Linked Life Data

9372599

Source:http://linkedlifedata.com/resource/pubmed/id/9372599

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6-7
pubmed:dateCreated
1998-2-27
pubmed:abstractText
This paper summarizes the findings obtained for three different series of original compounds designed as potential H3-antagonists starting from thioperamide structure. The compounds were tested in functional and binding assays to estimate their potency, affinity and selectivity for histamine H3 receptors. Among them, many non-thiourea/isothiourea derivatives acted as selective H3 competitive antagonists and, particularly, 4(5)-[2-[4(5)-cyclohexylimidazol-2-ylthio]ethyl] imidazole (dIII) proved to be the most potent H3 blocker vs (R)-alpha-methylhistamine in electrically-stimulated ileum. This imidazole derivative, devoid of thiourea dependent toxic effects, with high affinity displaced biphasically [3H]-N alpha-methylhistamine bound to rat brain H3 sites. Thus, such compound could be proposed as the prototype molecule for the development of new non-thiourea/isothiourea H3-antagonists and as experimental tool to explore the intriguing question of H3 receptor heterogeneity.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0014-827X
pubmed:author
pubmed:issnType
Print
pubmed:volume
52
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
463-9
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:articleTitle
In vitro characterization of potency, affinity and selectivity of H3-antagonists: from thioperamide to thioperamide unrelated imidazole derivatives.
pubmed:affiliation
Istituto di Farmacologia e Farmacognosia, Università degli Studi di Parma, Facoltà di Farmacia, Italy.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't