Inside Cover: Tritium-Labeled N1-[3-(1H-imidazol-4-yl)propyl]-N2-propionylguanidine ([3H]UR-PI294), a High-Affinity Histamine H3 and H4 Receptor Radioligand / NG-Acylated Aminothiazolylpropylguanidines as Potent and Selective Histamine H2 Receptor Agonists (ChemMedChem 2/2009)

✍ Scribed by Patrick Igel; David Schnell; Günther Bernhardt; Roland Seifert; Armin Buschauer; Anja Kraus; Prasanta Ghorai; Tobias Birnkammer; Sigurd Elz; Stefan Dove

• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: English
• Weight: 393 KB
• Volume: 4
• Category: Article
• ISSN: 1860-7179
• DOI: 10.1002/cmdc.200990005

✦ Synopsis

Abstract

The inside cover picture shows the human histamine H~2~ receptor and the H~2~ and H~3~/H~4~ receptor‐selective ligands identified. Bioisosteric replacement of the imidazole ring of the N^G^‐acyl‐imidazolylpropylguanidine with 2‐aminothiazole yielded potent and selective H~2~ receptor agonists. In contrast, modification of the acyl group gave a high‐affinity H~3~/H~4~‐selective tritiated radioligand. For more details, see the Full Papers by A. Buschauer et al. on p. 225 ff and p. 232 ff.magnified image