Effect of organochlorine insecticides on nicotinic acetylcholine receptor-rich membranes.

Abstract:

:The so-called generalized polarization (GP) of the fluorescent probe Laurdan and the steady-state fluorescence anisotropy of the probe diphenylhexatriene (DPH) and its phenylpropionic derivative (PA-DPH) were used to study the effects of several organochlorine insecticides of the chlorophenylethane, chlorinated cyclohexane and chlorinated cyclodiene families on the Torpedo nicotinic acetylcholine receptor (AChR)-rich native membrane. All insecticides, with the exception of Lindane, augmented Laurdan GP both in the native membrane and in model lipid systems. Most organochlorine compounds produced a concentration-dependent decrease of DPH and PA-DPH anisotropy in the AChR-rich membrane. These compounds exhibited a dual behavior vis-à-vis the native AChR-rich membrane, exerting disordering effects at the bilayer core while ordering and/or excluding water molecules from the lipid-protein interface region, as sensed by DPH anisotropy and Laurdan GP, respectively. Furthermore, all insecticides decreased the efficiency of fluorescence resonance energy transfer between the intrinsic protein and Laurdan, albeit to different extents. On the basis of all these observations, the existence of potential target sites for insecticides in the protein-lipid interface region is postulated.

journal_name

Neuropharmacology

journal_title

Neuropharmacology

authors

Massol RH,Antollini SS,Barrantes FJ

doi

10.1016/s0028-3908(99)00194-x

subject

Has Abstract

pub_date

2000-04-03 00:00:00

pages

1095-106

issue

6

eissn

0028-3908

issn

1873-7064

pii

S002839089900194X

journal_volume

39

pub_type

杂志文章
  • An increase in tryptophan in brain may be a general mechanism for the effect of stress on sensitivity to pain.

    abstract::The role of the stress-induced increase in the uptake of tryptophan in brain in opioid-induced analgesia was investigated by modifying the uptake of amino acid in brain with injections of competing amino acids. Blockade of analgesia by valine (200 mg/kg, i.p.) alone, and by valine and tyrosine (100 mg/kg, i.p.), but n...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(85)90185-6

    authors: Kelly SJ,Franklin KB

    更新日期:1985-11-01 00:00:00

  • Dysregulation and restoration of homeostatic network plasticity in fragile X syndrome mice.

    abstract::Chronic activity perturbations in neurons induce homeostatic plasticity through modulation of synaptic strength or other intrinsic properties to maintain the correct physiological range of excitability. Although similar plasticity can also occur at the population level, what molecular mechanisms are involved remain un...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2018.06.011

    authors: Jewett KA,Lee KY,Eagleman DE,Soriano S,Tsai NP

    更新日期:2018-08-01 00:00:00

  • Effects of gamma-aminobutyric acid and glycine on synaptic excitability of neurones in the solitary tract nucleus.

    abstract::In the solitary tract nucleus, neuronal responsiveness to synaptic input from peripheral afferent fibres has been found to decrease as the frequency of that input is increased. The present study investigated the possibility that glycine and gamma-aminobutyric acid (GABA) are (1) involved in this phenomenon of "frequen...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(91)90149-6

    authors: Feldman PD,Felder RB

    更新日期:1991-03-01 00:00:00

  • Effects of behaviorally active doses of thyrotropin-releasing hormone and its analog MK-771 on dopaminergic neuronal systems in the brain of the rat.

    abstract::The effects of thyrotropin-releasing hormone (TRH) and an analog of this hormone, MK-771, were determined on body shaking behavior and on biochemical estimates of the activity of dopamine (DA) neurons in the rat. Both compounds elicited dose-related episodes of "wet-dog shakes". A dose of TRH (20 mg/kg, i.p.) which ca...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(84)90105-9

    authors: Yamada K,Demarest KT,Moore KE

    更新日期:1984-07-01 00:00:00

  • Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas.

    abstract::Selective inhibitors of the glycine transporter 1 (GlyT1) have been implicated in central nervous system disorders related to hypoglutamatergic function such as schizophrenia. The selective GlyT1 inhibitors ALX5407 (NFPS) and LY2365109 {[2-(4-benzo[1,3]dioxol-5-yl-2-tert-butylphenoxy)ethyl]-methylamino}-acetic acid in...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2008.06.016

    authors: Perry KW,Falcone JF,Fell MJ,Ryder JW,Yu H,Love PL,Katner J,Gordon KD,Wade MR,Man T,Nomikos GG,Phebus LA,Cauvin AJ,Johnson KW,Jones CK,Hoffmann BJ,Sandusky GE,Walter MW,Porter WJ,Yang L,Merchant KM,Shannon HE,S

    更新日期:2008-10-01 00:00:00

  • Rats are the smart choice: Rationale for a renewed focus on rats in behavioral genetics.

    abstract::Due in part to their rich behavioral repertoire rats have been widely used in behavioral studies of drug abuse-related traits for decades. However, the mouse became the model of choice for researchers exploring the genetic underpinnings of addiction after the first mouse study was published demonstrating the capabilit...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2013.05.047

    authors: Parker CC,Chen H,Flagel SB,Geurts AM,Richards JB,Robinson TE,Solberg Woods LC,Palmer AA

    更新日期:2014-01-01 00:00:00

  • Memantine is a clinically well tolerated N-methyl-D-aspartate (NMDA) receptor antagonist--a review of preclinical data.

    abstract::N-methyl-D-aspartate (NMDA) receptor antagonists have therapeutic potential in numerous CNS disorders ranging from acute neurodegeneration (e.g. stroke and trauma), chronic neurodegeneration (e.g. Parkinson's disease, Alzheimer's disease, Huntington's disease, ALS) to symptomatic treatment (e.g. epilepsy, Parkinson's ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0028-3908(99)00019-2

    authors: Parsons CG,Danysz W,Quack G

    更新日期:1999-06-01 00:00:00

  • Modulation of release of acetylcholine from the striatum by a proposed excitatory amino acid antagonist U-54494A: comparison with known antagonists, diazepam and phenytoin.

    abstract::The effect of (U-54494A) cis-3,4-dichloro-N-methyl-N-[2-(1-Pyrrolidinyl)- cyclohexyl] benzamide monohydrochloride, an excitatory amino acid antagonist, on N-methyl-D-aspartic acid (NMDA)- and K(+)-evoked release of [3H]acetylcholine [( 3H]ACh) from slices of striatum was investigated. For the purpose of comparison, MK...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(92)90019-l

    authors: Sethy VH,Sage GP

    更新日期:1992-02-01 00:00:00

  • Potential antidepressant activity of rolipram and other selective cyclic adenosine 3',5'-monophosphate phosphodiesterase inhibitors.

    abstract::Following intraperitoneal administration, the selective cAMP phosphodiesterase (PDE) inhibitors rolipram, ICI 63 197 and Ro 20-1724 were investigated in mice in comparison with imipramine for their effectiveness in two classical test models for prediction of clinical antidepressant activity: antagonism of reserpine-in...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(83)90239-3

    authors: Wachtel H

    更新日期:1983-03-01 00:00:00

  • The effects of analgesics on quickly-learned conditioned suppression in mice.

    abstract::Mice were found to exhibit a marked suppression of motor activity when placed into the same experimental chamber in which they had previously received electrical shocks. This suppression was found to be a stable response when mice, 6-8 weeks of age, received shocks of frequencies of 1/10 or 1/30 Hz, and their motility...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(82)90134-4

    authors: Kameyama T,Nagasaka M

    更新日期:1982-12-01 00:00:00

  • Cannabinoid CB(1) receptor activation stimulates neurite outgrowth and inhibits capsaicin-induced Ca(2+) influx in an in vitro model of diabetic neuropathy.

    abstract::Cannabinoid CB(1) receptors mediate, in part, the neuroprotectant properties of endocannabinoids, and altered signalling via the CB(1) receptor may contribute to the pathogenesis of diabetic neuropathy. We investigated CB(1) receptor function in PC12 cells differentiated into a neuronal phenotype with nerve growth fac...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2009.04.017

    authors: Zhang F,Challapalli SC,Smith PJ

    更新日期:2009-08-01 00:00:00

  • Caffeine and muscarinic antagonists act in synergy to inhibit haloperidol-induced catalepsy.

    abstract::The possible synergism between caffeine and muscarinic antagonists to inhibit haloperidol-induced catalepsy was investigated with the bar test in rats. Pretreatment with low doses of caffeine (1-3 mg/kg), a non-selective adenosine antagonist, dose dependently reduced the intensity and increased the onset latency of ca...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(03)00202-8

    authors: Moo-Puc RE,Góngora-Alfaro JL,Alvarez-Cervera FJ,Pineda JC,Arankowsky-Sandoval G,Heredia-López F

    更新日期:2003-09-01 00:00:00

  • Depletion of noradrenaline in the hypothalamus reduces the febrile responses induced by prostaglandin E2, thyrotropin-releasing hormone and beta-endorphin in rats.

    abstract::The effects of pretreatment of rats with an intrahypothalamic injection of 6-hydroxydopamine on the thermal responses induced by intrahypothalamic injection of noradrenaline, prostaglandin E2, thyrotropin-releasing hormone or beta-endorphin were assessed. Administration of either noradrenaline (2-10 micrograms), prost...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(85)90188-1

    authors: Lin MT,Chern YF,Chen SY

    更新日期:1985-11-01 00:00:00

  • Selective regulation of recombinantly expressed mGlu7 metabotropic glutamate receptors by G protein-coupled receptor kinases and arrestins.

    abstract::mGlu7 receptors are coupled to Gi/Go-proteins and activate multiple transduction pathways, including inhibition of adenylyl cyclase activity and stimulation of ERK1/2 and JNK pathways. mGlu7 receptors play an important role in cognition and emotion and are involved in stress-related disorders such as anxiety and depre...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2013.10.013

    authors: Iacovelli L,Felicioni M,Nisticò R,Nicoletti F,De Blasi A

    更新日期:2014-02-01 00:00:00

  • Characterisation of an mGlu8 receptor-selective agonist and antagonist in the lateral and medial perforant path inputs to the dentate gyrus.

    abstract::Since its characterisation in 2001, the mGlu8-selective agonist DCPG has been widely used to explore the potential functional role of this group III mGlu receptor within the central nervous system. This research has implicated mGlu8 receptors in a number of disease states and conditions such as epilepsy and anxiety, s...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2012.11.020

    authors: Mercier MS,Lodge D,Fang G,Nicolas CS,Collett VJ,Jane DE,Collingridge GL,Bortolotto ZA

    更新日期:2013-04-01 00:00:00

  • The anthelmintic pyrantel acts as a low efficacious agonist and an open-channel blocker of mammalian acetylcholine receptors.

    abstract::Pyrantel is an anthelmintic which acts as an agonist of nicotinic receptors (AChRs) of nematodes and exerts its therapeutic effects by depolarizing their muscle membranes. Here we explore at the single-channel level the action of pyrantel at mammalian muscle AChR. AChR currents are elicited by pyrantel. However, openi...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(01)00057-0

    authors: Rayes D,De Rosa MJ,Spitzmaul G,Bouzat C

    更新日期:2001-08-01 00:00:00

  • GRP receptor and AMPA receptor cooperatively regulate itch-responsive neurons in the spinal dorsal horn.

    abstract::Gastrin-releasing peptide (GRP) receptor-expressing (GRPR)+ neurons have a central role in the spinal transmission of itch. Because their fundamental regulatory mechanisms are not yet understood, it is important to determine how such neurons are excited and integrate itch sensation. In this study, we investigated the ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2020.108025

    authors: Kiguchi N,Uta D,Ding H,Uchida H,Saika F,Matsuzaki S,Fukazawa Y,Abe M,Sakimura K,Ko MC,Kishioka S

    更新日期:2020-06-15 00:00:00

  • Coupling to protein kinases A and C of adenosine A2B receptors involved in the facilitation of noradrenaline release in the prostatic portion of rat vas deferens.

    abstract::In the prostatic portion of rat vas deferens, the non-selective adenosine receptor agonist NECA (0.1-30 microM), but not the A(2A) agonist CGS 21680 (0.001-10 microM), caused a facilitation of electrically evoked noradrenaline release (up to 43 +/- 4%), when inhibitory adenosine A(1) receptors were blocked. NECA-elici...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2004.03.015

    authors: Queiroz G,Quintas C,Talaia C,Gonçalves J

    更新日期:2004-08-01 00:00:00

  • TSPO activation modulates the effects of high pressure in a rat ex vivo glaucoma model.

    abstract::We previously reported that elevated pressure induces axonal swelling and facilitates the synthesis of the neurosteroid, allopregnanolone (AlloP), in the ex vivo rat retina. Exogenously applied AlloP attenuates the axonal swelling, suggesting that the neurosteroid plays a neuroprotective role against glaucomatous pres...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2016.09.001

    authors: Ishikawa M,Yoshitomi T,Covey DF,Zorumski CF,Izumi Y

    更新日期:2016-12-01 00:00:00

  • In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.

    abstract::The demonstrated functional interaction of metabotropic glutamate 5 (mGlu₅) receptors with N-methyl-d-aspartate (NMDA) receptors has prompted speculation that their activation may offer a potential treatment for aspects of schizophrenia. Development of selective mGlu₅ agonists has been difficult, but several different...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2012.07.030

    authors: Gilmour G,Broad LM,Wafford KA,Britton T,Colvin EM,Fivush A,Gastambide F,Getman B,Heinz BA,McCarthy AP,Prieto L,Shanks E,Smith JW,Taboada L,Edgar DM,Tricklebank MD

    更新日期:2013-01-01 00:00:00

  • Adaptive changes in the 5-HT2 binding site after chronic administration of agonists and antagonists.

    abstract::This study confirms and extends an earlier report that acute administration of the serotonin (5-HT) antagonist, mianserin, caused a marked decrease in the density of 5-HT2 binding sites in brain of the rat (Blackshear and Sanders-Bush, 1982). Using [3H]ketanserin, a selective ligand for the 5-HT2 site, the present stu...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(86)90146-2

    authors: Blackshear MA,Martin LL,Sanders-Bush E

    更新日期:1986-11-01 00:00:00

  • Neuronal oscillations: A physiological correlate for targeting mitochondrial dysfunction in neurodegenerative diseases?

    abstract::Increasingly in the realm of neurological disorders, particularly those involving neurodegeneration, mitochondrial dysfunction is emerging at the core of their pathogenic processes. Most of these diseases still lack effective treatment and are hampered by a shortfall in the development of novel medicines. Clearly new ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2015.10.033

    authors: Chan F,Lax NZ,Davies CH,Turnbull DM,Cunningham MO

    更新日期:2016-03-01 00:00:00

  • Non-invasive brain stimulation in neurological diseases.

    abstract::Non-invasive brain stimulation has shown its potential to modulate brain plasticity in humans. Endeavour has been made to utilize brain stimulation in neurological diseases to enhance adaptive processes and prevent potential maladaptive ones. In stroke for instance both sensorimotor and higher cognitive impairment, su...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2012.05.016

    authors: Schulz R,Gerloff C,Hummel FC

    更新日期:2013-01-01 00:00:00

  • Blood pressure and heart rate responses to microinjection of vasopressin into the nucleus tractus solitarius region of the rat.

    abstract::The nucleus tractus solitarius (NTS) region in the rat has been shown to receive arginine vasopressin (AVP) and oxytocin (OT) neurophysin-containing neuronal projections from the suprachiasmatic (SNC) and paraventricular nucleus (PVN). Thus, vasopressin and oxytocin might have central influences on the circulation. Th...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(82)90012-0

    authors: Matsuguchi H,Sharabi FM,Gordon FJ,Johnson AK,Schmid PG

    更新日期:1982-07-01 00:00:00

  • Nicotinic receptors in non-human primates: Analysis of genetic and functional conservation with humans.

    abstract::Nicotinic acetylcholine receptors (nAChRs) are highly conserved between humans and non-human primates. Conservation exists at the level of genomic structure, protein structure and epigenetics. Overall homology of nAChRs at the protein level is 98% in macaques versus 89% in mice, which is highly relevant for evaluating...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2015.01.023

    authors: Shorey-Kendrick LE,Ford MM,Allen DC,Kuryatov A,Lindstrom J,Wilhelm L,Grant KA,Spindel ER

    更新日期:2015-09-01 00:00:00

  • Subtype-selective nicotinic acetylcholine receptor agonists can improve cognitive flexibility in an attentional set shifting task.

    abstract::Nicotinic acetylcholine receptors (nAChRs) are considered to be viable targets to enhance cognition in patients diagnosed with schizophrenia. Activation of nAChRs with selective nicotinic receptor agonists may provide effective means to pharmacologically treat cognitive deficits observed in schizophrenia. Cognitive fl...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2016.01.006

    authors: Wood C,Kohli S,Malcolm E,Allison C,Shoaib M

    更新日期:2016-06-01 00:00:00

  • Agonist activation of a nicotinic acetylcholine receptor.

    abstract::How does an agonist activate a receptor? In this article I consider the activation process in muscle nicotinic acetylcholine receptors (AChRs), a prototype for understanding the energetics of binding and gating in other ligand-gated ion channels. Just as movements that generate gating currents activate voltage-gated i...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2014.10.004

    authors: Auerbach A

    更新日期:2015-09-01 00:00:00

  • Biomarkers in translational research of Alzheimer's disease.

    abstract::The identification and characterization of amyloid-beta (Abeta) and tau as the main pathological substrates of Alzheimer's disease (AD) have driven many efforts in search for suitable biomarkers for AD. In the last decade, research in this area has focused on developing a better understanding of the principles that go...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2010.04.006

    authors: Tarawneh R,Holtzman DM

    更新日期:2010-09-01 00:00:00

  • Muscarinic receptor subtype distribution in the central nervous system and relevance to aging and Alzheimer's disease.

    abstract::Muscarinic acetylcholine receptors (mAChRs) are G proteincoupled receptors (GPCRs) that mediate the metabotropic actions of acetylcholine (ACh). There are five subtypes of mAChR, M1 - M5, which are expressed throughout the central nervous system (CNS) on numerous cell types and represent promising treatment targets fo...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2017.11.018

    authors: Lebois EP,Thorn C,Edgerton JR,Popiolek M,Xi S

    更新日期:2018-07-01 00:00:00

  • Brainstem prolactin-releasing peptide contributes to cancer anorexia-cachexia syndrome in rats.

    abstract::Up to 80% of cancer patients are affected by the cancer anorexia-cachexia syndrome (CACS), which leads to excessive body weight loss, reduced treatment success and increased lethality. The area postrema/nucleus of the solitary tract (AP/NTS) region emerged as a central nervous key structure in this multi-factorial pro...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2020.108289

    authors: Navarro I Batista K,Schraner M,Riediger T

    更新日期:2020-12-01 00:00:00