Abstract:
:Dural plasma extravasation produced by electrical stimulation of the trigeminal ganglion was measured in rats and the concomitant expression of c-fos mRNA produced in the trigeminal nucleus caudalis (NtV) was measured using in situ hybridization techniques. The non-peptide NK1 receptor selective antagonist CP-99,994 (1-3000 micrograms kg-1) and the 5HT1D receptor agonist sumatriptan (1-1000 micrograms kg-1) reduced dural plasma extravasation dose-dependently with ID50S of 52 micrograms kg-1 and 30 micrograms kg-1 respectively. CP-99,994 (1000 micrograms kg-1). a compound known to have good brain penetration, decreased c-fos mRNA expression in the NtV by 37 +/- 7% without disruption of the blood brain barrier (BBB). Sumatriptan (1000 micrograms kg-1), known to be poorly brain penetrant, had no significant effect on c-fos mRNA expression in the NtV unless the BBB was disrupted by infusion of a hyperosmolar mannitol solution after which sumatriptan decreased c-fos mRNA expression by 65 +/- 11%. The results suggest that brain penetrant NK1 receptor antagonists may have anti-migraine effects peripherally through blockade of dural extravasation and centrally by inhibition of nociceptive pathways. Furthermore the data indicates that the anti-migraine action of sumatriptan must be predominantly peripherally mediated, be it via inhibition of plasma extravasation or direct vasoconstriction, since it had little effect on the activation of neurones in the NtV unless the BBB was disrupted.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Shepheard SL,Williamson DJ,Williams J,Hill RG,Hargreaves RJdoi
10.1016/0028-3908(94)00153-jsubject
Has Abstractpub_date
1995-03-01 00:00:00pages
255-61issue
3eissn
0028-3908issn
1873-7064pii
002839089400153Jjournal_volume
34pub_type
杂志文章abstract::Opioids are thought to increase the excitability of hippocampal pyramidal cells by decreasing release of neurotransmitter from inhibitory interneurons. This study compared the actions of the opioid agonist normorphine, and the GABA receptor antagonist bicuculline, on the responses of CA1 pyramidal cells to afferent st...
journal_title:Neuropharmacology
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journal_title:Neuropharmacology
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journal_title:Neuropharmacology
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更新日期:2013-08-01 00:00:00
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journal_title:Neuropharmacology
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journal_title:Neuropharmacology
pub_type: 杂志文章
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journal_title:Neuropharmacology
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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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(84)90047-9
更新日期:1984-11-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.neuropharm.2016.03.024
更新日期:2017-01-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2010.06.008
更新日期:2010-11-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2020.108070
更新日期:2020-06-15 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(90)90090-e
更新日期:1990-04-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(97)00167-6
更新日期:1997-11-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2006.09.011
更新日期:2007-03-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(88)90077-9
更新日期:1988-07-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2016.10.010
更新日期:2017-02-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2020-03-15 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:1985-06-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(03)00202-8
更新日期:2003-09-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(87)90101-8
更新日期:1987-09-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2016.12.013
更新日期:2017-04-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2018.10.018
更新日期:2019-01-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2015.10.024
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/j.neuropharm.2017.09.006
更新日期:2017-11-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.neuropharm.2011.04.029
更新日期:2012-02-01 00:00:00
abstract::Thyroid hormone deficiency during early developmental stages causes a multitude of functional and morphological deficits in the brain. In the present study we investigate the effects of a mutated thyroid hormone receptor TR alpha 1 and the resulting receptor-mediated hypothyroidism on the development of GABAergic neur...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2010.02.005
更新日期:2010-06-01 00:00:00
abstract::4-Alkylated analogues of homoibotenic acid (HIBO) have previously shown high potency and selectivity at ionotropic and metabotropic glutamic acid receptor (iGluR and mGluR) subtypes. Compounds with different selectivity profiles are valuable pharmacological tools for neuropharmacological studies, and the series of 4-a...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2005.05.007
更新日期:2005-01-01 00:00:00
abstract::The metabotropic glutamate receptor 2 (mGlu2) plays an important role in the presynaptic control of glutamate release and several mGlu2 positive allosteric modulators (PAMs) have been under assessment for their potential as antipsychotics. The binding mode of mGlu2 PAMs is better characterized in functional terms whil...
journal_title:Neuropharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.neuropharm.2016.08.040
更新日期:2017-03-15 00:00:00