Abstract：
:The effects of the glutamate receptor antagonist gamma-D-glutamylaminomethyl sulfonic acid (GAMS) on inward currents induced by bath application of kainic acid (KA) or alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) were studied with single-electrode voltage clamp methods in Xenopus oocytes injected 3-5 days previously with mRNA from the brain of E16-17 chick embryos. Both AMPA and KA induced smooth inward currents, with Hill coefficients of 1.5 (AMPA) and 2.1 (KA). GAMS, at concentrations up to 1 mM, produced no reliable antagonism of AMPA-induced currents but showed a consistent, dose-dependent and reversible antagonism of KA-induced responses; the slope of the Schild plot was 0.76 and the pA2 value 4.32. In the presence of GAMS, however, the Hill coefficient for AMPA is reduced significantly and approaches unity, suggesting that AMPA interacts with both KA and AMPA binding sites on chick brain glutamate receptors. The selectivities of three quinoxalinedione antagonists (6,7-dinitroquinoxaline-2,3-dione [DNQX], 6-cyano-7- nitroquinoxaline-2,3-dione [CNQX] and 6-nitro-7-sulfamoyl-benzo(F)quinoxaline-2,3-dione [NBQX]) were then compared with that shown by GAMS. DNQX, CNQX and NBQX all blocked the effects of both KA and AMPA completely, competitively, reversibly and dose-dependently, with Schild-plot slopes very close to 1.0. Against AMPA, observed pA2 values were 6.58 for DNQX, 6.43 for CNQX and 6.77 for NBQX. Against KA, pA2 values were 6.42 for DNQX, 6.56 for CNQX and 7.21 for NBQX.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Zhou N,Hammerland LG,Parks TNdoi
10.1016/0028-3908(93)90185-6subject
Has Abstractpub_date
1993-08-01 00:00:00pages
767-75issue
8eissn
0028-3908issn
1873-7064journal_volume
32pub_type
杂志文章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
更新日期：2009-08-01 00:00:00
abstract：:In the rat subthalamic nucleus, which plays a critical role in the control of motor behaviour, specific binding of [3H]-prazosin was detected by radioligand binding to homogenates and by autoradiography in slices. [3H]-Prazosin binding to homogenates (Bmax 71 +/- 5 fmol/mg protein; Kd 0.27 +/- 0.05 nM) was competed fo...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(03)00315-0
更新日期：2003-12-01 00:00:00
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journal_title：Neuropharmacology
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journal_title：Neuropharmacology
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abstract：:Acute morphine administration produces analgesia and reward, but prolonged use may lead to analgesic tolerance in patients chronically treated for pain and to compulsive intake in opioid addicts. Moreover, long-term exposure may induce physical dependence, manifested as somatic withdrawal symptoms in the absence of th...
journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：2008-03-01 00:00:00
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pub_type： 杂志文章
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journal_title：Neuropharmacology
pub_type： 杂志文章,评审
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更新日期：2014-06-01 00:00:00
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journal_title：Neuropharmacology
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更新日期：2018-07-15 00:00:00
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pub_type： 杂志文章
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更新日期：1994-06-01 00:00:00
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更新日期：2002-07-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章,评审
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更新日期：2013-01-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(03)00041-8
更新日期：2003-04-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(90)90138-h
更新日期：1990-10-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.01.020
更新日期：2015-06-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2016.01.030
更新日期：2016-06-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2008.01.007
更新日期：2008-04-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章,评审
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(83)90258-7
更新日期：1983-01-01 00:00:00
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journal_title：Neuropharmacology
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.05.025
更新日期：2013-03-01 00:00:00
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journal_title：Neuropharmacology
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更新日期：2018-12-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2009.06.014
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.02.014
更新日期：2013-07-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2007.03.015
更新日期：2007-06-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章,评审
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更新日期：2010-05-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：2017-03-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(89)90069-5
更新日期：1989-01-01 00:00:00
abstract：:The effects of nefiracetam on GABA-induced chloride currents were studied with rat dorsal root ganglion neurons in primary culture using the whole-cell patch-clamp technique. The dose-response curve for GABA-induced currents was shifted by 16 microM to lower concentrations by 10 microM nefiracetam while the maximal re...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(96)00074-3
更新日期：1996-01-01 00:00:00
abstract：:Anti-emetic drugs such as the tachykinin NK(1) receptor antagonists are useful to control emesis induced by diverse challenges. Evidence suggests pungent capsaicin-like TRPV1 activators also have broad inhibitory anti-emetic activity. However, pungent compounds are associated with undesirable effects including adverse...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2009.10.002
更新日期：2010-02-01 00:00:00
abstract：:The impairment of social behaviors induced by social defeat stress exposure as juveniles is resistant to some antidepressants and an antipsychotic, although the underlying mechanisms and/or therapeutic target are not yet clear. In this study, we investigated the involvement of the glutamatergic neuronal system in the ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2018.12.020
更新日期：2019-04-01 00:00:00
