Design, synthesis and biological evaluation of naphthalimidebased fluorescent probes for α₁-adrenergic receptors

Abstract

α₁-Adrenergic receptors (α₁-ARs), as one of the most important members of G protein-coupled receptors (GPCRs), can mediate lots of physiological responses of the sympathetic nervous system. Until now, α₁-ARs have been divided into at least three subtypes, α_1A, α_1B, and α_1D, which distribute in various tissues and organs. In this research, we designed and synthesized several napthalimide-based small-molecule fluorescent probes for α₁-ARs, which mainly contained two parts: the pharmacophore (quinazoline and phenylpiperazine) that binds to α₁-ARs and the fluorophore (naphthalimide) that labels the receptors with fluorescent properties. Moreover, some of these compounds demonstrated potent affinity to α₁-ARs and cell imaging potential.