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Synthesis and pharmacological characterization of novel fluorescent histamine H2-receptor ligands derived from aminopotentidine.

Xie, Sheng-Xue ; Petrache, Georgiana ; Schneider, Erich ; Ye, Qi-Zhuang ; Bernhardt, Günther ; Seifert, Roland ; Buschauer, Armin


In an effort to develop a non-radioactive alternative to the [3H]tiotidine and [125I]iodoaminopotentidine binding assays for the histamine H2-receptor (H2R), primary amines related to aminopotentidine were prepared and coupled with the succinimidyl esters of the bulky fluorescent dyes S0536 and BODIPY 650/665-X. The primary amines exhibited different degrees of antagonistic potency at the human ...


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