The GABAA receptor-gated ion channel: biochemical and pharmacological studies of structure and function.


:In the past few years, substantial advances have been made in analyzing the structure and function of the GABA receptor-gated Cl- channel. A major goal is to identify the molecular characteristics of the GABAA receptor that are necessary for maintaining normal GABAergic neurotransmission. Future studies will undoubtedly include techniques that have been used successfully to construct a detailed structural and dynamic model of the nACHR-gated ion channel. These include X-ray scattering, single group rotation theory, and genetic homology, deletion and site-directed mutation studies. Such techniques will make it possible to identify the structural defects that give rise to abnormal GABA receptor function and possibly to sleep, anxiety and seizure disorders.


Biochem Pharmacol


Biochemical pharmacology


Schwartz RD




Has Abstract


1988-09-15 00:00:00














  • Immunospecific targeting of liposomes to erythrocytes.

    abstract::Immunoliposomes were made by covalently linking Fab' fragments (from rabbit antimouse erythrocyte IgG) to reverse-phase evaporation vesicles (REV) via maleimido-4-(p-phenylbutyrate) phosphatidylethanolamine (MPB-PE) as anchor molecule. These immunoliposomes were characterized in terms of size, charge, stability and an...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Peeters PA,Claessens CA,Eling WM,Crommelin DJ

    更新日期:1988-06-01 00:00:00

  • Effect of pentylenetetrazol on carbaryl-induced changes in striatal catecholamines.

    abstract::Administration of pentylenetetrazol (PTZ) (60 mg/kg, s.c.) to normal or carbaryl (200 mg/kg, p.o.) treated adult male albino rats produced characteristic changes in the steady-state levels of striatal dopamine (DA), noradrenaline (NA) and homovanillic acid (HVA) at different time intervals (0.5, 1.0 and 2.0 hr). The e...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ray SK,Poddar MK

    更新日期:1985-02-15 00:00:00

  • Induction by staurosporine of hepatocyte growth factor production in human skin fibroblasts independent of protein kinase inhibition.

    abstract::Staurosporine is one of the most potent and well known inhibitors of protein kinases, and it is often used to study the involvement of protein kinases in signal transduction pathways. We now report that staurosporine can induce the production of hepatocyte growth factor (HGF) independently of protein kinase inhibition...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yagi Y,Sotani T,Nagao T,Horio T,Yamamoto I,Gohda E

    更新日期:2003-11-01 00:00:00

  • Reactive oxygen species are required for β2 adrenergic receptor-β-arrestin interactions and signaling to ERK1/2.

    abstract::The β2-adrenergic receptor (β2AR) is the prototypical member of the heptahelical G protein-coupled receptor (GPCR) superfamily and is well-known to elicit biological effects through both G protein-dependent and G protein-independent signaling cascades. Agonism of β2AR has been described to promote phosphorylation and ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Singh M,Moniri NH

    更新日期:2012-09-01 00:00:00

  • The prodigiosins, proapoptotic drugs with anticancer properties.

    abstract::The family of natural red pigments, called prodigiosins (PGs), characterised by a common pyrrolylpyrromethene skeleton, are produced by various bacteria. Some members have immunosuppressive properties and apoptotic effects in vitro and they have also displayed antitumour activity in vivo. Understanding the mechanism o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Pérez-Tomás R,Montaner B,Llagostera E,Soto-Cerrato V

    更新日期:2003-10-15 00:00:00

  • Isolation and characterization at cholinergic nicotinic receptors of a neurotoxin from the venom of the Acanthophis sp. Seram death adder.

    abstract::The present study describes the isolation of the first neurotoxin (acantoxin IVa) from Acanthophis sp. Seram death adder venom and an examination of its activity at nicotinic acetylcholine receptor (nAChR) subtypes. Acantoxin IVa (MW 6815; 0.1-1.0 microM) caused concentration-dependent inhibition of indirect twitches ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wickramaratna JC,Fry BG,Loiacono RE,Aguilar MI,Alewood PF,Hodgson WC

    更新日期:2004-07-15 00:00:00

  • Effect of repeated administration of 11-hydroxy-delta 8-tetrahydrocannabinol, an active metabolite of delta 8-tetrahydrocannabinol, on the hepatic microsomal drug-metabolizing enzyme system of mice.

    abstract::The effects of delta 8-tetrahydrocannabinol (delta 8-THC) and its major and active metabolite, 11-hydroxy-delta 8-tetrahydrocannabinol (11-OH-delta 8-THC), on the hepatic microsomal drug-metabolizing enzyme system were studied in mice. The repeated administration of 11-OH-delta 8-THC (5 mg/kg/day, i.v.) for 3 or 7 day...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Watanabe K,Arai M,Narimatsu S,Yamamoto I,Yoshimura H

    更新日期:1986-06-01 00:00:00

  • Inhibition of glycosaminoglycan synthesis in anatomically intact rat patellar cartilage by paracetamol-induced serum sulfate depletion.

    abstract::We have studied the effect of low sulfate concentrations on the glycosaminoglycan synthesis in rat patellar cartilage in vivo as well as in vitro. The oral administration of 200 mg/kg paracetamol to male Wistar rats resulted in a significant reduction of the serum sulfate concentration. Reduced serum sulfate availabil...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: van der Kraan PM,de Vries BJ,Vitters EL,van den Berg WB,van de Putte LB

    更新日期:1988-10-01 00:00:00

  • Dissociation of the striatal D-2 dopamine receptor from adenylyl cyclase following 6-hydroxydopamine-induced denervation.

    abstract::Intracellular cyclic AMP accumulation following exposure to dopamine (DA) agonists and and antagonists was measured in striatal slices from rats with a unilateral 6-hydroxydopamine (6-OHDA) lesion of the nigrostriatal pathway and which showed contralateral circling to apomorphine. Both DA (10-320 microM) and the D-1 a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Thomas KL,Rose S,Jenner P,Marsden CD

    更新日期:1992-07-07 00:00:00

  • On the mechanisms of phenothiazine-induced mitochondrial permeability transition: Thiol oxidation, strict Ca2+ dependence, and cyt c release.

    abstract::Phenothiazines (PTZ) are drugs widely used in the treatment of schizophrenia. Trifluoperazine, a piperazinic PTZ derivative, has been described as inhibitor of the mitochondrial permeability transition (MPT). We reported previously the antioxidant activity of thioridazine at relatively low concentrations associated to...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Cruz TS,Faria PA,Santana DP,Ferreira JC,Oliveira V,Nascimento OR,Cerchiaro G,Curti C,Nantes IL,Rodrigues T

    更新日期:2010-10-15 00:00:00

  • Alpha-galactosylceramide modulates the induction of indoleamine 2,3-dioxygenase in antigen presenting cells.

    abstract::The glycolipid alpha-galactosylceramide (alpha-GalCer), when presented on CD1 molecules by antigen presenting cells (APCs) to invariant NKT (iNKT cells), is a potent immunomodulator. Indoleamine 2,3-dioxygenase (IDO), an enzyme catalyzing the catabolism of L-tryptophan along the kynurenine pathway, is inducible in APC...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Fallarini S,Paoletti T,Panza L,Lombardi G

    更新日期:2008-09-15 00:00:00

  • Hydroxypropyl-beta-cyclodextrin as delivery system for thyroid hormones, regulating glutathione S-transferase expression in rat hepatocyte co-cultures.

    abstract::Thyroid hormones play a role in the regulation of glutathione S-transferase (GST) expression. Here, co-cultures of rat hepatocytes with bile duct epithelial cells have been used to study the direct effects of both triiodothyronine (T3) and thyroxine (T4) on GST activities and proteins. Because T3 and T4 are poorly wat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Vanhaecke T,Derde MP,Vercruysse A,Rogiers V

    更新日期:2001-05-01 00:00:00

  • Inhibition of carcinogen-bioactivating cytochrome P450 1 isoforms by amiloride derivatives.

    abstract::We examined the effects of amiloride derivatives, especially 5-(N-ethyl-N-isopropyl)amiloride (EIPA), on the activity of cytochrome P450 (CYP) 1 isoforms, known to metabolize carcinogenic polycyclic aromatic hydrocarbons (PAHs), such as benzo(a)pyrene (BP), into mutagenic metabolites and whose cellular expression can ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sparfel L,Huc L,Le Vee M,Desille M,Lagadic-Gossmann D,Fardel O

    更新日期:2004-05-01 00:00:00

  • Parkin is transcriptionally regulated by the aryl hydrocarbon receptor: Impact on α-synuclein protein levels.

    abstract::Parkin (PRKN) is a ubiquitin E3 ligase that catalyzes the ubiquitination of several proteins. Mutations in the human Parkin gene, PRKN, leads to degeneration of dopaminergic (DA) neurons, resulting in autosomal recessive early-onset parkinsonism and the loss of PRKN function is linked to sporadic Parkinson's disease (...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: González-Barbosa E,García-Aguilar R,Vega L,Cabañas-Cortés MA,Gonzalez FJ,Segovia J,Morales-Lázaro SL,Cisneros B,Elizondo G

    更新日期:2019-10-01 00:00:00

  • Sensitization of human neutrophil defense activities through activation of platelet-activating factor receptors by ginkgolide B, a bioactive component of the Ginkgo biloba extract EGB 761.

    abstract::Ginkgolide B (GKB, BN 52021) was described as a platelet-activating factor (Paf) receptor antagonist. However, it is not known whether all GKB biological effects are mediated through Paf receptor antagonism only. To gain insight into the drug mode of action, we investigated here the effects of GKB per se on functional...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lenoir M,Pedruzzi E,Rais S,Drieu K,Perianin A

    更新日期:2002-04-01 00:00:00

  • Recovery after hypoglycemic brain injury. Action of some biological substances on the cerebral metabolism.

    abstract::In artificially ventilated beagle dogs a severe hypoglycemic condition was induced by insulin injection, while the posthypoglycemic recovery was induced by glucose treatment at the end of a 20-min period of spontaneous electroencephalographic silence. The motor area of the cerebral cortex was analyzed for glycolytic m...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Benzi G,Gorini A,Dossena M,Taglietti M,Fulle D,Pastoris O

    更新日期:1983-03-15 00:00:00

  • Anti-morphine anti-idiotypic antibodies. Opiate receptor binding and isolated tissue responses.

    abstract::Anti-idiotypic antibodies which recognize the opiate receptor were generated in guinea pigs following immunization against purified rabbit anti-morphine antibodies. The anti-idiotypic antibodies produced a concentration-dependent inhibition of [3H]naloxone binding to opiate receptors in a membranous mouse brain prepar...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ng DS,Isom GE

    更新日期:1985-08-15 00:00:00

  • Melatonin protects against methotrexate-induced memory deficit and hippocampal neurogenesis impairment in a rat model.

    abstract::Methotrexate (MTX) is a chemotherapy agent linked to cognitive deficits in cancer patients received chemotherapy treatment. MTX decreases cell proliferation in the hippocampus, which is concomitant with cognitive deficits in animal models. The present study aimed to investigate the disadvantages of MTX on cognition as...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sirichoat A,Krutsri S,Suwannakot K,Aranarochana A,Chaisawang P,Pannangrong W,Wigmore P,Welbat JU

    更新日期:2019-05-01 00:00:00

  • Reversal of antigen-dependent signaling by two mutations in antibody/receptor chimera: implication of inverse agonism in cytokine receptor superfamily.

    abstract::Understanding the receptor activation mechanism is essential for the rational design of pharmacologically active ligand molecules. However, the activation mechanism of most cytokine receptors remains still unclear, and while agonism and antagonism have been described for ligand-mimetic peptides, there has been no repo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kawahara M,Ishii S,Tsumoto K,Kumagai I,Ueda H,Nagamune T

    更新日期:2004-08-01 00:00:00

  • Vasoactive intestinal polypeptide does not affect thyroid follicular cell membrane potential or input resistance.

    abstract::It has been suggested that vasoactive intestinal polypeptide (VIP) has a role as a neurotransmitter and that it participates in the control of hormone release from thyroid follicles. Many hormones and neurotransmitters alter the ionic permeability properties of the plasma membrane of their target cells when they bind ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Green ST

    更新日期:1987-12-15 00:00:00

  • Induction in vitro and complete coding region sequence of cytochrome P4501A1 cDNA from cultured whole rat conceptuses during early organogenesis.

    abstract::Exposures of cultured whole rat conceptuses during organogenesis to 3-methylcholanthrene (MC; 0.025-25 microM), 5,6-benzoflavone (BNF; 5-100 microM) or benz[a]anthracene (BA; 5-100 microM) were effected by placement of each of these "MC-type" inducing agents in the culture medium at the time of explantation on day 9.5...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chapman DE,Yang HY,Watters JJ,Juchau MR

    更新日期:1994-11-01 00:00:00

  • Src-family kinase inhibitors block early steps of caveolin-1-enhanced lung metastasis by melanoma cells.

    abstract::In advanced stages of cancer disease, caveolin-1 (CAV1) expression increases and correlates with increased migratory and invasive capacity of the respective tumor cells. Previous findings from our laboratory revealed that specific ECM-integrin interactions and tyrosine-14 phosphorylation of CAV1 are required for CAV1-...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ortiz R,Díaz J,Díaz-Valdivia N,Martínez S,Simón L,Contreras P,Lobos-González L,Guerrero S,Leyton L,Quest AFG

    更新日期:2020-07-01 00:00:00

  • Genetic expression of aflatoxin metabolism. Effects of 3-methylcholanthrene and beta-naphthoflavone on hepatic microsomal metabolism and mutagenic activation of aflatoxins.

    abstract::The effects of pretreatment with 3-methylcholanthrene (MC) and beta-naphthoflavone (beta NF) on the hepatic microsome-mediated mutagenesis of aflatoxin B1 (AFB1) and benzo[a]pyrene, and on the metabolism of aflatoxins B1 and B2, were investigated in inbred mouse strains. The inbred strains of mice studied included Ah ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Raina V,Williams CJ,Gurtoo HL

    更新日期:1983-12-15 00:00:00

  • The effect of ifosfamide and its metabolites on intracellular glutathione levels in vitro and in vivo.

    abstract::The effect of ifosfamide and its metabolites on intracellular levels of glutathione in P388 cells in vitro has been studied. It is demonstrated that glutathione depletion occurs only in the presence of 4-hydroperoxyifosfamide and chloroacetaldehyde. In contrast isophosphoramide mustard had no effect on glutathione lev...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lind MJ,McGown AT,Hadfield JA,Thatcher N,Crowther D,Fox BW

    更新日期:1989-06-01 00:00:00

  • Drug metabolism in hepatocyte sandwich cultures of rats and humans.

    abstract::Adult hepatocytes from rat and man were maintained for 2 weeks between two gel layers in a sandwich configuration to study the influence of this culture technique on the preservation of basal activities of xenobiotic-metabolizing phase I and phase II enzymes. The response of these enzyme activities to an enzyme induce...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kern A,Bader A,Pichlmayr R,Sewing KF

    更新日期:1997-10-01 00:00:00

  • Entrectinib reverses cytostatic resistance through the inhibition of ABCB1 efflux transporter, but not the CYP3A4 drug-metabolizing enzyme.

    abstract::Entrectinib is a new tyrosine kinase inhibitor that was recently approved for the treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC). In this study, we aimed to characterize its potential to act as a modulator of pharmacokinetic cytostatic resistance and perpetrator of drug interactions. In accum...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Vagiannis D,Yu Z,Novotna E,Morell A,Hofman J

    更新日期:2020-08-01 00:00:00

  • The interactions of apamin and tetraethylammonium are differentially affected by single mutations in the pore mouth of small conductance calcium-activated potassium (SK) channels.

    abstract::Valine residues in the pore region of SK2 (V366) and SK3 (V520) were replaced by either an alanine or a phenylalanine to evaluate the impact on the interactions with the allosteric blocker apamin. Unlike TEA which showed high sensitivity to phenylalanine mutated channels, the binding affinity of apamin to the phenylal...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dilly S,Philippart F,Lamy C,Poncin S,Snyders D,Seutin V,Liégeois JF

    更新日期:2013-02-15 00:00:00

  • Covalent coupling of doxorubicin in protein microspheres is a major determinant of tumour drug disposition.

    abstract::Doxorubicin is shown to be present in albumin microspheres (10-40 microns) in two forms: the native drug and a fraction of drug covalently coupled to the protein matrix probably via glutaraldehyde. Upon trypsin digestion the fraction covalently coupled is released and can be resolved from native doxorubicin by high pe...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Cummings J,Willmott N,Marley E,Smyth J

    更新日期:1991-06-15 00:00:00

  • Production of adenosine and nucleoside analogs by the exchange reaction catalyzed by rat liver adenosine kinase.

    abstract::We have previously shown [8] that rat liver adenosine kinase can produce [14C]AMP from [14C]adenosine (Ado) and unlabelled adenosine monophosphate (AMP), in the absence of ATP, by an exchange reaction. In this study, we investigated whether Ado or AMP could be replaced in this exchange reaction by other nucleosides or...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mimouni M,Bontemps F,Van den Berghe G

    更新日期:1995-11-09 00:00:00

  • Testing double mutants of the enzyme nitroreductase for enhanced cell sensitisation to prodrugs: effects of combining beneficial single mutations.

    abstract::Prodrug activation gene therapy for cancer involves expressing prodrug-activating enzymes in tumour cells, so they can be selectively killed by systemically administered prodrug. For example, Escherichia colinfsB nitroreductase (E.C., sensitises cells to the prodrug CB1954 (5-[aziridin-1-yl]-2,4-dinitro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Jaberipour M,Vass SO,Guise CP,Grove JI,Knox RJ,Hu L,Hyde EI,Searle PF

    更新日期:2010-01-15 00:00:00