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(12) Patent Application Publication (10) Pub. No.: US 2015/0025060A1 Tamarkin Et Al
US 2015.0025060A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0025060A1 Tamarkin et al. (43) Pub. Date: Jan. 22, 2015 (54) FOAMABLE COMPOSITIONS AND KITS (30) Foreign Application Priority Data COMPRISING ONE ORMORE OF A CHANNEL AGENT, ACHOLINERGICAGENT, Oct. 25, 2002 (IL) .......................................... 1524.86 A NITRC OXDE DONOR AND RELATED AGENTS AND THEIR USES Publication Classification (71) Applicant: Foamix Pharmaceuticals Ltd., Rehovot (51) Int. Cl. (IL) A613 L/554 (2006.01) A 6LX3 L/505 (2006.01) (72) Inventors: Dov Tamarkin, Macabim (IL); Meir A647/10 (2006.01) Eini, Ness Ziona (IL); Doron Friedman, A613 L/4422 (2006.01) Karmei Yosef (IL); Tal Berman, Rishon (52) U.S. Cl. Le Ziyyon (IL); Alex Besonov, Rehovot CPC ........... A6 IK3I/554 (2013.01); A61 K3I/4422 (IL) (2013.01); A61 K3I/505 (2013.01); A61 K 47/10 (2013.01) (21) Appl. No.: 14/448,670 USPC ....................... 514/211.03: 514/356; 514/275 (22) Filed: Jul. 31, 2014 (57) ABSTRACT Related U.S. Application Data The present invention relates to a foamable therapeutic com position comprising: (a) a therapeutically effective concen (63) Continuation of application No. 1 1/767,442, filed on tration of at least one active agent selected from the group Jun. 22, 2007, which is a continuation-in-part of appli consisting of a channel agent, a cholinergic agent, and a nitric cation No. 10/911.367, filed on Aug. 4, 2004, said oxide donor; and (b) a foamable carrier comprising: application No. 1 1/767,442 is a continuation-in-part of i. -
Vimpat, INN-Lacosamide
European Medicines Agency Evaluation of Medicines for Human Use Doc.Ref.: EMEA/460925/2008 ASSESSMENT REPORT FOR Vimpat International Nonproprietary Name: lacosamide Procedure No. EMEA/H/C/000863 Assessment Report as adopted by the CHMP with all information of a commercially confidential nature deleted. 7 Westferry Circus, Canary Wharf, London, E14 4HB, UK Tel. (44-20) 74 18 84 00 Fax (44-20) 75 23 70 51 E-mail: [email protected] http://www.emea.europa.eu © European Medicines Agency, 2008. Reproduction is authorised provided the source is acknowledged TABLE OF CONTENTS Page 1. BACKGROUND INFORMATION ON THE PROCEDURE........................................... 3 1.1 Submission of the dossier ........................................................................................................ 3 1.2 Steps taken for the assessment of the product.......................................................................... 3 2 SCIENTIFIC DISCUSSION................................................................................................. 4 2.1 Introduction.............................................................................................................................. 4 2.2 Quality aspects......................................................................................................................... 4 2.3 Non-clinical aspects............................................................................................................... 11 2.4 Clinical aspects ..................................................................................................................... -
Product Update Price List Winter 2014 / Spring 2015 (£)
Product update Price list winter 2014 / Spring 2015 (£) Say to affordable and trusted life science tools! • Agonists & antagonists • Fluorescent tools • Dyes & stains • Activators & inhibitors • Peptides & proteins • Antibodies hellobio•com Contents G protein coupled receptors 3 Glutamate 3 Group I (mGlu1, mGlu5) receptors 3 Group II (mGlu2, mGlu3) receptors 3 Group I & II receptors 3 Group III (mGlu4, mGlu6, mGlu7, mGlu8) receptors 4 mGlu – non-selective 4 GABAB 4 Adrenoceptors 4 Other receptors 5 Ligand Gated ion channels 5 Ionotropic glutamate receptors 5 NMDA 5 AMPA 6 Kainate 7 Glutamate – non-selective 7 GABAA 7 Voltage-gated ion channels 8 Calcium Channels 8 Potassium Channels 9 Sodium Channels 10 TRP 11 Other Ion channels 12 Transporters 12 GABA 12 Glutamate 12 Other 12 Enzymes 13 Kinase 13 Phosphatase 14 Hydrolase 14 Synthase 14 Other 14 Signaling pathways & processes 15 Proteins 15 Dyes & stains 15 G protein coupled receptors Cat no. Product name Overview Purity Pack sizes and prices Glutamate: Group I (mGlu1, mGlu5) receptors Agonists & activators HB0048 (S)-3-Hydroxyphenylglycine mGlu1 agonist >99% 10mg £112 50mg £447 HB0193 CHPG Sodium salt Water soluble, selective mGlu5 agonist >99% 10mg £59 50mg £237 HB0026 (R,S)-3,5-DHPG Selective mGlu1 / mGlu5 agonist >99% 10mg £70 50mg £282 HB0045 (S)-3,5-DHPG Selective group I mGlu receptor agonist >98% 1mg £42 5mg £83 10mg £124 HB0589 S-Sulfo-L-cysteine sodium salt mGlu1α / mGlu5a agonist 10mg £95 50mg £381 Antagonists HB0049 (S)-4-Carboxyphenylglycine Competitive, selective group 1 -
Neuroscience Products
Neuroscience Products CATALOG CATALOG NUMBER U.S. $ NUMBER U.S. $ -A- 3-(N-ACETYLAMINO)-5-(N-DECYL-N- 1 mg 27.50 159549 METHYLAMINO)BENZYL ALCOHOL 5 mg 89.40 o A23187 0-5 C [103955-90-4] (ADMB) See: Antibiotic A23187 A Protein Kinase C activator. Ref.: Proc. Nat. Acad. Sci. USA, 83, 4214 AA-861 20 mg 72.70 (1986). 159061 Purity: 95% 100 mg 326.40 C20H34N2O2 MW 334.5 0oC Orally active, specific and potent inhibitor of 5-lipoxygenase. N-ACETYL-ASP-GLU 25 mg 45.00 153036 [3106-85-2] 100 mg 156.00 Ref.: 1. Yoshimoto, T., et.al., Biochim. o Biophys. Acta, 713, 470 (1982). 2. Ashida, -20-0 C An endogenous neuropeptide with high 250 mg 303.65 Y., et.al., Prostaglandins, 26, 955 (1983). 3. affinity for a brain "Glutamate" receptor. Ancill, R.J., et.al., J. Int. Med. Res., 18, 75 Ref: Zaczek, R., et al., Proc. Natl. Acad. (1990). Sci. (USA), 80, 1116 (1983). C21H26O3 MW 326.4 C11H16N2O8 MW 304.3 ABL PROTEIN TYROSINE KINASE 250 U 47.25 N-ACETYL-2-BENZYLTRYPTAMINE 195876 (v-abl) 1 KU 162.75 See: Luzindole -70oC Recombinant Expressed in E. coli ACETYL-DL-CARNITINE 250 mg 60.00 A truncated form of the v-abl protein 154690 [2504-11-2] 1 g 214.00 tyrosine kinase which contains the 0oC Hydrochloride minimum region needed for kinase activity Crystalline and fibroblast transformation. Suppresses C9H17NO4 • HCl MW 239.7 apoptosis and induces resistance to anti-cancer compounds. O-ACETYL-L-CARNITINE CHLORIDE 500 mg 11.45 Activity: 100 KU/ml 159062 [5080-50-2] 1 g 20.65 Unit Definition: one unit is the amount of 0-5oC (R-(-)-2-Acetyloxy-3-carboxy-N,N,N-trimethyl 5 g 97.45 enzyme which catalyzes the transfer of 1 -1-propanaminium chloride) pmol of phosphate to EAIYAAPFAKKK per Purity: >88% minute at 30°C, pH 7.5. -
Identifying Nootropic Drug Targets Via Large-Scale Cognitive GWAS and Transcriptomics
bioRxiv preprint doi: https://doi.org/10.1101/2020.02.06.934752; this version posted February 6, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY-NC-ND 4.0 International license. Title: Identifying Nootropic Drug Targets via Large-Scale Cognitive GWAS and Transcriptomics Max Lam1, 2, 3,4, Chia-Yen, Chen3,5,6, Xia Yan7,8, W. David Hill9, 10, Joey W. Trampush11, Jin Yu1, Emma Knowles12,13,14, Gail Davies9, 10, Eli Stahl15, 16, Laura Huckins15, 16, David C. Liewald10, Srdjan Djurovic17, 18, Ingrid Melle18, 19, Andrea Christoforou20, Ivar Reinvang21, Pamela DeRosse1, 22, 23, Astri J. Lundervold24, Vidar M. Steen18, 20, Thomas Espeseth19, 21, Katri Räikkönen25, Elisabeth Widen26, Aarno Palotie26, 27, 28, Johan G. Eriksson29, 30, 31, Ina Giegling32, Bettina Konte32, Annette M. Hartmann32, Panos Roussos15, 16, 33, Stella Giakoumaki34, Katherine E. Burdick15, 33, 35, Antony Payton36, William Ollier37, 38, Ornit Chiba- Falek39, Deborah K. Koltai39, 40 , Anna C. Need41, Elizabeth T. Cirulli42, Aristotle N. Voineskos43, Nikos C. Stefanis44, 45, 46, Dimitrios Avramopoulos47, 48, Alex Hatzimanolis44, 45, 46, Nikolaos Smyrnis44, 45, Robert M. Bilder49, Nelson A. Freimer49, Tyrone D. Cannon50, 51, Edythe London49, Russell A. Poldrack52, Fred W. Sabb53, Eliza Congdon49, Emily Drabant Conley54, Matthew A. Scult55, Dwight Dickinson56, Richard E. Straub57, Gary Donohoe58, Derek Morris58, Aiden Corvin59, Michael Gill59, Ahmad R. Hariri55, Daniel R. Weinberger57, Neil Pendleton60, Panos Bitsios61, Dan Rujescu32, Jari Lahti25, 62, Stephanie Le Hellard18, 20, Matthew C. -
Effect of Pentobarbital on Ph and Electrolyte Levels After Induced Seizure in Rats
View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Elsevier - Publisher Connector Seizure (2007) 16, 397—401 www.elsevier.com/locate/yseiz Effect of pentobarbital on pH and electrolyte levels after induced seizure in rats R. Uribe-Escamilla a, D. Mota-Rojas b,P.Sa´nchez-Aparicio b, M. Alonso-Spilsbury b, R. Gonza´lez-Pin˜a c, A. Alfaro-Rodrı´guez a,* a Laboratory of Neurochemistry, National Institute of Rehabilitation, SSA, Me´xico City, Mexico b Department of Animal Production and Agriculture, Universidad Auto´noma Metropolitana-Xochimilco, Me´xico City, Mexico c Laboratory of Neuroplasticity of National Institute of Rehabilitation, SSA, Me´xico City, Mexico Received 29 November 2006; received in revised form 25 January 2007; accepted 20 February 2007 KEYWORDS Summary We studied the effects of high doses of pentobarbital (PB) and carba- Pentobarbital; mazepine (CBZ) on electrolyte levels and pH in an epileptic animal model. Pento- Pentylenetetrazole; barbital decreased Ca2+ and Na+ levels without pentylenetetrazole (PTZ). After this, Carbamazepine; Ca2+ and Na+ levels continued to decrease except when CBZ was used, which Electrolytes preserved the Ca2+ levels PTZ may have opposed effects on PB. Our results suggest that PB causes changes in electrolyte levels and pH, but these changes are diminished by CBZ. # 2007 British Epilepsy Association. Published by Elsevier Ltd. All rights reserved. Introduction The conditions grouped under the term epilepsy constitute an area of continuing medical need. It has One of 11 people has epilepsy problems, experiencing been estimated that about 20% of the patients with at least one seizure at some points. -
(12) United States Patent (10) Patent No.: US 9.482,672 B2 Gong Et Al
USOO9482672B2 (12) United States Patent (10) Patent No.: US 9.482,672 B2 Gong et al. (45) Date of Patent: Nov. 1, 2016 (54) METHODS FOR DIAGNOSING IRRITABLE 2002fO197661 A1 12/2002 Niles et al. BOWEL, SYNDROME 2003,022903.0 A1 12/2003 Theoharides 2008.OO57590 A1 3/2008 Urdea et al. (71) Applicant: NESTEC S.A., Vevey (CH) 2008/0085524 A1 4/2008 Lois (72) Inventors: Hua Gong, San Diego, CA (US); Shui FOREIGN PATENT DOCUMENTS Long Wang, San Diego, CA (US); JP 2000-065820 A 3, 2000 Sharat Singh, Rancho Santa Fe, CA JP 2003-277378. A 10, 2003 (US) JP 2007-506100 A 3, 2007 JP 2007-1864.57 A 7/2007 JP 2008-521817. A 6, 2008 (73) Assignee: Nestec S.A., Vevey (CH) JP 2008-530537 A 8, 2008 JP 2009-52.1690 A 6, 2009 (*) Notice: Subject to any disclaimer, the term of this WO O3.011812 A1 2, 2003 patent is extended or adjusted under 35 WO 2005/O29091 A2 3, 2005 U.S.C. 154(b) by 0 days. WO 2007/076411 A1 7/2005 WO 2006/06877O A1 6, 2006 WO 2006/084.299 A2 8, 2006 (21) Appl. No.: 14/222,531 WO 2008/O14414 A2 1, 2008 WO 2008/022177 A2 2, 2008 (22) Filed: Mar. 21, 2014 WO 2009,045291 A2 4/2009 (65) Prior Publication Data OTHER PUBLICATIONS US 2014/O1997.09 A1 Jul. 17, 2014 Jones et al. The Lancet, vol. 320, Issue 8308, pp. 1115-1172, Nov. 20, 1982, Abstract Only.* Related U.S. Application Data Thevarajah et al. -
Antinociceptive Effect of Gabapentin in Visceral Pain Is Not Mediated by GABAA Or Opioid Receptors
British Journal of Medicine & Medical Research 4(31): 5062-5073, 2014 SCIENCEDOMAIN international www.sciencedomain.org Antinociceptive Effect of Gabapentin in Visceral Pain is not Mediated by GABAA or Opioid Receptors Atefeh Parhizgar1, Manzumeh Shamsi Meymandi1,2*, Gholamreza Sepehri1,2, Ehsan Sepehri1 and Gioia Heravi1,2 1Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran. 2Department of Physiology and Pharmacology, Kerman University of Medical Sciences, Kerman, Iran. Authors’ contributions This work was carried out in collaboration between all authors. Author AP conducted the study and literature searches. Author MSM designed the study, performed the statistical analysis, and wrote the first draft of the manuscript. Author GS wrote the protocol and the final manuscript. Authors ES and GH managed the analyses and experimental part of study. All authors read and approved the final manuscript. Received 14th February 2014 rd Original Research Article Accepted 23 March 2014 Published 10th July 2014 ABSTRACT Aims: There is evidence supporting the antinociceptive effect of gabapentin in visceral pain, however, the underlying mechanism(s) is not determined yet. So this study was performed to evaluate probable involvement of opioid and GABAergic receptors in the gabapentin effects on acetic acid-induced visceral pain in mice. Place and Duration of Study: Kerman Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran, between June 2012 and March 2013. Methodology: The acetic acid test was induced by intraperitoneal injection (i.p.) of acetic acid 0.6% (10ml/kg of body weight) in male mice. Writhing reflex was measured as the number of abdominal contractions in 45min. -
Anti-Angiogenic Activity of Chloride and Potassium Channel Modulators
Kamili et al. Future Journal of Pharmaceutical Sciences (2020) 6:24 Future Journal of https://doi.org/10.1186/s43094-020-00041-1 Pharmaceutical Sciences RESEARCH Open Access Anti-angiogenic activity of chloride and potassium channel modulators: repurposing ion channel modulators Chandana Kamili1* , Hima Sowmya Kandoti1, Sharadha Radhakrishnan1, Abbulu Konde1 and Uma Maheshwara Rao Vattikutti2 Abstract Background: Excessive angiogenesis can be the root cause of many pathological conditions. Various types of ion channels are found on the endothelial cells. These ion channels play a vital role in the multi-stepped process of angiogenesis. The study aims to investigate the anti-angiogenic effects of specific ion channel modulators mefloquine (volume-regulated chloride channel blocker), lubiprostone (ClC-2 channel agonist), and 4-aminopyridine (voltage-gated potassium channel blocker). Results: The anti-angiogenic activity of ion channel modulators was screened by measuring its effects on the area of neovascularization and histopathological studies by in vivo (corneal neovascularization) method and by in vitro assays, endothelial cell proliferation assay, cell migration assay, and matrigel cord-like morphogenesis assay. The test and standard drug (bevacizumab) groups were compared with the control group using one-way ANOVA, followed by post hoc test, and Dunnett’s test to compare the mean of all the groups with the control mean. The results revealed that mefloquine at the dose of 0.6% w/v and 1.0% w/v, lubiprostone at the dose of 0.5% w/v and 1.0% w/ v, and 4-aminopyridine at the dose of 2% w/v and 4% w/v showed significant anti-angiogenic property. -
Aminobutyric Acid Receptors
Commentary Absinthe and ␥-aminobutyric acid receptors Richard W. Olsen* Department of Molecular and Medical Pharmacology, University of California School of Medicine, Los Angeles, CA 90095-1735 bsinthe is an emerald-green liqueur style led to a negative reaction and major Athat achieved fantastic popularity at support for prohibition in France and the close of the 19th century. It was asso- elsewhere. One can see the negative side ciated with the Bohemian lifestyle and was of absinthe drinking in many of the poems credited with the inspiration of famous written about it and the pictures drawn artists and poets (1, 2). Because of its about it, as in Degas (Fig. 1). The ‘‘mad- widespread abuse and the associated tox- ness in a bottle,’’ i.e., absinthe, was doubly icity of its content of oil of wormwood, attacked for its reputation for inducing absinthe was made illegal in most coun- insane and criminal acts, as well as con- tries in the 1910s. The most likely ingre- vulsions and other toxicity (2). However, dient responsible for toxicity is believed to statistics showed that in France in 1907, be the terpenoid ␣-thujone (1–4). Oil of only about 1/40th of the inmates of insane wormwood has convulsant activity as well asylums were absinthe drinkers, and many as activity in killing worms and insects (5). of those would actually drink anything The mechanism of action of thujone has alcoholic (2). remained speculative until now. In a re- Finally, military and civilian leaders cent issue of PNAS, Hold et al. (6) pro- entering into World War I discouraged vided evidence that thujone acts as a alcohol abuse and absinthe in support of ␥ -aminobutyric acid type A (GABAA) the war effort. -
Redalyc.Towards a Translational Model of Panic Attack
Psychology & Neuroscience ISSN: 1984-3054 [email protected] Pontifícia Universidade Católica do Rio de Janeiro Brasil Schenberg, Luiz Carlos Towards a translational model of panic attack Psychology & Neuroscience, vol. 3, núm. 1, enero-junio, 2010, pp. 9-37 Pontifícia Universidade Católica do Rio de Janeiro Rio de Janeiro, Brasil Available in: http://www.redalyc.org/articulo.oa?id=207014856003 How to cite Complete issue Scientific Information System More information about this article Network of Scientific Journals from Latin America, the Caribbean, Spain and Portugal Journal's homepage in redalyc.org Non-profit academic project, developed under the open access initiative PSYCHOLOGY Psychology & Neuroscience, 2010, 3, 1, 9 - 37 NEUROSCIENCE DOI: 10.3922/j.psns.2010.1.003 Towards a translational model of panic attack Luiz Carlos Schenberg Universidade Federal do Espirito Santo, Brazil Abstract About 20 years ago, Deakin and Graeff proposed that whereas generalized anxiety disorder is produced by the overactivity of 5-HT excitatory projections from dorsal raphe nucleus to the areas of prefrontal cortex and amygdala which process distal threat, panic attacks are a dysfunction of 5-HT inhibitory projections from dorsal raphe nucleus to the dorsal periaqueductal gray matter, thereby releasing the responses to proximal threat, innate fear or anoxia. Besides, they suggested that the decrease in 5-HT1A neurotransmission in the hippocampus results in learned helplessness and depression. Accordingly, the Deakin Graeff hypothesis provided a unified frame to the widespread use of 5-HT selective reuptake inhibitors in generalized anxiety, panic disorder and depression. Competitor hypotheses implicate panic attacks with the abnormal functioning of locus coeruleus, basolateral amygdala, dorsomedial hypothalamus or an as-yet-unknown suffocation alarm system. -
Aminobutyric Acid Receptors
Commentary Absinthe and ␥-aminobutyric acid receptors Richard W. Olsen* Department of Molecular and Medical Pharmacology, University of California School of Medicine, Los Angeles, CA 90095-1735 bsinthe is an emerald-green liqueur style led to a negative reaction and major Athat achieved fantastic popularity at support for prohibition in France and the close of the 19th century. It was asso- elsewhere. One can see the negative side ciated with the Bohemian lifestyle and was of absinthe drinking in many of the poems credited with the inspiration of famous written about it and the pictures drawn artists and poets (1, 2). Because of its about it, as in Degas (Fig. 1). The ‘‘mad- widespread abuse and the associated tox- ness in a bottle,’’ i.e., absinthe, was doubly icity of its content of oil of wormwood, attacked for its reputation for inducing absinthe was made illegal in most coun- insane and criminal acts, as well as con- tries in the 1910s. The most likely ingre- vulsions and other toxicity (2). However, dient responsible for toxicity is believed to statistics showed that in France in 1907, be the terpenoid ␣-thujone (1–4). Oil of only about 1/40th of the inmates of insane wormwood has convulsant activity as well asylums were absinthe drinkers, and many as activity in killing worms and insects (5). of those would actually drink anything The mechanism of action of thujone has alcoholic (2). remained speculative until now. In a re- Finally, military and civilian leaders cent issue of PNAS, Hold et al. (6) pro- entering into World War I discouraged vided evidence that thujone acts as a alcohol abuse and absinthe in support of ␥ -aminobutyric acid type A (GABAA) the war effort.