Abstract:The high affinity dopamine D4 receptor ligand
APH199
and derivatives thereof exhibit bias toward the Gi signaling
pathway over β-arrestin recruitment compared to quinpirole.
Based on APH199, two novel groups of D4 subtype selective
ligands were designed and evaluated, in which the original benzyl
phenylsemicarbazide substructure was replaced by either a biphenylmethyl
urea or a biphenyl urea moiety. Functional assays revealed a range
of different bias profiles among the newly synthesized compounds,
namely, wit… Show more
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