Document Detail

5-hydroxytryptamine4 receptor agonists facilitate cholinergic transmission in the circular muscle of guinea pig ileum: antagonism by tropisetron and DAU 6285.
MedLine Citation:
PMID:  1315899     Owner:  NLM     Status:  MEDLINE    
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.
M Tonini; S M Candura; L Onori; T Coccini; L Manzo; C A Rizzi
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Life sciences     Volume:  50     ISSN:  0024-3205     ISO Abbreviation:  Life Sci.     Publication Date:  1992  
Date Detail:
Created Date:  1992-06-09     Completed Date:  1992-06-09     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0375521     Medline TA:  Life Sci     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  PL173-8     Citation Subset:  IM    
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
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MeSH Terms
Benzimidazoles / pharmacology*
Bicyclo Compounds / pharmacology*
Bicyclo Compounds, Heterocyclic*
Guinea Pigs
Ileum / drug effects*,  innervation,  physiology
Indoles / pharmacology*
Muscle Contraction / drug effects
Muscle, Smooth / drug effects*,  innervation,  physiology
Piperidines / pharmacology
Receptors, Cholinergic / drug effects*
Receptors, Serotonin / drug effects*
Scopolamine / pharmacology
Serotonin / pharmacology
Synaptic Transmission / drug effects
Tetrodotoxin / pharmacology
Reg. No./Substance:
0/Benzimidazoles; 0/Bicyclo Compounds; 0/Bicyclo Compounds, Heterocyclic; 0/Indoles; 0/Piperidines; 0/Receptors, Cholinergic; 0/Receptors, Serotonin; 123258-98-0/DAU 6285; 134296-40-5/(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide; 4368-28-9/Tetrodotoxin; 50-67-9/Serotonin; 51-34-3/Scopolamine; 81098-60-4/Cisapride; 89565-68-4/tropisetron

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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