Abstract：
:The effects of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ), an alkylating agent producing irreversible blockade of various membrane bound receptors in brain, were investigated on four different types of serotonin receptors, 5-HT1A, 5-HT1B, 5-HT2A and 5-HT3, in various brain regions in the rat. In addition, the fate of central benzodiazepine- and "R"-zacopride-specific binding sites was also examined in rats treated with EEDQ. Membrane binding assays and/or quantitative autoradiography with appropriate radioligands indicated that EEDQ inactivated 5-HT1A, 5-HT1B and 5-HT2A sites, but was poorly active on 5-HT3, benzodiazepine and "R" sites. Among the receptors affected by EEDQ, hippocampal 5-HT1A sites were the most sensitive to the alkylating agent (ID50 approximately 1 mg/kg i.p.), followed by the cortical 5-HT2A (ID50 approximately 3 mg/kg i.p.) and the striatal 5-HT1B (ID50 approximately 6 mg/kg i.p.) sites. Pretreatment by selective ligands partially protected hippocampal 5-HT1A sites from irreversible inactivation by EEDQ (10 mg/kg i.p.) with the following order of efficacy: WAY 100635 > spiperone > BMY 7378 > ipsapirone. Similarly, pretreatment by spiperone (5 mg/kg i.p.) also reduced the ability of EEDQ to inactivated cortical 5-HT2A receptors. Analyses of the time-course recovery of respective binding sites after EEDQ administration showed that the turnover rate of 5-HT1A sites did not significantly differ in the dorsal raphe nucleus and in various forebrain areas (hippocampus, septum, cerebral cortex; half-life: approximately 4 days), but was lower than that of cortical 5-HT2A sites (half-life: 2.9 days).
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Gozlan H,Laporte AM,Thibault S,Schechter LE,Bolaños F,Hamon Mdoi
10.1016/0028-3908(94)90072-8subject
Has Abstractpub_date
1994-03-01 00:00:00pages
423-31issue
3-4eissn
0028-3908issn
1873-7064journal_volume
33pub_type
杂志文章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
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更新日期：1985-11-01 00:00:00
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journal_title：Neuropharmacology
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(96)00010-x
更新日期：1996-04-01 00:00:00
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pub_type： 杂志文章
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doi：10.1016/0028-3908(82)90053-3
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：1997-04-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：1993-11-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2003.11.031
更新日期：2004-05-01 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：2020-06-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2014.02.019
更新日期：2014-07-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(01)00134-4
更新日期：2001-11-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.02.007
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.2014.07.019
更新日期：2015-01-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2016.07.033
更新日期：2016-11-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2014.12.007
更新日期：2015-07-01 00:00:00
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journal_title：Neuropharmacology
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doi：10.1016/j.neuropharm.2007.07.009
更新日期：2007-10-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2017.01.022
更新日期：2017-05-01 00:00:00
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journal_title：Neuropharmacology
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更新日期：2017-04-01 00:00:00
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journal_title：Neuropharmacology
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journal_title：Neuropharmacology
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更新日期：2004-11-01 00:00:00
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journal_title：Neuropharmacology
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更新日期：2017-02-01 00:00:00
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更新日期：2019-10-01 00:00:00
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journal_title：Neuropharmacology
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doi：10.1016/j.neuropharm.2014.11.027
更新日期：2015-04-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：2017-02-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(91)90203-n
更新日期：1991-02-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(94)90188-0
更新日期：1994-07-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2017.11.041
更新日期：2018-03-01 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：2012-02-01 00:00:00
