Abstract:
:Heterogeneous binding interactions of cerebellar GABA(A) receptors were investigated with GABA agonists and neurosteroids. GABA(A) receptors of rat cerebellum were labelled with [(3)H]ethynylbicycloorthobenzoate (EBOB), a convulsant radioligand. Saturation analysis revealed a homogenous, nanomolar population of [(3)H]EBOB binding. Both GABA and 5alpha-tetrahydrodeoxycorticosterone (5alpha-THDOC) displaced [(3)H]EBOB binding heterogeneously, with nanomolar and micromolar potencies. The nanomolar phase of displacement by GABA was selectively abolished by 100 microM furosemide. Physiological concentrations of allopregnanolone (8 nM) and 5alpha-THDOC (20 nM) increased the displacing effects of nanomolar GABA. GABA (0.3 microM ) and 5alpha-THDOC (0.3 microM ) potentiated the micromolar population of displacement by the other. Taurine inhibited [(3)H]EBOB binding also heterogeneously, with micromolar and millimolar potencies, and 0.3 microM 5alpha-THDOC potentiated this inhibition. 5beta-THDOC did not affect [(3)H]EBOB binding significantly but in 1 microM it antagonised selectively the nanomolar displacement by 5alpha-THDOC. [(3)H]EBOB binding to hippocampal GABA(A) receptors was inhibited by GABA and allopregnanolone with low (micromolar) potencies and with slope values higher than unity referring to allosteric interaction. High affinity displacement of cerebellar [(3)H]EBOB binding by GABA agonists and neurosteroids can be associated with constitutively open alpha(6)betadelta GABA(A) receptors, tonic GABAergic inhibitory neurotransmission and its modulation by physiological concentrations of neurosteroids.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Maksay G,Bíró Tdoi
10.1016/j.neuropharm.2005.04.003subject
Has Abstractpub_date
2005-09-01 00:00:00pages
431-8issue
4eissn
0028-3908issn
1873-7064pii
S0028-3908(05)00142-5journal_volume
49pub_type
杂志文章abstract::Purine nucleotides, such as ATP and ADP, activate ionotropic P2X and metabotropic P2Y receptors to regulate neurotransmitter release in the peripheral as well as central nervous system. Here we report another type of ATP-induced presynaptic modulation of glutamate release in rat medullary dorsal horn neurons. Glutamat...
journal_title:Neuropharmacology
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abstract::The mechanisms underlying improvement of neuromuscular transmission deficits by glucocorticoids are still a matter of debate despite these compounds have been used for decades in the treatment of autoimmune myasthenic syndromes. Besides their immunosuppressive action, corticosteroids may directly facilitate transmitte...
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abstract::D-Tubocurarine is a potent competitive antagonist of two members of the ligand-gated ion channel family, the muscle-type nicotinic acetylcholine receptor (AChR) and serotonin type-3 receptor (5HT3R). We have used a series of analogs of D-tubocurarine to determine the effects of methylation, stereoisomerization and hal...
journal_title:Neuropharmacology
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更新日期:1998-01-01 00:00:00
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journal_title:Neuropharmacology
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doi:10.1016/j.neuropharm.2004.03.001
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abstract::Gliomas are the leading cause of cancer-related mortality worldwide, and the incidence is increasing. Because gliomas often become resistant to radiation treatment, it is urgent to develop novel therapeutic methods that are more effective and less toxic than current therapies so as to enhance patient survival and qual...
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.neuropharm.2011.04.029
更新日期:2012-02-01 00:00:00
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更新日期:1985-01-01 00:00:00
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journal_title:Neuropharmacology
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更新日期:1991-12-01 00:00:00
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pub_type: 杂志文章
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pub_type: 杂志文章
doi:10.1016/0028-3908(84)90012-1
更新日期:1984-08-01 00:00:00
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journal_title:Neuropharmacology
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更新日期:2018-09-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(85)90073-5
更新日期:1985-03-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2013.03.013
更新日期:2013-08-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(89)90032-4
更新日期:1989-04-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2015.09.003
更新日期:2016-02-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(84)90231-4
更新日期:1984-10-01 00:00:00
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abstract::The majority of existing research on the function of metabotropic glutamate (mGlu) receptor 1 focuses on G protein-mediated outcomes. However, similar to other G protein-coupled receptors (GPCR), it is becoming apparent that mGlu1 receptor signaling is multi-dimensional and does not always involve G protein activation...
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pub_type: 杂志文章
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更新日期:2013-04-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:1990-03-01 00:00:00
abstract::About 20-30% of patients with epilepsy continue to have seizures despite carefully monitored treatment with antiepileptic drugs. The mechanisms explaining why some patients' respond and others prove resistant to antiepileptic drugs are poorly understood. It has been proposed that pharmacoresistance is related to reduc...
journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2002-01-01 00:00:00
abstract::The present experiments investigated the ability of LY392098, a novel positive allosteric modulator of AMPA receptors, to potentiate AMPA receptor-mediated currents of neurons in the prefrontal cortex (PFC). Co-application of LY392098 (0.03-10 microM) with AMPA (5 microM) enhanced current through AMPA receptor/channel...
journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2001-06-01 00:00:00
abstract::The homotrimeric P2X3 receptor, one of the seven members of the ATP-gated P2X receptor family, plays a crucial role in sensory neurotransmission. P2X3 receptor antagonists have been identified as promising drugs to treat chronic cough and are suggested to offer pain relief in chronic pain such as neuropathic pain. Her...
journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2019-11-01 00:00:00