Drug Discov Ther. 2014;8(1):11-17.

Design, synthesis and biological evaluation of naphthalimide-based fluorescent probes for α1-adrenergic receptors.

Zhang W, Chen LZ, Ma Z, Du LP, Li MY


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, α1A, α1B, and α1D, 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.

KEYWORDS: α1-Adrenergic receptors, fluorescent probes, high affinity, cell imaging

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