Developmental Deltamethrin: Effects on Cognition, Neurotransmitter Systems, Inflammatory Cytokines and Cell Death
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Picrotoxin-Like Channel Blockers of GABAA Receptors
COMMENTARY Picrotoxin-like channel blockers of GABAA receptors Richard W. Olsen* Department of Molecular and Medical Pharmacology, Geffen School of Medicine, University of California, Los Angeles, CA 90095-1735 icrotoxin (PTX) is the prototypic vous system. Instead of an acetylcholine antagonist of GABAA receptors (ACh) target, the cage convulsants are (GABARs), the primary media- noncompetitive GABAR antagonists act- tors of inhibitory neurotransmis- ing at the PTX site: they inhibit GABAR Psion (rapid and tonic) in the nervous currents and synapses in mammalian neu- system. Picrotoxinin (Fig. 1A), the active rons and inhibit [3H]dihydropicrotoxinin ingredient in this plant convulsant, struc- binding to GABAR sites in brain mem- turally does not resemble GABA, a sim- branes (7, 9). A potent example, t-butyl ple, small amino acid, but it is a polycylic bicyclophosphorothionate, is a major re- compound with no nitrogen atom. The search tool used to assay GABARs by compound somehow prevents ion flow radio-ligand binding (10). through the chloride channel activated by This drug target appears to be the site GABA in the GABAR, a member of the of action of the experimental convulsant cys-loop, ligand-gated ion channel super- pentylenetetrazol (1, 4) and numerous family. Unlike the competitive GABAR polychlorinated hydrocarbon insecticides, antagonist bicuculline, PTX is clearly a including dieldrin, lindane, and fipronil, noncompetitive antagonist (NCA), acting compounds that have been applied in not at the GABA recognition site but per- huge amounts to the environment with haps within the ion channel. Thus PTX major agricultural economic impact (2). ͞ appears to be an excellent example of al- Some of the other potent toxicants insec- losteric modulation, which is extremely ticides were also radiolabeled and used to important in protein function in general characterize receptor action, allowing and especially for GABAR (1). -
Picrotoxinin and Diazepam Bind to Two Distinct Proteins: Further Evidence That Pentobarbital May Act at the Picrotoxinin Site1
0270~6474/81/0109-1036$02.00/O The Journal of Neuroscience Copyright 0 Society for Neuroscience Vol. 1, No. 9, pp. 1036-1042 Printed in U.S.A. September 1981 PICROTOXININ AND DIAZEPAM BIND TO TWO DISTINCT PROTEINS: FURTHER EVIDENCE THAT PENTOBARBITAL MAY ACT AT THE PICROTOXININ SITE1 WILLIAM C. DAVIS AND MAHARAJ K. TICKU2 Division of Molecular Pharmacology, Department of Pharmacology, The University of Texas Health Science Center at San Antonio, San Antonio. Texas 78284 Abstract a-[3H]Dihydropicrotoxinin (DHP) and [3H]diazepam binding proteins were solubilized from rat brain membranes with 1% Lubrol-Px. Gel filtration of the Lubrol-solubilized fraction revealed that [3H]DHP and [3H]diazepam bind to two distinct peaks with apparent molecular weights of 185,000 and 61,000, respectively. The signal-to-noise ratio of [3H]DHP binding to 185,000-dalton fractions was improved significantly. [3H]DHP bound to the 185,000-dalton fraction with two binding constants. Muscimol and pentobarbital, while enhancing [3H]diazepam binding to membrane and crude Lubrol-solubilized fractions, failed to enhance [3H]diazepam binding to the 61,000-dalton fraction. Pentobarbital inhibited the binding of [3H]DHP to the 185,000-dalton fraction with an IC5” value of 60 + 12 PM. The binding of [3H]DHP also was inhibited by several depressant and convulsant drugs which affect y-aminobutyric acid (GABA)-mediated transmission. These results provide strong evidence that picrotoxinin and diazepam bind to two distinct proteins and that pentobarbital may act at the picrotoxinin-sensitive site of the benzodiazepine . GABA receptor. ionophore complex. The y-aminobutyric acid (GABA) receptor system ap- Olsen, 1978, 1979; Olsen et al., 1979). -
解 説 GABA Synapse
日 本 農 薬 学 会 誌10, 555-567 (1985) 解 説 GABA支 配 の 神 経 シ ナ ッ プ ス -殺 虫 剤 の タ ー ゲ ッ ト?- 田 中 啓 司 三共株式会社農薬研究所 (昭和60年5月20日 受理) GABA Synapse: A Target Site of Insecticides? Keiji TANAKA Agricultural Chemicals Research Laboratories, Sanhyo Co., Ltd., Yasu-cho, Yasu-gun, Shiga 520-23, Japan やavermectin8)の 出現 で あ る. は じ め に 節 足 動 物 に お け るGABAの 作 用 1950年 に γ-aminobutyric acid (GABA) が マ ウス脳 か ら単 離 同 定1,2)さ れ てか ら, そ の 神 経 伝 達 物 質 と し て Usherwoodら9, 10)は, 昆 虫 の抑 制 性 の神 経 一筋 接 合 部 の 歴 史 が 始 ま る. しか し, 長 い間, この ア ミノ酸 の脳 内 位 でGABAが 当 時 構 造 未 知 で あ った 抑 制 性 の神 経 伝 達 で の 作 用 は 不 明 の まま で, た ん にご代 謝 産 物 で あ ろ うと考 物 質 と 同様 にご作 用 す る こ とを 見 い だ した. GABAは 抑 制 え られ た 時 が あ った ほ どで あ る3). そ の 薬理 作用 が 発 見 性 神 経 が 入 りこ んで い る 筋 線 維 膜 の"input"コ ン ダ ク され た の は 哺 乳動 物 で は な く, 甲殻 類 を用 い て の研 究 で, タ ンス を 増 加 させ る. -
Neurochemical and Behavioral Features in Genetic Absence Epilepsy and in Acutely Induced Absence Seizures
Hindawi Publishing Corporation ISRN Neurology Volume 2013, Article ID 875834, 48 pages http://dx.doi.org/10.1155/2013/875834 Review Article Neurochemical and Behavioral Features in Genetic Absence Epilepsy and in Acutely Induced Absence Seizures A. S. Bazyan1 and G. van Luijtelaar2 1 Institute of Higher Nervous Activity and Neurophysiology, Russian Academy of Science, Russian Federation, 5A Butlerov Street, Moscow 117485, Russia 2 Biological Psychology, Donders Centre for Cognition, Donders Institute for Brain, Cognition and Behavior, Radboud University Nijmegen, P.O. Box 9104, 6500 HE Nijmegen, The Netherlands Correspondence should be addressed to G. van Luijtelaar; [email protected] Received 21 January 2013; Accepted 6 February 2013 Academic Editors: R. L. Macdonald, Y. Wang, and E. M. Wassermann Copyright © 2013 A. S. Bazyan and G. van Luijtelaar. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The absence epilepsy typical electroencephalographic pattern of sharp spikes and slow waves (SWDs) is considered to be dueto an interaction of an initiation site in the cortex and a resonant circuit in the thalamus. The hyperpolarization-activated cyclic nucleotide-gated cationic Ih pacemaker channels (HCN) play an important role in the enhanced cortical excitability. The role of thalamic HCN in SWD occurrence is less clear. Absence epilepsy in the WAG/Rij strain is accompanied by deficiency of the activity of dopaminergic system, which weakens the formation of an emotional positive state, causes depression-like symptoms, and counteracts learning and memory processes. -
Toxicity and Mode of Action of Avermectin B1 Against Insects Terence Simon Corbitt, B.Sc. a Thesis Submitted for the Degree of D
1 Toxicity and Mode of Action of Avermectin B1 against insects Terence Simon Corbitt, B.Sc. A Thesis Submitted for the degree of Doctor of Philosophy of the University of London and for the Diploma of Membership of Imperial College. Department of Pure and Applied Biology Imperial College Silwood Park Ascot, Berkshire SL5 7PY August 1987 2 ACKNOWLEDGEMENTS I would like to thank my supervisor Dr. D.J. Wright for his supervision and advice during the course of this work and presentation of this thesis. I would also like to thank the following: Dr A. Green (Merck Sharp and Dohme, New Jersey) for helpful advice and donation of [3H]AVMB1 and AVMB-j, Drs J. Hardie, D.J.Galley, M. Djamgoz and Mr I. Fosbrook for advice and help given during this study. Thanks also to Ms S.Smith of TDRI, Porton, Wilts, for the Spodoptera 1i ttorali s, and to Mr T.Carty of the Institute of Virology, Oxford for the Heliothis armigera cultures. This work was carried out with the aid of a grant from the Science and Engineering Research Council. Insect culture was carried out under MAFF licence No. PHF 909/52 (116). I would like to thank my parents for their interest and continual support during my education. Thanks also to Tom for plant culture, Sarah for typing my tables, Chris Addison and other friends who made my stay at Silwood Park enjoyable. I would like to say a special thank you to Tanya for her help and friendship. This thesis is dedicated to my wife Anne for her support and understanding during the preparation of this work. -
Studying GABAA Receptors Using AII Amacrine Cells in the Rat Retina by Tuan Van Trinh
Studying GABAA Receptors using AII Amacrine Cells in the Rat Retina By Tuan Van Trinh MASTER THESIS IN PHARMACY Department of Biomedicine/ Centre for Pharmacy University of Bergen May 2018 The picture of AII amacrine cells in front page is adapted from Zhou et al., 2016. 2 ACKNOWLEDGEMENTS This study was carried out at the department of Biomedicine, University of Bergen, during the period August 2012 to April 2013. Due to a serious illness, the project was interrupted, and continued again in April 2018 to May 2018. I would like to thank several people for their support during this project. First I would like to express my sincere gratitude to my supervisor prof. Ph.d Margaret Lin Veruki and co-supervisor prof. dr. med. Espen Hartveit for valuable advice and much appreciated guidance during the period. Ph.d. Yifan Zhou is thanked for helping me with collecting the data, and of course thanks to Marte Nørve Årvik, Lise Skålvik Amble and all my co-workers and lab personnel that have helped me during this period. To my family and my friends thank you for supporting me during this hard period of life. Bergen, May 2018 3 TABLE OF CONTENTS ACKNOWLEDGEMENTS……………………………………………………..3 TABLE OF CONTENTS………………………………………………………..4 ABBREVIATIONS……...………………………………………………………8 AIMS……………………...…………………………………………………....11 SUMMARY……………………...…………………………………………….13 1.0 INTRODUCTION AND THEORY……………………………………………16 1.1 Nerve cell and signal communication ………………………………16 1.1.1 Cell membrane……………………………..……………………...17 1.1.2 The membrane potential………….…………………….……….……..18 1.1.3 The -
Rapid Throughput Analysis of GABAA Receptor Subtype Modulators and Blockers Using Disbac1(3) Membrane Potential Red
Molecular Pharmacology Fast Forward. Published on April 20, 2017 as DOI: 10.1124/mol.117.108563 This article has not been copyedited and formatted. The final version may differ from this version. Mol #108563 TITLE PAGE Rapid Throughput Analysis of GABAA Receptor Subtype Modulators and Blockers Using DiSBAC1(3) Membrane Potential Red Dye Atefeh Mousavi Nik, Brandon Pressly, Vikrant Singh, Shane Antrobus, Susan Hulsizer, Michael A. Rogawski, Heike Wulff and Isaac N. Pessah Department of Molecular Biosciences, School of Veterinary Medicine (A.M.N., S.A., S.H., Downloaded from I.N.P.); Department of Pharmacology (B.P., V.S., M.A.R., H.W.), School of Medicine, University of California, Davis, Davis, CA 95616, USA; and Department of Neurology molpharm.aspetjournals.org (M.A.R.), School of Medicine, University of California, Davis, Sacramento, CA 95817; The Medical Investigation of Neurodevelopmental Disorders (MIND) Institute (I.N.P.), Sacramento, CA 95817, USA at ASPET Journals on September 30, 2021 1 Molecular Pharmacology Fast Forward. Published on April 20, 2017 as DOI: 10.1124/mol.117.108563 This article has not been copyedited and formatted. The final version may differ from this version. Mol #108563 RUNNING TITLE PAGE Running title: Analysis of GABAA receptor modulators with potentiometric dye Corresponding author: Isaac N. Pessah, Department of Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, One Shields Avenue, Davis, CA 95616, USA. Phone: (530) 752- 6696; E-mail: [email protected] Number of -
British Chemical and Physiological Abstracts
BRITISH CHEMICAL AND PHYSIOLOGICAL ABSTRACTS ISSUED BY THE Bureau of Chemical and Physiological Abstracts [Supported by the Chemical Society, the Society of Chemical Industry, the Physiological Society, the Biochemical Society, and the Anatomical Society of Great Britain and Ireland] JULY, 1 9 4 3 BUREAU: Chairman : L. H. LAMPITT, D.Sc., F.I.C. Hon. Treasurer: F. P. DUNN, B.Sc., F.I.C. JULIAN L. BAKER, F.I.C. C. R. HARINGTON, M.A., Ph.D., F.R.S. G. L. BROWN, M.Sc., M.B., ‘Ch.B. L. A. JORDAN, D.Sc., F.I.C. H. W. CREMER, M.Sc., F.I.C., M.I.Chem.E. G. A. R. KON, M.A., D.Sc., F.R.S. C. W. DAVIES, D.Sc., F.I.C. H. McCOMBIE, D.S.O., M.C., Ph.D., D.Sc ., F.I.C. H. J. T. ELLINGHAM, B.Sc., Ph.D., F.I.C. B. A. McSWINEY, B.A., M.B., Sc.D. E d ito r : T. F. BURTON, B.Sc. Assistant Editors: J. H. BIRKINSHAW, D.Sc., F.I.C.* W. JEVONS, D.Sc., Ph.D. E. E. TURNER, M.A., D.Sc., F.I.C., F.R.S. H. BURTON, M.Sc., D.Sc., F.I.C. F. L. USHER, D.Sc. ' F. G. CROSSE, F.I.C. H. WREN, M.A., D.Sc., P h.D. A. A. ELDRIDGE, B.Sc., F.I.C. SAMSON WRIGHT, M.D., F.R.C.P.* Assisted by J. D. BOYD (Anatomy), A. HADDOW (Tumours), F. O. HOWITT (Biochemistry), A. G. -
Dissertation
DISSERTATION Titel der Dissertation „Isolation of positive, allosteric GABAA receptor modulators from Chinese herbal drugs traditionally used in the treatment of anxiety and insomnia“ Verfasserin Mag. pharm. Judith Singhuber angestrebter akademischer Grad Doktorin der Naturwissenschaften (Dr.rer.nat.) Wien, 2011 Studienkennzahl lt. A 091 449 Studienblatt: Dissertationsgebiet lt. Dr.-Studium der Naturwissenschaften Pharmazie Studienblatt: Betreuerin / Betreuer: Univ. Prof. Mag. Dr. Brigitte Kopp For Maximillian & Lennox ACKNOWLEDGMENTS In this place I would like to thank the people which contributed to the success of my thesis: Prof. Brigitte Kopp, my supervisor, for providing an interesting topic and for her guidance. Prof. Steffen Hering (Department of Pharmacology and Toxicology, University of Vienna) for the possibility to work in his Department. Dr. Igor Baburin (Department of Pharmacology and Toxicology, University of Vienna) for the pharmacological investigations on the 56 extracts and the HPLC fractions of A. macrocephala and C. monnieri. Dr. Sophia Khom (former Department of Pharmacology and Toxicology, University of Vienna) for her assistance as well as interesting discussions on GABAergic neurotransmission and other topics. Prof. Gerhard F. Ecker (Department of Medicinal Chemistry) for the binary QSAR and help with the pharmacophore model. Prof. Ernst Urban (Department of Medicinal Chemistry, University of Vienna) und Prof. Hanspeter Kählig (Institute of Organic Chemistry, University of Vienna) for the NMR- measurements. Dr. -
Ionotropic GABA Receptors and Distal Retinal on and OFF Responses
Hindawi Publishing Corporation Scientifica Volume 2014, Article ID 149187, 23 pages http://dx.doi.org/10.1155/2014/149187 Review Article Ionotropic GABA Receptors and Distal Retinal ON and OFF Responses E. Popova Department of Physiology, Medical Faculty, Medical University, 1431 Sofia, Bulgaria Correspondence should be addressed to E. Popova; [email protected] Received 11 February 2014; Revised 24 April 2014; Accepted 27 May 2014; Published 20 July 2014 Academic Editor: Marco Sassoe-Pognetto Copyright © 2014 E. Popova. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. In the vertebrate retina, visual signals are segregated into parallel ON and OFF pathways, which provide information for light increments and decrements. The segregation is first evident at the level of the ON and OFF bipolar cells in distal retina. The activity of large populations of ON and OFF bipolar cells is reflected in the b- and d-waves of the diffuse electroretinogram (ERG). The role of gamma-aminobutyric acid (GABA), acting through ionotropic GABA receptors in shaping the ON and OFF responses in distal retina, is a matter of debate. This review summarized current knowledge about the types of the GABAergic neurons and ionotropic GABA receptors in the retina as well as the effects of GABA and specific AGABA and GABAC receptor antagonists on the activity of the ON and OFF bipolar cells in both nonmammalian and mammalian retina. Special emphasis is put on the effects on b- and d-waves of the ERG as a useful tool for assessment of the overall function of distal retinal ON and OFF channels. -
Ionotropic GABA Receptors and Distal Retinal on and OFF Responses
Hindawi Publishing Corporation Scientifica Volume 2014, Article ID 149187, 23 pages http://dx.doi.org/10.1155/2014/149187 Review Article Ionotropic GABA Receptors and Distal Retinal ON and OFF Responses E. Popova Department of Physiology, Medical Faculty, Medical University, 1431 Sofia, Bulgaria Correspondence should be addressed to E. Popova; [email protected] Received 11 February 2014; Revised 24 April 2014; Accepted 27 May 2014; Published 20 July 2014 Academic Editor: Marco Sassoe-Pognetto Copyright © 2014 E. Popova. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. In the vertebrate retina, visual signals are segregated into parallel ON and OFF pathways, which provide information for light increments and decrements. The segregation is first evident at the level of the ON and OFF bipolar cells in distal retina. The activity of large populations of ON and OFF bipolar cells is reflected in the b- and d-waves of the diffuse electroretinogram (ERG). The role of gamma-aminobutyric acid (GABA), acting through ionotropic GABA receptors in shaping the ON and OFF responses in distal retina, is a matter of debate. This review summarized current knowledge about the types of the GABAergic neurons and ionotropic GABA receptors in the retina as well as the effects of GABA and specific AGABA and GABAC receptor antagonists on the activity of the ON and OFF bipolar cells in both nonmammalian and mammalian retina. Special emphasis is put on the effects on b- and d-waves of the ERG as a useful tool for assessment of the overall function of distal retinal ON and OFF channels. -
Exposure to Amitraz, Fipronil and Permethrin Affects Cell Viability And
Mangia et al. Parasites & Vectors (2018) 11:437 https://doi.org/10.1186/s13071-018-3020-4 RESEARCH Open Access Exposure to amitraz, fipronil and permethrin affects cell viability and ABC transporter gene expression in an Ixodes ricinus cell line Carlo Mangia1*, Alice Vismarra1, Marco Genchi1, Sara Epis2,7, Claudio Bandi3,7, Giulio Grandi4, Lesley Bell-Sakyi5, Domenico Otranto6, Benedetta Passeri1 and Laura Kramer1 Abstract Background: Over-expression of ATP-binding cassette (ABC) transporter proteins has been implicated in resistance of ticks to acaricides. Tick cell lines are useful for investigating resistance mechanisms, as development of an in vitro model for the study of acaricide resistance would contribute to improving knowledge of the molecular basis behind drug processing and exclusion in ticks. In the present study, cultures of the Ixodes ricinus-derived cell line IRE/CTVM19 were treated with the acaricides amitraz, permethrin or fipronil to determine modulation of ABC transporter gene expression. Cells were treated with different drug concentrations (25, 50, 100, 150 μM) and incubated for ten days. Cell morphology, viability, metabolic activity and relative expression of ABC (B1, B6, B8 and B10) genes were determined at day 10 post-treatment. Results: Cell morphology determined by light microscopy was altered following treatment with all drugs, but only at high concentrations, while total cell numbers decreased with increasing drug dose. Cell viability determined by trypan blue exclusion was not significantly different from untreated controls (P > 0.1) following treatment with amitraz and permethrin, but high concentrations of fipronil caused decrease (up to 37%, P < 0.01) in viability. At all drug concentrations, fipronil and permethrin induced dose-dependent reduction in cell metabolic activity measured by MTT assay (P < 0.01).