Source:http://linkedlifedata.com/resource/pubmed/id/15942125
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2005-6-20
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pubmed:abstractText |
The effect of loperamide on tachykinin NK(2)- and NK(3)-receptor-mediated 5-HT outflow from guinea pig colonic mucosa was investigated in vitro. The selective tachykinin NK(2)-receptor agonist [beta-Ala(8)]-neurokinin A(4-10) (betaAla-NKA) or the selective NK(3)-receptor agonist senktide elicited an increase in 5-HT outflow from whole colonic strips, but not from mucosa-free muscle layer preparations. The enhancing effect of betaAla-NKA and senktide was prevented by the selective NK(2)-receptor antagonist GR94800 or the selective NK(3)-receptor antagonist SB222200. Loperamide concentration-dependently suppressed the senktide-evoked 5-HT outflow, but failed to affect the betaAla-NKA-evoked 5-HT outflow. The kappa-opioid receptor antagonist nor-binaltorphimine or the delta-opioid receptor antagonist naltrindole displaced the concentration-response curve for the suppressant action of loperamide to the right without significant depression of the maximum. However, the mu-opioid receptor antagonist CTOP did not affect the suppressant effect of loperamide. We concluded that the NK(3) receptor-triggered 5-HT release from colonic mucosa is suppressed by loperamide-sensitive mechanisms, whereas the NK(2)-receptor-triggered 5-HT release is loperamide-insensitive. Our data also suggest that the suppressant effect of loperamide is probably mediated by the activation of kappa- and delta-opioid receptors located on intrinsic neurons.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antidiarrheals,
http://linkedlifedata.com/resource/pubmed/chemical/Loperamide,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Tachykinin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Substance P,
http://linkedlifedata.com/resource/pubmed/chemical/senktide
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1347-8613
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
98
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
175-80
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15942125-Animals,
pubmed-meshheading:15942125-Antidiarrheals,
pubmed-meshheading:15942125-Colon,
pubmed-meshheading:15942125-Guinea Pigs,
pubmed-meshheading:15942125-Intestinal Mucosa,
pubmed-meshheading:15942125-Loperamide,
pubmed-meshheading:15942125-Male,
pubmed-meshheading:15942125-Peptide Fragments,
pubmed-meshheading:15942125-Receptors, Tachykinin,
pubmed-meshheading:15942125-Serotonin,
pubmed-meshheading:15942125-Substance P
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pubmed:year |
2005
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pubmed:articleTitle |
Loperamide inhibits tachykinin NK3-receptor-triggered serotonin release without affecting NK2-receptor-triggered serotonin release from guinea pig colonic mucosa.
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pubmed:affiliation |
Department of Pharmacology, Dokkyo University School of Medicine, Tochigi, Japan. s-kojima@dokkymed.ac.jp
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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