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Highly potent and selective acylguanidine-type histamine H2 receptor agonists: synthesis and structure-activity relationships of mono- and bivalent ligands

URN to cite this document:
urn:nbn:de:bvb:355-epub-222378
Birnkammer, Tobias
Date of publication of this fulltext: 20 Oct 2011 09:00


Abstract (English)

Potent and selective histamine H2 receptor (H2R) agonists, including brain-penetrating compounds, are required as pharmacological tools to evaluate the (patho)physiological role of H2Rs. Moreover, H2R agonists might be of therapeutic value as drugs, for example, in the treatment of acute myelogenous leukemia. Previously, acylguanidine-type H2R agonists with reduced basicity were synthesized in ...

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Translation of the abstract (German)

Selektive Histamin H2-Rezeptor-Agonisten rücken, u.a. aufgrund ihres Einflusses auf Leukämiezellen und der möglichen neuropharmakologischen Wirkung, immer mehr in den Fokus. Bereits in den letzten Jahrzehnten wurden zahlreiche H2R-Agonisten wie 5-Methylhistamin, Dimaprit, Impromidin und Arpromidin beschrieben. Nach der Entdeckung der H3 und H4 Rezeptoren wurde jedoch deren H2R-Selektivität ...

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