| pubmed-article:2521513 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C1707455 | lld:lifeskim |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C0360055 | lld:lifeskim |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C2917412 | lld:lifeskim |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C0871161 | lld:lifeskim |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C0701391 | lld:lifeskim |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C0078743 | lld:lifeskim |
| pubmed-article:2521513 | lifeskim:mentions | umls-concept:C0733434 | lld:lifeskim |
| pubmed-article:2521513 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:2521513 | pubmed:dateCreated | 1989-3-3 | lld:pubmed |
| pubmed-article:2521513 | pubmed:abstractText | The well-documented 5-HT3 receptor antagonists, ICS 205-930 and GR38032F, have been compared with regard to their inhibitory activity at 5-HT3 receptors to another gastrokinetic agent, zacopride. Zacopride and ICS 205-930 showed similar affinity (-log kB approximately 8.0), whereas GR38032F showed lower affinity (-log ka approximately 7.0) at 5-HT3 receptors in the guinea pig ileum. After i.v. administration to anesthetized rats, zacopride was approximately 10-fold more potent than either ICS 205-930 or GR38032F, which were equipotent as inhibitors of serotonin-induced bradycardia (5-HT3-mediated activation of the von Bezold Jarisch reflex). After oral administration to anesthetized rats, zacopride remained approximately 10-fold more potent than ICS 205-903, which was approximately 2-fold more potent than GR38032F as an inhibitor of serotonin-induced bradycardia. Furthermore, the inhibitory effectiveness of GR38032F persisted for less than 3 hr after oral administration and for less than 15 min after intravenous administration. ICS 205-930 produced maximal inhibition of serotonin-induced bradycardia for over 3 hr with heart rate returning to control values 6 hr after oral administration. Zacopride possessed the longest duration of inhibitory effectiveness in urethane-anesthetized rats with maximal inhibition still apparent 6 hr after oral administration. All three agents inhibited cisplatin-induced emesis after i.v. administration in dogs with zacopride being 10-fold more potent than ICS 205-930 or GR38032F, which were equipotent. These comparative data with three 5-HT3 receptor antagonists indicate that in animals, zacopride was more potent and longer acting than either ICS 205-930 or GR38032F. Furthermore, after oral administration to rats, GR38032F was slightly less potent than ICS 205-930 and possessed the shortest duration of action. | lld:pubmed |
| pubmed-article:2521513 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2521513 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2521513 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:2521513 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2521513 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:2521513 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:2521513 | pubmed:author | pubmed-author:CohenM LML | lld:pubmed |
| pubmed-article:2521513 | pubmed:author | pubmed-author:LacefieldWW | lld:pubmed |
| pubmed-article:2521513 | pubmed:author | pubmed-author:GiddaJ SJS | lld:pubmed |
| pubmed-article:2521513 | pubmed:author | pubmed-author:BloomquistWW | lld:pubmed |
| pubmed-article:2521513 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2521513 | pubmed:volume | 248 | lld:pubmed |
| pubmed-article:2521513 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2521513 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2521513 | pubmed:pagination | 197-201 | lld:pubmed |
| pubmed-article:2521513 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
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| pubmed-article:2521513 | pubmed:year | 1989 | lld:pubmed |
| pubmed-article:2521513 | pubmed:articleTitle | Comparison of the 5-HT3 receptor antagonist properties of ICS 205-930, GR38032F and zacopride. | lld:pubmed |
| pubmed-article:2521513 | pubmed:affiliation | Department of Cardiovascular Pharmacology, Eli Lilly and Company, Indianapolis, Indiana. | lld:pubmed |
| pubmed-article:2521513 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:2521513 | pubmed:publicationType | Comparative Study | lld:pubmed |
| pubmed-article:2521513 | pubmed:publicationType | In Vitro | lld:pubmed |
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