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Synthesis and structure-activity relationships of NG-acylated arylalkylguanidines and related compounds as histamine receptor ligands: searching for selective H4R agonists

URN to cite this document:
urn:nbn:de:bvb:355-opus-11072
Igel, Patrick
Date of publication of this fulltext: 16 Jan 2009 15:23


Abstract (English)

In previous studies NG-acylated imidazolylpropylguanidines, originally developed as histamine H2 receptor (H2R) agonists with reduced basicity relative to guanidine-type H2R agonists, turned out to be also highly potent at the histamine H3 receptor (H3R) and histamine H4 receptor (H4R). Particularly at the H4R, the compounds showed high agonistic efficacies. This thesis aimed at the design, ...

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Translation of the abstract (German)

In vorausgegangenen Untersuchungen wurden in einer Serie von NG-acylierten Imidazolylpropylguanidinen, die ursprünglich als Histamin H2 Rezeptor (H2R) Agonisten mit reduzierter Basizität ausgehend von H2R Agonisten des Guanidin-Typs entwickelten wurden, hochpotente Histamin H3 Rezeptor (H3R) und Histamin H4 Rezeptor (H4R) Liganden identifiziert. Diese Verbindungen zeigten insbesondere am H4R ...

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