannis, Watertown, 7,393,842 B2 7/2008 Makriyannis et al. MA (US); Venkata Kiran Vemuri, 7,745.440 B2 6/2010 Makriyannis et al. Boston, MA (US) 7,872,006 B2 1/2011 Moritani et al. 8,084,451 B2 * 12/2011 Makriyannis et al. ........ 514,241 (73) Assignee: University of Connecticut, Farmington, 2004/0192667 A1 9/2004 Makriyannis et al. CT (US) 2004/0248956 Al 12/2004 Hagmann et al. (*) Notice: Subject to any disclaimer, the term of this FOREIGN PATENT DOCUMENTS past is tituted under 35 EP O576,357 A1 12/1993 .S.C. 154(b) by ayS. EP O656354 A1 6, 1995 This patent is Subject to a terminal disis- FREP 2758.723O658546 A1 6,T 19951998 Ca10. FR 2856683 A1 12/2004 WO 9719063 A1 5, 1997 (21) Appl. No.: 13/202,499 WO 972.1682 A1 6, 1997 WO 2005OOO820 1, 2005 (22) PCT Filed: Feb. 19, 2009 WO 2006067443 6, 2006 WO 2006O74445 A2 T 2006 (86). PCT No.: PCT/US2O09/OO 1054 WO 2007061948 A2 5, 2007 S371 (c)(1), OTHER PUBLICATIONS (2), (4) Date: Nov. 11, 2011 Fan, H. et al., “Analogs of JHU75528, a PET ligand for imaging of (87) PCT Pub. -
Novel Approaches in Clinical Development of Cannabinoid Drugs
Novel approaches in clinical development of cannabinoid drugs Linda Klumpers novel approaches in clinical development of cannabinoid drugs Novel approaches in clinical development of cannabinoid drugs proefschrift ter verkrijging van de graad van Doctor aan de Universiteit Leiden, op gezag van de Rector Magnificus prof. mr. C.J.J.M. Stolker, volgens besluit van het College voor Promoties, te verdedigen op dinsdag 21 januari 2014, klokke 16:15 uur door Linda Elvira Klumpers, geboren te Rotterdam in 1980 Promotiecommissie chapter i 7 Introduction to the endocannabinoid system as a target for drug development promotores Prof. dr. J.M.A. van Gerven chapter ii 49 Professor of Clinical Neuropsychopharmacology, Leiden University Medical Center Novel ∆9-tetrahydrocannabinol formulation Namisol® has bene- and Centre for Human Drug Research ficial pharmacokinetics and promising pharmacodynamic effects Prof. dr. A.F. Cohen Professor of Clinical Pharmacology, Leiden University Medical Center and Centre chapter iii 79 for Human Drug Research Manipulating brain connectivity with ∆9-tetrahydrocannabinol: a pharmacological resting state fmri study overige leden chapter iv 115 Prof. dr. P.H. van der Graaf Surinabant, a selective cb¡ antagonist, inhibits thc-induced Professor of Bio-pharmaceutical Sciences, Leiden University central nervous system and heart rate effects in humans Dr. J.T. Tamsma Internist and Medical Director of the Leiden University Medical Center chapter v 145 Prof. dr. R.F. Witkamp Peripheral selectivity of the novel cannabinoid receptor