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Synthesis and pharmacological activity of fluorescent histamine H1 receptor antagonists related to mepyramine,

Li, Liantao ; Kracht, Julia ; Peng, Shiqi ; Bernhardt, Günther ; Buschauer, Armin



Abstract

Fluorescently labeled histamine H1 receptor antagonists were synthesized starting from N-demethylmepyramine by introduction of ω-aminoalkyl chains (2–8 methylene groups in length) followed by derivatization of the terminal NH2 group with various fluorophores (fluorescein, naphthofluorescein, rhodamine, tetramethylrhodamine, BODIPY, dansyl, and nitrobenzoxadiazole (NBD)). On the isolated guinea ...

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