Abstract：
:Non-peptide antagonists of the NK1 and NK2 receptors were tested as inhibitors of the reaction time in the rat tail-flick and on the decrease of reaction time induced by the intrathecal injection of the NK1 receptor selective agonist [Sar9,Met(O2)11]SP or of the NK2 selective agonist NKA-(4-10). The decrease in reaction time produced by the NK1 agonist lasted less than 11 min while that evoked by the NK2 agonist persisted 26 min after injection. When given intrathecally, CP-96,345 and its chloro analog, Cl-CP, blocked dose-dependently both the behavioral responses and the decreases of reaction time induced by 6.5 nmol of [Sar9,Met(O2)11]SP while they failed to modify the hyperalgesic response to 6.5 nmol NKA-(4-10); CP-96,345 was found more potent than Cl-CP and was also active as an antagonist when given intravenously. In contrast, SR 48968 (6.5 and 65 nmol) blocked the NKA-(4-10)-induced decreases in reaction time and was inactive against the hyperalgesic effect of [Sar9,Met(O2)11]SP. The three antagonists blocked in a reversible manner, were inactive on their own on reaction time and non-toxic. The results indicate that the non-peptide CP-96,345 readily crosses the blood brain barrier and acts as a selective antagonist on spinal NK1 receptors, while SR 48968 is selective on NK2 receptors in the rat spinal cord. Hence, CP-96,345 and SR 48968 highlight a functional role of NK1 and NK2 receptors in spinal sensory neurotransmission.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Picard P,Boucher S,Regoli D,Gitter BD,Howbert JJ,Couture Rdoi
10.1016/0014-2999(93)90782-dsubject
Has Abstractpub_date
1993-03-02 00:00:00pages
255-61issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(93)90782-Djournal_volume
232pub_type
杂志文章abstract：:The relationship between isometric tension and the increase in cyclic GMP level associated with the initial phase of drug-induced contraction of taenia coli was studied. Maximal contraction induced by 100 micrometers carbachol or 124 mM KCl occurred in 30 sec and was associated with an increase in cyclic GMP levels of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1981-03-12 00:00:00
abstract：:The study concerned the effect of arachidonic acid metabolites on the inflammatory reaction in granulation tissue of open wounds in rats. Metabolites or inhibitors were applied in a wound chamber attached to circular, open, full-thickness skin wounds 5 days post-wounding. The adjacent wound served as control. Blood fl...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1998-06-12 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00354-8
更新日期：1996-07-25 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00114-z
更新日期：1995-05-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1986-01-14 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1998-10-23 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90681-x
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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更新日期：2012-06-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1989-05-02 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1994-03-11 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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更新日期：2001-10-19 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90104-p
更新日期：1991-11-13 00:00:00
abstract：:Anandamide (AEA), an endogenous cannabinoid and vanilloid receptor ligand, possesses anti-inflammatory properties. Transport of AEA through cytoplasm is facilitated by heat shock protein (HSP) Hsp70, which enhances the rate of cellular AEA uptake, possibly via direct interactions. In lungs, increased HSP expression is...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.06.045
更新日期：2011-10-01 00:00:00
