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PRODUCT INFORMATION α-Bungarotoxin (trifluoroacetate salt) Item No. 16385 Synonyms: α-Bgt, α-BTX Peptide Sequence: IVCHTTATSPISAVTCPPGENLCY Ile Val Cys His Thr Thr Ala Thr Ser Pro RKMWCDAFCSSRGKVVELGCAA Ile Ser Ala Val Thr Cys Pro Pro Gly Glu TCPSKKPYEEVTCCSTDKCNPHP KQRPG, trifluoroacetate salt Asn Leu Cys Tyr Arg Lys Met Trp Cys Asp (Modifications: Disulfide bridge between Ala Phe Cys Ser Ser Arg Gly Lys Val Val 3-23, 16-44, 29-33, 48-59, 60-65) Glu Leu Gly Cys Ala Ala Thr Cys Pro Ser MF: C338H529N97O105S11 • XCF3COOH FW: 7,984.2 Lys Lys Pro Tyr Glu Glu Val Thr Cys Cys Supplied as: A solid Ser Thr Asp Lys Cys Asn Pro His Pro Lys Storage: -20°C Gln Arg Pro Gly Stability: ≥2 years • XCF COOH Solubility: Soluble in aqueous buffers 3 Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures α-Bungarotoxin (trifluoroacetate salt) is supplied as a solid. A stock solution may be made by dissolving the α-bungarotoxin (trifluoroacetate salt) in water. The solubility of α-bungarotoxin (trifluoroacetate salt) in water is approximately 1 mg/ml. We do not recommend storing the aqueous solution for more than one day. Description α-Bungarotoxin is a snake venom-derived toxin that irreversibly binds nicotinic acetylcholine receptors (Ki = ~2.5 µM in rat) present in skeletal muscle, blocking action of acetylcholine at the postsynaptic membrane and leading to paralysis.1-3 It has been widely used to characterize activity at the neuromuscular junction, which has numerous applications in neuroscience research.4,5 References 1. -
British Chemical Abstracts
BRITISH CHEMICAL ABSTRACTS _ ' A.-PURE CHEMISTRY | DECEMBER, 1935. General, Physical, and Inorganic Chemistry. Slight correction to the Rydberg constant for 1000 A. have been photographed and arranged into hydrogen (H1). R. C. Williams and R. C. Gibbs three progressions for wliich formuła; are given. (Physical Rev., 1934, [ii], 45, 491). L. S. T. They are due to normal O. Otlier bands at shorter T riplet 3p complex of the hydrogen molecule. XX and between 1210 and 1000 A. liave also been G. H. D ieke (Physical Rev., 1935, [ii], 48, CIO—614; measured. L. S. T. cf. this vol., 917).—M any peculiarities in the Fulcher Oxygen in the sun’s chromosphere. T. R oyds bands of H2 can be explained by the interaction of (Naturę, 1935, 136, 606—607).—The observed infra- the ?yjM\ with tlie 3f>?£ level (cf. following abstract). red O emission lines 7771, 7774, and 7775 show th at N.' M. B. 02 is a normal and probably abundant constituent of 3p3I, -> 2s3L bands of HD and D2. G. H. the sun’s chromosphere. L. S. T. D ieke (Physical Rev., 1935, [ii], 48, 606—609; cf. New emission spectrum of sulphur in the this yoL, 555).—Fuli data for the system in the photographic infra-red. M. D k sib an t and J. extreme red and near infra-red are tabulated, and D uchesne (Compt. rend., 1935, 201, 597—598).— the band consts. are calc. N. M. B. Bands at 6650—7765 A., degraded to the violet, and Vibration and rotation spectrum of the mole attributed to S2, are described. -
(12) Patent Application Publication (10) Pub. No.: US 2003/0105159 A1 Mccleary Et Al
US 200301 05159A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0105159 A1 McCleary et al. (43) Pub. Date: Jun. 5, 2003 (54) KAVALACTONE COMPOSITIONS AND Publication Classification METHODS OF USE (51) Int. Cl." ....................... A61K 31/35; A61K 31/366; (76) Inventors: Joel McCleary, The Plains, VA (US); A61K 35/78; A61K 31/16 Peter S. Staats, Towson, MD (US) (52) U.S. Cl. ........................... 514/460; 514/625; 424/760 Correspondence Address: FISH & RICHARDSON PC 225 FRANKLIN ST BOSTON, MA 02110 (US) (57) ABSTRACT (21) Appl. No.: 10/214,624 (22) Filed: Aug. 8, 2002 This invention relates tO kavalactone-containing composi tions, and more particularly to compositions having com Related U.S. Application Data pounds derived from kavalactones and from capsaicinoids. The compositions are useful in modulating pain, and thus (60) Provisional application No. 60/311,437, filed on Aug. can be used to mediate, or eliminate, Sensations of pain, 10, 2001. thereby providing pain relief and reduction. US 2003/0105159 A1 Jun. 5, 2003 KAVALACTONE COMPOSITIONS AND METHODS 0006. In one embodiment, the invention relates to an OF USE analgesic topical composition having: (a) a kavalactone; (b) capsaicinoid or Synthetic derivatives thereof; and (c) a CROSS-REFERENCE TO RELATED pharmaceutically acceptable carrier; wherein the weight APPLICATIONS ratio of(a):(b) is from 5000:1 to 1:2 (e.g., 800:1 to 1:1; 500:1 to 5:1). In other aspects, the composition includes an effec 0001. This application claims benefit of U.S. application tive amount of kavalactones, active kavalactones, or capsai Ser. -
(12) Patent Application Publication (10) Pub. No.: US 2016/017.4603 A1 Abayarathna Et Al
US 2016O174603A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2016/017.4603 A1 Abayarathna et al. (43) Pub. Date: Jun. 23, 2016 (54) ELECTRONIC VAPORLIQUID (52) U.S. Cl. COMPOSITION AND METHOD OF USE CPC ................. A24B 15/16 (2013.01); A24B 15/18 (2013.01); A24F 47/002 (2013.01) (71) Applicants: Sahan Abayarathna, Missouri City, TX 57 ABSTRACT (US); Michael Jaehne, Missouri CIty, An(57) e-liquid for use in electronic cigarettes which utilizes- a TX (US) vaporizing base (either propylene glycol, vegetable glycerin, (72) Inventors: Sahan Abayarathna, MissOU1 City,- 0 TX generallyor mixture at of a 0.001 the two) g-2.0 mixed g per with 1 mL an ratio. herbal The powder herbal extract TX(US); (US) Michael Jaehne, Missouri CIty, can be any of the following:- - - Kanna (Sceletium tortuosum), Blue lotus (Nymphaea caerulea), Salvia (Salvia divinorum), Salvia eivinorm, Kratom (Mitragyna speciosa), Celandine (21) Appl. No.: 14/581,179 poppy (Stylophorum diphyllum), Mugwort (Artemisia), Coltsfoot leaf (Tussilago farfara), California poppy (Eschscholzia Californica), Sinicuichi (Heimia Salicifolia), (22) Filed: Dec. 23, 2014 St. John's Wort (Hypericum perforatum), Yerba lenna yesca A rtemisia scoparia), CaleaCal Zacatechichihichi (Calea(Cal termifolia), Leonurus Sibericus (Leonurus Sibiricus), Wild dagga (Leono Publication Classification tis leonurus), Klip dagga (Leonotis nepetifolia), Damiana (Turnera diffiisa), Kava (Piper methysticum), Scotch broom (51) Int. Cl. tops (Cytisus scoparius), Valarien (Valeriana officinalis), A24B 15/16 (2006.01) Indian warrior (Pedicularis densiflora), Wild lettuce (Lactuca A24F 47/00 (2006.01) virosa), Skullcap (Scutellaria lateriflora), Red Clover (Trifo A24B I5/8 (2006.01) lium pretense), and/or combinations therein. -
Studies on the Pharmacology of Conopharyngine, an Indole Alkaloid of the Voacanga Series
Br. J. Pharmac. Chemother. (1967), 30, 173-185. STUDIES ON THE PHARMACOLOGY OF CONOPHARYNGINE, AN INDOLE ALKALOID OF THE VOACANGA SERIES BY P. R. CARROLL AND G. A. STARMER From the Department of Pharmacology, University of Sydney, New South Wales, Australia (Received January 17, 1967) Conopharyngine, the major alkaloid present in the leaves of Tabernaemontana (Conopharyngia) pachysiphon var. cumminsi (Stapf) H. Huber was isolated and identified by Thomas & Starmer (1963). The same alkaloid has also been found in the stem bark of a Nigerian variety of the same species by Patel & Poisson (1966) and in the stem bark of Conopharyngia durissima by Renner, Prins & Stoll (1959). Conopharyn- gine is an indole alkaloid of the voacanga type, being 18-carbomethoxy-12,13- dimethoxyibogamine (Fig. 1) and is thus closely related to voacangine and coronaridine. Me.0OC Fig. 1. Conopharyngine (18-carbomethoxy-12,13-dimethoxyibogamine). Some confusion exists in that an alkaloid with an entirely different structure, but also named conopharyngine, was isolated from a cultivated variety of Conopharyngia pachysiphon by Dickel, Lucas & Macphillamy (1959). This compound was shown to be the 3-D-9-glucoside of 55-20a-amino-3 8-hydroxypregnene, and was reported to possess marked hypotensive properties. The presence of steroid alkaloids in the Tabernaemontaneae was hitherto unknown and it was suggested by Raffauf & Flagler (1960) and Bisset (1961) that the plant material was open to further botanical confir- mation. The roots of the conopharyngia species are used in West Africa to treat fever (Kennedy, 1936), including that of malaria (Watt & Breyer-Brandwijk, 1962). The only report on the pharmacology of conopharyngine is that of Zetler (1964), who included it in a study of some of the effects of 23 natural and semi-synthetic alkaloids 174 P. -
Potentially Harmful Drugs in the Elderly: Beers List
−This Clinical Resource gives subscribers additional insight related to the Recommendations published in− March 2019 ~ Resource #350301 Potentially Harmful Drugs in the Elderly: Beers List In 1991, Dr. Mark Beers and colleagues published a methods paper describing the development of a consensus list of medicines considered to be inappropriate for long-term care facility residents.12 The “Beers list” is now in its sixth permutation.1 It is intended for use by clinicians in outpatient as well as inpatient settings (but not hospice or palliative care) to improve the care of patients 65 years of age and older.1 It includes medications that should generally be avoided in all elderly, used with caution, or used with caution or avoided in certain elderly.1 There is also a list of potentially harmful drug-drug interactions in seniors, as well as a list of medications that may need to be avoided or have their dosage reduced based on renal function.1 This information is not comprehensive; medications and interactions were chosen for inclusion based on potential harm in relation to benefit in the elderly, and availability of alternatives with a more favorable risk/benefit ratio.1 The criteria no longer address drugs to avoid in patients with seizures or insomnia because these concerns are not unique to the elderly.1 Another notable deletion is H2 blockers as a concern in dementia; evidence of cognitive impairment is weak, and long-term PPIs pose risks.1 Glimepiride has been added as a drug to avoid. Some drugs have been added with cautions (dextromethorphan/quinidine, trimethoprim/sulfamethoxazole), and some have had cautions added (rivaroxaban, tramadol, SNRIs). -
Herbal Medicines in Pregnancy and Lactation : an Evidence-Based
00 Prelims 1410 10/25/05 2:13 PM Page i Herbal Medicines in Pregnancy and Lactation An Evidence-Based Approach Edward Mills DPh MSc (Oxon) Director, Division of Clinical Epidemiology Canadian College of Naturopathic Medicine North York, Ontario, Canada Jean-Jacques Duguoa MSc (cand.) ND Naturopathic Doctor Toronto Western Hospital Assistant Professor Division of Clinical Epidemiology Canadian College of Naturopathic Medicine North York, Ontario, Canada Dan Perri BScPharm MD MSc Clinical Pharmacology Fellow University of Toronto Toronto, Ontario, Canada Gideon Koren MD FACMT FRCP Director of Motherisk Professor of Medicine, Pediatrics and Pharmacology University of Toronto Toronto, Ontario, Canada With a contribution from Paul Richard Saunders PhD ND DHANP 00 Prelims 1410 10/25/05 2:13 PM Page ii © 2006 Taylor & Francis Medical, an imprint of the Taylor & Francis Group First published in the United Kingdom in 2006 by Taylor & Francis Medical, an imprint of the Taylor & Francis Group, 2 Park Square, Milton Park, Abingdon, Oxon OX14 4RN Tel.: ϩ44 (0)20 7017 6000 Fax.: ϩ44 (0)20 7017 6699 E-mail: [email protected] Website: www.tandf.co.uk/medicine All rights reserved. No part of this publication may be reproduced, stored in a retrieval system, or trans- mitted, in any form or by any means, electronic, mechanical, photocopying, recording, or otherwise, without the prior permission of the publisher or in accordance with the provisions of the Copyright, Designs and Patents Act 1988 or under the terms of any licence permitting limited copying issued by the Copyright Licensing Agency, 90 Tottenham Court Road, London W1P 0LP. -
The Endocannabinoid 2-Arachidonoylglycerol Negatively Regulates Habituation by Suppressing Excitatory Recurrent Network Activity
3588 • The Journal of Neuroscience, February 20, 2013 • 33(8):3588–3601 Cellular/Molecular The Endocannabinoid 2-Arachidonoylglycerol Negatively Regulates Habituation by Suppressing Excitatory Recurrent Network Activity and Reducing Long-Term Potentiation in the Dentate Gyrus Yuki Sugaya,1 Barbara Cagniard,1 Maya Yamazaki,2 Kenji Sakimura,2 and Masanobu Kano1 1Department of Neurophysiology, Graduate School of Medicine, The University of Tokyo, Tokyo 113-0033, Japan and 2Department of Cellular Neurobiology, Brain Research Institute, Niigata University, Niigata 951-8585, Japan Endocannabinoids are known to mediate retrograde suppression of synaptic transmission, modulate synaptic plasticity, and influence learning and memory. The 2-arachidonoylglycerol (2-AG) produced by diacylglycerol lipase ␣ (DGL␣) is regarded as the major endo- cannabinoid that causes retrograde synaptic suppression. To determine how 2-AG signaling influences learning and memory, we sub- jected DGL␣ knock-out mice to two learning tasks. We tested the mice using habituation and odor-guided transverse patterning tasks that are known to involve the dentate gyrus and the CA1, respectively, of the hippocampus. We found that DGL␣ knock-out mice showed significantly faster habituation to an odor and a new environment than wild-type littermates with normal performance in the transverse patterning task. In freely moving animals, long-term potentiation (LTP) induced by theta burst stimulation was significantly larger at perforantpath–granulecellsynapsesinthedentategyrusofDGL␣knock-outmice.Importantly,priorinductionofsynapticpotentiation -
The Iboga Alkaloids
The Iboga Alkaloids Catherine Lavaud and Georges Massiot Contents 1 Introduction ................................................................................. 90 2 Biosynthesis ................................................................................. 92 3 Structural Elucidation and Reactivity ...................................................... 93 4 New Molecules .............................................................................. 97 4.1 Monomers ............................................................................. 99 4.1.1 Ibogamine and Coronaridine Derivatives .................................... 99 4.1.2 3-Alkyl- or 3-Oxo-ibogamine/-coronaridine Derivatives . 102 4.1.3 5- and/or 6-Oxo-ibogamine/-coronaridine Derivatives ...................... 104 4.1.4 Rearranged Ibogamine/Coronaridine Alkaloids .. ........................... 105 4.1.5 Catharanthine and Pseudoeburnamonine Derivatives .. .. .. ... .. ... .. .. ... .. 106 4.1.6 Miscellaneous Representatives and Another Enigma . ..................... 107 4.2 Dimers ................................................................................. 108 4.2.1 Bisindoles with an Ibogamine Moiety ....................................... 110 4.2.2 Bisindoles with a Voacangine (10-Methoxy-coronaridine) Moiety ........ 111 4.2.3 Bisindoles with an Isovoacangine (11-Methoxy-coronaridine) Moiety . 111 4.2.4 Bisindoles with an Iboga-Indolenine or Rearranged Moiety ................ 116 4.2.5 Bisindoles with a Chippiine Moiety ... ..................................... -
S42003-021-02488-1.Pdf
ARTICLE https://doi.org/10.1038/s42003-021-02488-1 OPEN In situ imaging reveals disparity between prostaglandin localization and abundance of prostaglandin synthases ✉ Kyle D. Duncan 1,5, Xiaofei Sun 2,3,5, Erin S. Baker 4, Sudhansu K. Dey 2,3 & Ingela Lanekoff 1 Prostaglandins are important lipids involved in mediating many physiological processes, such as allergic responses, inflammation, and pregnancy. However, technical limitations of in-situ prostaglandin detection in tissue have led researchers to infer prostaglandin tissue dis- tributions from localization of regulatory synthases, such as COX1 and COX2. Herein, we apply a novel mass spectrometry imaging method for direct in situ tissue localization of 1234567890():,; prostaglandins, and combine it with techniques for protein expression and RNA localization. We report that prostaglandin D2, its precursors, and downstream synthases co-localize with the highest expression of COX1, and not COX2. Further, we study tissue with a conditional deletion of transformation-related protein 53 where pregnancy success is low and confirm that PG levels are altered, although localization is conserved. Our studies reveal that the abundance of COX and prostaglandin D2 synthases in cellular regions does not mirror the regional abundance of prostaglandins. Thus, we deduce that prostaglandins tissue localization and abundance may not be inferred by COX or prostaglandin synthases in uterine tissue, and must be resolved by an in situ prostaglandin imaging. 1 Department of Chemistry-BMC, Uppsala University, Uppsala, Sweden. 2 Division of Reproductive Sciences, Cincinnati Children’s Hospital Medical Center, Cincinnati, OH 45229, USA. 3 College of Medicine, University of Cincinnati, Cincinnati, OH 45221, USA. -
Randomized Controlled Pilot Trial of Cabergoline, Hydergine and Levodopa/Carbidopa: Los Angeles Cocaine Rapid Efficacy Screening
Blackwell Science, LtdOxford, UKADDAddiction1359-6357© 2005 Society for the Study of Addiction 100•••• Original Article Cabergoline, hydergine, levodopa/carbidopa Steven Shoptaw et al. RESEARCH REPORT Randomized controlled pilot trial of cabergoline, hydergine and levodopa/carbidopa: Los Angeles Cocaine Rapid Efficacy Screening Trial (CREST) Steven Shoptaw1, Donnie W. Watson2, Chris Reiber1, Richard A. Rawson1, Margaret A. Montgomery3, Maria D. Majewska3 & Walter Ling1 UCLA Integrated Substance Abuse Programs, Los Angeles, CA1 , Friends Research Institute, Inc., Los Angeles, CA2 and National Institute on Drug Abuse, Division of Treatment Research and Development, Bethesda, MD, USA3 Correspondence to: ABSTRACT Steven Shoptaw PhD UCLA/Integrated Substance Abuse Programs Aim This study tested three dopaminergic medications against a common 11075 Santa Monica Blvd unmatched placebo condition: hydergine 1 mg three times daily (n = 15); Suite 200 levodopa/carbidopa 25/100 mg three times daily (n = 15); cabergoline 0.5 mg Los Angeles per week (n = 15); and placebo three times daily (n = 15) as potential pharma- CA 90025 USA cotherapies for cocaine dependence. E-mail: [email protected] Design The four-parallel group, Cocaine Rapid Efficacy Screening Trial (CREST) design featured a 2-week baseline period followed by randomization to an 8-week medication condition that included 1 hour per week of cognitive RESEARCH REPORT behavioral drug counseling. A safety evaluation was conducted 4 weeks after termination. Measures Outcomes included cocaine metabolites measured in urine, reten- tion and self-reports for drug use, cocaine craving, clinical improvement, mood and HIV risk behaviors. Results Participants assigned to receive cabergoline provided more urine sam- ples negative for cocaine metabolites (42.4%) than those assigned to receive pla- cebo (25.0%), a statistically significant difference after controlling for baseline differences in self-reported cocaine use (F = 2.95, df = 3; P = 0.05). -
Plant-Based Medicines for Anxiety Disorders, Part 2: a Review of Clinical Studies with Supporting Preclinical Evidence
CNS Drugs 2013; 24 (5) Review Article Running Header: Plant-Based Anxiolytic Psychopharmacology Plant-Based Medicines for Anxiety Disorders, Part 2: A Review of Clinical Studies with Supporting Preclinical Evidence Jerome Sarris,1,2 Erica McIntyre3 and David A. Camfield2 1 Department of Psychiatry, Faculty of Medicine, University of Melbourne, Richmond, VIC, Australia 2 The Centre for Human Psychopharmacology, Swinburne University of Technology, Melbourne, VIC, Australia 3 School of Psychology, Charles Sturt University, Wagga Wagga, NSW, Australia Correspondence: Jerome Sarris, Department of Psychiatry and The Melbourne Clinic, University of Melbourne, 2 Salisbury Street, Richmond, VIC 3121, Australia. Email: [email protected], Acknowledgements Dr Jerome Sarris is funded by an Australian National Health & Medical Research Council fellowship (NHMRC funding ID 628875), in a strategic partnership with The University of Melbourne, The Centre for Human Psychopharmacology at the Swinburne University of Technology. Jerome Sarris, Erica McIntyre and David A. Camfield have no conflicts of interest that are directly relevant to the content of this article. 1 Abstract Research in the area of herbal psychopharmacology has revealed a variety of promising medicines that may provide benefit in the treatment of general anxiety and specific anxiety disorders. However, a comprehensive review of plant-based anxiolytics has been absent to date. Thus, our aim was to provide a comprehensive narrative review of plant-based medicines that have clinical and/or preclinical evidence of anxiolytic activity. We present the article in two parts. In part one, we reviewed herbal medicines for which only preclinical investigations for anxiolytic activity have been performed. In this current article (part two), we review herbal medicines for which there have been both preclinical and clinical investigations for anxiolytic activity.