Drug interactions at GABA A receptors

Drug interactions at GABA A receptors Neurotransmitter receptor systems have been the focus of intensive pharmacological research for more than 20 years for basic and applied scientific reasons, but only recently has there been a better understanding of their key features. One of these systems includes the type A receptor for the γ-aminobutyric acid (GABA), which forms an integral anion channel from a pentameric subunit assembly and mediates most of the fast inhibitory neurotransmission in the adult vertebrate central nervous system. Up to now, depending on the definition, 16–19 mammalian subunits have been cloned and localized on different genes. Their assembly into proteins in a poorly defined stoichiometry forms the basis of functional and pharmacological GABA A receptor diversity, i.e. the receptor subtypes. The latter has been well documented in autoradiographic studies using ligands that label some of the receptors’ various binding sites, corroborated by recombinant expression studies using the same tools. Significantly less heterogeneity has been found at the physiological level in native receptors, where the subunit combinations have been difficult to dissect. This review focuses on the characteristics, use and usefulness of various ligands and their binding sites to probe GABA A receptor properties and to gain insight into the biological function from fish to man and into evolutionary conserved GABA A receptor heterogeneity. We also summarize the properties of the novel mouse models created for the study of various brain functions and review the state-of-the-art imaging of brain GABA A receptors in various human neuropsychiatric conditions. The data indicate that the present ligands are only partly satisfactory tools and further ligands with subtype-selective properties are needed for imaging purposes and for confirming the behavioral and functional results of the studies presently carried out in gene-targeted mice with other species, including man. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Progress in Neurobiology Elsevier

Loading next page...
 
/lp/elsevier/drug-interactions-at-gaba-a-receptors-E4Fh860yOW
Publisher
Elsevier
Copyright
Copyright © 2002 Elsevier Science Ltd
ISSN
0301-0082
DOI
10.1016/S0301-0082(02)00013-8
Publisher site
See Article on Publisher Site

Abstract

Neurotransmitter receptor systems have been the focus of intensive pharmacological research for more than 20 years for basic and applied scientific reasons, but only recently has there been a better understanding of their key features. One of these systems includes the type A receptor for the γ-aminobutyric acid (GABA), which forms an integral anion channel from a pentameric subunit assembly and mediates most of the fast inhibitory neurotransmission in the adult vertebrate central nervous system. Up to now, depending on the definition, 16–19 mammalian subunits have been cloned and localized on different genes. Their assembly into proteins in a poorly defined stoichiometry forms the basis of functional and pharmacological GABA A receptor diversity, i.e. the receptor subtypes. The latter has been well documented in autoradiographic studies using ligands that label some of the receptors’ various binding sites, corroborated by recombinant expression studies using the same tools. Significantly less heterogeneity has been found at the physiological level in native receptors, where the subunit combinations have been difficult to dissect. This review focuses on the characteristics, use and usefulness of various ligands and their binding sites to probe GABA A receptor properties and to gain insight into the biological function from fish to man and into evolutionary conserved GABA A receptor heterogeneity. We also summarize the properties of the novel mouse models created for the study of various brain functions and review the state-of-the-art imaging of brain GABA A receptors in various human neuropsychiatric conditions. The data indicate that the present ligands are only partly satisfactory tools and further ligands with subtype-selective properties are needed for imaging purposes and for confirming the behavioral and functional results of the studies presently carried out in gene-targeted mice with other species, including man.

Journal

Progress in NeurobiologyElsevier

Published: Jun 1, 2002

References

  • Central benzodiazepine receptor occupancy by zolpidem in the human brain as assessed by positron emission tomography
    Abadie, P; Rioux, P; Scatton, B; Zarifian, E; Barre, L; Patat, A; Baron, J.C
  • Relationships between trait and state anxiety and the central benzodiazepine receptor: a PET study
    Abadie, P; Boulenger, J.P; Benali, K; Barre, L; Zarifian, E; Baron, J.C
  • Neurosteroids: a new brain function
    Baulieu, E.E; Robel, P
  • Modulation of human recombinant GABA A receptors by pregnanediols
    Belelli, D; Lambert, J.J; Peters, J.A; Gee, K.W; Lan, N.C
  • Genetic factors in addiction: QTL mapping and candidate gene studies implicate GABAergic genes in alcohol and barbiturate withdrawal in mice
    Buck, K.J; Finn, D.A
  • GABA and epileptogenesis: comparing gabrb3 gene-deficient mice with Angelman syndrome in man
    DeLorey, T.M; Olsen, R.W
  • GABA-mimetic activity and effects on diazepam binding of aminosulphonic acids structurally related to piperidine-4-sulphonic acid
    Falch, E; Jacobsen, P; Krogsgaard-Larsen, P; Curtis, D.R
  • Differential sensitivity of recombinant GABA A receptors expressed in Xenopus oocytes to modulation by topiramate
    Gordey, M; DeLorey, T.M; Olsen, R.W
  • The role of GABA A receptors in the acute and chronic effects of ethanol
    Grobin, A.C; Matthews, D.B; Devaud, L.L; Morrow, A.L
  • ( 18 F )Fluoroethylflumazenil: a novel tracer for PET imaging of human benzodiazepine receptors
    Gründer, G; Siessmeier, T; Lange-Asschenfeldt, C; Vernaleken, I; Buchholz, H.G; Stoeter, P; Drzezga, A; Lüddens, H; Rösch, F; Bartenstein, P
  • Ethanol actions on multiple ion channels: which are important?
    Harris, R.A
  • Ethanol increases GABA A responses in cells stably transfected with receptor subunits
    Harris, R.A; Proctor, W.R; McQuilkin, S.J; Klein, R.L; Mascia, M.P; Whatley, V; Whiting, P.J; Dunwiddie, T.V
  • Effects of GABA and various allosteric ligands on TBPS binding to cloned rat GABA A receptor subtypes
    Im, W.B; Pregenzer, J.F; Thomsen, D.R
  • The main determinant of furosemide inhibition on GABA A receptors is located close to the first transmembrane domain
    Jackel, C; Kleinz, R; Mäkelä, R; Hevers, W; Jezequel, S; Korpi, E.R; Lüddens, H
  • The multifaceted and widespread pathology of magnesium deficiency
    Johnson, S
  • Cis - and trans -4-aminocrotonic acid as GABA analogues of restricted conformation
    Johnston, G.A; Curtis, D.R; Beart, P.M; Game, C.J; McCulloch, R.M; Twitchin, B
  • Role of the PLC-related, catalytically inactive protein p130 in GABA A receptor function
    Kanematsu, T; Jang, I.S; Yamaguchi, T; Nagahama, H; Yoshimura, K; Hidaka, K; Matsuda, M; Takeuchi, H; Misumi, Y; Nakayama, K; Yamamoto, T; Akaike, N; Hirata, M; Nakayama, K.I
  • Furosemide interactions with brain GABA A receptors
    Korpi, E.R; Lüddens, H
  • Ethanol: novel actions on nerve cell physiology explain impaired functions
    Korpi, E.R; Mäkelä, R; Uusi-Oukari, M
  • Increased behavioral neurosteroid sensitivity in a rat line selectively bred for high alcohol sensitivity
    Korpi, E.R; Mäkelä, R; Romeo, E; Guidotti, A; Uusi-Oukari, M; Furnari, C; di Michele, F; Sarviharju, M; Xu, M; Rosenberg, P.H
  • A subunit isoform influences GABA A receptor modulation by propofol
    Krasowski, M.D; O’Shea, S.M; Rick, C.E; Whiting, P.J; Hadingham, K.L; Czajkowski, C; Harrison, N.L
  • Electrophysiological studies of the GABA A receptor ligand, 4-PIOL, on cultured hippocampal neurones
    Kristiansen, U; Lambert, J.D; Falch, E; Krogsgaard-Larsen, P
  • Alterations of GABA A receptor subunit mRNA levels associated with increases in punished responding induced by acute alprazolam administration: an in situ hybridization study
    Liu, M; Glowa, J.R
  • GABA A /benzodiazepine receptor heterogeneity: neurophysiological implications
    Lüddens, H; Korpi, E.R; Seeburg, P.H
  • Structure–activity relationship of furosemide-derived compounds as antagonists of cerebellum-specific GABA A receptors
    Lüddens, H; Lang, H.J; Korpi, E.R
  • Blunted furosemide action on cerebellar GABA A receptors in ANT rats selectively bred for high alcohol sensitivity
    Mäkelä, R; Lehtonen, M; Wisden, W; Lüddens, H; Korpi, E.R
  • Loreclezole and La 3+ differentiate cerebellar granule cell GABA A receptor subtypes
    Mäkelä, R; Wisden, W; Korpi, E.R
  • Dissociation of ( 35 S ) t -butylbicyclophosphorothionate binding differentiates convulsant and depressant drugs that modulate GABAergic transmission
    Maksay, G; Ticku, M.K
  • A novel GABA A antagonist ( 3 H )SR 95531: microscopic analysis of binding in the rat brain and allosteric modulation by several benzodiazepine and barbiturate receptor ligands
    McCabe, R.T; Wamsley, J.K; Yezuita, J.P; Olsen, R.W
  • Benzodiazepine antagonist Ro 15–1788: binding characteristics and interaction with drug-induced changes in dopamine turnover and cerebellar cGMP levels
    Möhler, H; Burkard, W.P; Keller, H.H; Richards, J.G; Haefely, W
  • GABA A receptor subtypes: a new pharmacology
    Möhler, H; Crestani, F; Rudolph, U
  • Linkage disequilibrium at the angelman syndrome gene UBE3A in autism families
    Nurmi, E.L; Bradford, Y; Chen, Y; Hall, J; Arnone, B; Gardiner, M.B; Hutcheson, H.B; Gilbert, J.R; Pericak-Vance, M.A; Copeland-Yates, S.A; Michaelis, R.C; Wassink, T.H; Santangelo, S.L; Sheffield, V.C; Piven, J; Folstein, S.E; Haines, J.L; Sutcliffe, J.S
  • Activation of protein kinase C by phorbol dibutyrate modulates GABA A receptor binding in rat brain slices
    Oh, S; Jang, C.G; Ma, T; Ho, I.K
  • PET analysis of alcohol interaction with the brain disposition of ( 11 C )flumazenil
    Pauli, S; Liljequist, S; Farde, L; Swahn, C.G; Halldin, C; Litton, J.E; Sedvall, G
  • Modulation of the GABA A receptor by depressant barbiturates and pregnane steroids
    Peters, J.A; Kirkness, E.F; Callachan, H; Lambert, J.J; Turner, A.J
  • Low brain GABA level is associated with poor seizure control
    Petroff, O.A; Rothman, D.L; Behar, K.L; Mattson, R.H
  • Benzodiazepine–GABA A receptor binding during absence seizures
    Prevett, M.C; Lammertsma, A.A; Brooks, D.J; Cunningham, V.J; Fish, D.R; Duncan, J.S
  • Benzodiazepine–GABA A receptors in idiopathic generalized epilepsy measured with ( 11 C )flumazenil and positron emission tomography
    Prevett, M.C; Lammertsma, A.A; Brooks, D.J; Bartenstein, P.A; Patsalos, P.N; Fish, D.R; Duncan, J.S
  • Brain region-dependent sensitivity of GABA A receptor-mediated responses to modulation by ethanol
    Proctor, W.R; Allan, A.M; Dunwiddie, T.V
  • Coupling between agonist and chloride ionophore sites of the GABA A receptor: agonist/antagonist efficacy of 4-PIOL
    Rabe, H; Picard, R; Uusi-Oukari, M; Hevers, W; Lüddens, H; Korpi, E.R
  • From ion currents to genomic analysis: recent advances in GABA A receptor research
    Rabow, L.E; Russek, S.J; Farb, D.H
  • Changes in benzodiazepine receptors in Alzheimer-type dementia
    Shimohama, S; Taniguchi, T; Fujiwara, M; Kameyama, M
  • GABA A receptors are differentially sensitive to zinc: dependence on subunit composition
    Smart, T.G; Moss, S.J; Xie, X; Huganir, R.L
  • GABA A receptor expression in glioma cells is triggered by contact with neuronal cells
    Synowitz, M; Ahmann, P; Matyash, M; Kuhn, S.A; Hofmann, B; Zimmer, C; Kirchhoff, F; Kiwit, J.C; Kettenmann, H
  • Relative contributions of passive equilibrium and active transport to the distribution of chloride in mammalian cortical neurons
    Thompson, S.M; Deisz, R.A; Prince, D.A
  • Barbiturate interactions at the human GABA A receptor: dependence on receptor subunit combination
    Thompson, S.A; Whiting, P.J; Wafford, K.A
  • Behavioral sensitivity and ethanol potentiation of the N -methyl- d -aspartate receptor antagonist MK-801 in a rat line selected for high ethanol sensitivity
    Toropainen, M; Nakki, R; Honkanen, A; Rosenberg, P.H; Laurie, D.J; Pelto-Huikko, M; Koistinaho, J; Eriksson, C.J; Korpi, E.R
  • Etomidate potentiation of GABA A receptor gated current depends on the subunit composition
    Uchida, I; Kamatchi, G; Burt, D; Yang, J
  • Diazepam sensitivity of the binding of an imidazobenzodiazepine, ( 3 H )Ro 15–4513, in cerebellar membranes from two rat lines developed for high and low alcohol sensitivity
    Uusi-Oukari, M; Korpi, E.R
  • Specific alterations in the cerebellar GABA A receptors of an alcohol-sensitive ANT rat line
    Uusi-Oukari, M; Korpi, E.R
  • Cation modulation of GABA A receptors in brain sections of AT and ANT rats
    Uusi-Oukari, M; Mäkelä, R; Soini, S; Korpi, E.R
  • Cerebellar GABA A receptors and anxiolytic action of diazepam
    Vekovischeva, O.Y; Haapalinna, A; Sarviharju, M; Honkanen, A; Korpi, E.R
  • Regional brain metabolic response to lorazepam in alcoholics during early and late alcohol detoxification
    Volkow, N.D; Wang, G.J; Overall, J.E; Hitzemann, R; Fowler, J.S; Pappas, N; Frecska, E; Piscani, K
  • The GABA A receptor gene family: new targets for therapeutic intervention
    Whiting, P.J
  • Modulation of ( 3 H )diazepam binding in rat cortical membranes by GABA A agonists
    Wong, E.H; Iversen, L.L
  • Pharmacologic actions of subtype-selective and novel GABAergic ligands in rat lines with differential sensitivity to ethanol
    Wong, G; Sarviharju, M; Toropainen, M; Matecka, D; Korpi, E.R
  • Effects of clozapine metabolites and chronic clozapine treatment on rat brain GABA A receptors
    Wong, G; Kuoppamaki, M; Hietala, J; Lüddens, H; Syvälahti, E; Korpi, E.R
  • Interaction of allosteric ligands with GABA A receptors containing one, two, or three different subunits
    Zezula, J; Slany, A; Sieghart, W
  • Development of GABA-mediated, chloride-dependent inhibition in CA1 pyramidal neurones of immature rat hippocampal slices
    Zhang, L; Spigelman, I; Carlen, P.L
  • Lanthanum-mediated modification of GABA A receptor deactivation, desensitization and inhibitory synaptic currents in rat cerebellar neurons
    Zhu, W.J; Wang, J.F; Corsi, L; Vicini, S

You’re reading a free preview. Subscribe to read the entire article.


DeepDyve is your
personal research library

It’s your single place to instantly
discover and read the research
that matters to you.

Enjoy affordable access to
over 18 million articles from more than
15,000 peer-reviewed journals.

All for just $49/month

Explore the DeepDyve Library

Search

Query the DeepDyve database, plus search all of PubMed and Google Scholar seamlessly

Organize

Save any article or search result from DeepDyve, PubMed, and Google Scholar... all in one place.

Access

Get unlimited, online access to over 18 million full-text articles from more than 15,000 scientific journals.

Your journals are on DeepDyve

Read from thousands of the leading scholarly journals from SpringerNature, Elsevier, Wiley-Blackwell, Oxford University Press and more.

All the latest content is available, no embargo periods.

See the journals in your area

DeepDyve

Freelancer

DeepDyve

Pro

Price

FREE

$49/month
$360/year

Save searches from
Google Scholar,
PubMed

Create folders to
organize your research

Export folders, citations

Read DeepDyve articles

Abstract access only

Unlimited access to over
18 million full-text articles

Print

20 pages / month

PDF Discount

20% off