Fluorescent ligands for the histamine H 2 receptor: synthesis and preliminary characterization

…, V Zuliana, M Hoffman, H Timmerman, R Leurs

Index: Malan, Sarel F.; Marle, Andre Van; Menge, Wiro M.; Zuliana, Valentina; Hoffman, Marcel; Timmerman, Henk; Leurs, Rob Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 24 p. 6495 - 6503

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Citation Number: 25

Abstract

3-[3-(Piperidinomethyl) phenoxy] alkyl, N-cyano-N′-[ω-[3-(1-piperidinylmethyl) phenoxy] alkyl] guanidine and 2-(5-methyl-4-imidazolyl) methyl thioethyl derivatives containing fluorescent functionalities were synthesized and the histamine H2 receptor affinity was evaluated using the H2 antagonist [125I]-aminopotentidine. The compounds exhibited weak to potent H2 receptor affinity with pKi values ranging from< 4 to 8.85. The highest H2 ...