Linked Life Data

9260265

Source:http://linkedlifedata.com/resource/pubmed/id/9260265

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1997-10-8
pubmed:abstractText
In search for novel leads for histamine H3-receptor antagonists a number of amine derivatives of different (1 H-imidazol-4-yl)anilines and omega-(1 H-imidazol-4-yl)alkanamines were prepared. Pharmacological in vitro H3-receptor investigations of the prepared urea, amide, inverse amide, thioamide, and thiourea derivatives on synaptosomes of rat cerebral cortex proved that the aniline derivatives are inactive at H3-receptors, whereas derivatives of the omega-(1 H-imidazol-4-yl)-alkanamines showed moderate to good activity. Some compounds are active in the nanomolar concentration range. The most potent compounds in this series are the thioamide derivative 7 and the urea derivatives 11, 12 of 3-(1 H-imidazol-4-yl) propanamine. Therefore, the urea derivatives were tested in vitro on isolated organs of the guinea pig for their activity on the other two histamine receptor subtypes proving their high selectivity. In vivo studies of the effects of the urea derivatives 11 and 12 on brain Nt-methylhistamine levels, a test of central H3-receptor activity after peroral application to mice, showed no detectable activity. Thus, the urea type antagonists are useful potent and selective H3-receptor tools for in vitro studies and for investigations of ligand-receptor interactions.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0031-7144
pubmed:author
pubmed:issnType
Print
pubmed:volume
52
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
419-23
pubmed:dateRevised
2007-1-29
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
Search for novel leads for histamine H3-receptor antagonists: amine derivatives.
pubmed:affiliation
Institut für Pharmazie I, Freie Universität Berlin, Germany.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't