|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
1994-9-14
|
|
pubmed:abstractText |
We have investigated the in vivo motor stimulating and gastroprokinetic properties of the azabicycloalkyl benzimidazolone derivative BIMU 1 (3-ethyl-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H- benzimidazole-1-carboxamide hydrochloride) and its binding profile at 5-hydroxytryptamine3 and 5-hydroxytryptamine4 receptors, in an attempt to assess the serotonergic mechanism underlying its prokinetic action. BIMU 1 dose-dependently (0.01-0.3 mg/kg i.v.) increased the motility of a denervated pouch of canine stomach. This excitatory action was sensitive to muscarinic blockade. A similar stimulatory effect was exerted by the benzamidic prokinetic agent cisapride (0.03-0.3 mg/kg i.v.) but not by the 5-HT3 receptor antagonist ondansetron (up to 1 mg/kg i.v.). The significance for propulsive efficacy of the motor stimulating activity of BIMU 1 was evaluated in a model of gastric emptying of liquids in the conscious dog. The emptying rate of a non-caloric liquid meal instilled through a gastric fistula was accelerated by both BIMU 1 (0.01-1 mg/kg i.v. and 0.1-3 mg/kg p.o.) and cisapride (0.03-1 mg/kg i.v. and 0.3-10 mg/kg p.o.). Ondansetron (1 mg/kg i.v.) did not show any effect. The activity of the 5-HT4 receptor antagonist DAU 6285 was evaluated in the gastric emptying model per se and in interaction experiments on the accelerating action of BIMU 1 (0.3 mg/kg i.v.).(ABSTRACT TRUNCATED AT 250 WORDS)
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/(endo-N-8-methyl-8-azabicyclo(3.2.1)...,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Ulcer Agents,
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/Ondansetron,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Apr
|
|
pubmed:issn |
0028-1298
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:volume |
349
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
338-45
|
|
pubmed:dateRevised |
2010-11-18
|
|
pubmed:meshHeading |
pubmed-meshheading:8058105-Animals,
pubmed-meshheading:8058105-Anti-Ulcer Agents,
pubmed-meshheading:8058105-Benzimidazoles,
pubmed-meshheading:8058105-Bicyclo Compounds,
pubmed-meshheading:8058105-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:8058105-Cisapride,
pubmed-meshheading:8058105-Dogs,
pubmed-meshheading:8058105-Dose-Response Relationship, Drug,
pubmed-meshheading:8058105-Female,
pubmed-meshheading:8058105-Gastric Emptying,
pubmed-meshheading:8058105-Gastrointestinal Motility,
pubmed-meshheading:8058105-Male,
pubmed-meshheading:8058105-Muscle Denervation,
pubmed-meshheading:8058105-Neostriatum,
pubmed-meshheading:8058105-Ondansetron,
pubmed-meshheading:8058105-Piperidines,
pubmed-meshheading:8058105-Serotonin Antagonists,
pubmed-meshheading:8058105-Serotonin Receptor Agonists,
pubmed-meshheading:8058105-Stomach,
pubmed-meshheading:8058105-Swine,
pubmed-meshheading:8058105-Tumor Cells, Cultured
|
|
pubmed:year |
1994
|
|
pubmed:articleTitle |
Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors.
|
|
pubmed:affiliation |
Research and Development Division, Boehringer Ingelheim Italia, Milan.
|
|
pubmed:publicationType |
Journal Article,
In Vitro
|
