Compound 31a, both potent and subtype-selective, enabled H 1R visualization using confocal microscopy at a concentration of 10 nM. Incorporation of a boron-dipyrromethene (BODIPY) 630/650-based fluorophore conferred high binding affinity to our H 1R fluorescent ligands, remarkably overriding the linker SAR observed in corresponding unlabeled congeners.
2 acetyl pyridine inmr series#
Here, we report a series of high-affinity H 1R fluorescent ligands varying in peptide linker composition, orthosteric targeting moiety, and fluorophore. We previously reported a H 1R fluorescent ligand, bearing a peptide-linker, based on antagonist VUF13816 and sought to further explore structure–activity relationships (SARs) around the linker, orthostere, and fluorescent moieties.
2 acetyl pyridine inmr plus#
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