Red-fluorescent argininamide-type NPY Y 1 receptor antagonists as pharmacological tools

…, N Pluym, S Teng, G Bernhardt, A Buschauer

Index: Keller, Max; Erdmann, Daniela; Pop, Nathalie; Pluym, Nikola; Teng, Shangjun; Bernhardt, Guenther; Buschauer, Armin Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 9 p. 2859 - 2878

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Citation Number: 20

Abstract

Abstract Fluorescently labelled NPY Y 1 receptor (Y 1 R) ligands were synthesized by connecting pyrylium and cyanine dyes with the argininamide-type Y 1 R antagonist core structure by linkers, covering a wide variety in length and chemical nature, attached to the guanidine group. The most promising fluorescent probes had Y 1 R affinities (radioligand binding) and antagonistic activities (calcium assay) in the one-to two-digit nanomolar ...