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rdf:type |
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lifeskim:mentions |
umls-concept:C0020885,
umls-concept:C0026845,
umls-concept:C0063322,
umls-concept:C0085979,
umls-concept:C0167813,
umls-concept:C0243192,
umls-concept:C0597357,
umls-concept:C0599668,
umls-concept:C0680242,
umls-concept:C1282913,
umls-concept:C1521797
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pubmed:issue |
21
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pubmed:dateCreated |
1992-6-9
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pubmed:abstractText |
The effect of 5-hydroxytryptamine (5-HT), BIMU 8 (endo-N-(8-methyl-8-azabicyclo [3.2.1.] oct-3-yl)-2,3-dihydro-3-(1-methyl)ethyl-2-oxo-1H-benzimidazole-1- carboxamide hydrochloride) and cisapride was studied on the electrically-induced neurogenic cholinergic twitch contractions in the guinea pig ileum circular muscle. These compounds caused a concentration-dependent increase in the amplitude of submaximal twitch contractions with the following rank order of potency: 5-HT greater than BIMU 8 = cisapride. The effect of 5-HT was competitively antagonized by tropisetron (ICS 205-930) (apparent pA2 value: 6.4), suggesting an interaction at 5-hydroxytryptamine4 (5-HT4) receptors. The novel benzimidazolone derivative DAU 6285 (endo-6-methoxy-8-methyl-8-azabicyclo [3.2.1.] oct-3-yl-2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylate hydrochloride), antagonized the effect of 5-HT, BIMU 8 and cisapride with apparent pA2 values in the range 7.1-7.3. Our findings demonstrate that cholinergic neurones innervating the circular coat are endowed with excitatory 5-HT4 receptors. DAU 6285 is approximately 5-9-fold more potent than tropisetron as antagonist at these receptors.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/(endo-N-8-methyl-8-azabicyclo-(3.2.1...,
http://linkedlifedata.com/resource/pubmed/chemical/Benzimidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Cisapride,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cholinergic,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Scopolamine Hydrobromide,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrodotoxin,
http://linkedlifedata.com/resource/pubmed/chemical/tropisetron
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pubmed:status |
MEDLINE
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pubmed:issn |
0024-3205
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
PL173-8
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:1315899-Animals,
pubmed-meshheading:1315899-Benzimidazoles,
pubmed-meshheading:1315899-Bicyclo Compounds,
pubmed-meshheading:1315899-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:1315899-Cisapride,
pubmed-meshheading:1315899-Female,
pubmed-meshheading:1315899-Guinea Pigs,
pubmed-meshheading:1315899-Ileum,
pubmed-meshheading:1315899-Indoles,
pubmed-meshheading:1315899-Male,
pubmed-meshheading:1315899-Muscle, Smooth,
pubmed-meshheading:1315899-Muscle Contraction,
pubmed-meshheading:1315899-Piperidines,
pubmed-meshheading:1315899-Receptors, Cholinergic,
pubmed-meshheading:1315899-Receptors, Serotonin,
pubmed-meshheading:1315899-Scopolamine Hydrobromide,
pubmed-meshheading:1315899-Serotonin,
pubmed-meshheading:1315899-Synaptic Transmission,
pubmed-meshheading:1315899-Tetrodotoxin
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pubmed:year |
1992
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pubmed:articleTitle |
5-hydroxytryptamine4 receptor agonists facilitate cholinergic transmission in the circular muscle of guinea pig ileum: antagonism by tropisetron and DAU 6285.
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pubmed:affiliation |
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
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pubmed:publicationType |
Journal Article,
In Vitro
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