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N(G)-Acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent

Igel, Patrick ; Schneider, Erich ; Schnell, David ; Elz, Sigurd ; Seifert, Roland ; Buschauer, Armin


3-(1H-imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H3 receptor (hH3R) and human histamine H4 receptor (hH4R). With the aim to increase selectivity for the hH4R, the guanidine group in 4 was acylated. N1-Acetyl-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-PI288, 13) was a potent full agonist at hH4R (pEC50: 8.31, α: 1.00), ...


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