BioScience Trends. 2014;8(1):11-17. (DOI: )
Design, synthesis and biological evaluation of naphthalimide-based fluorescent probes for ?1-adrenergic receptors.
Zhang W, Chen LZ, Ma Z, Du LP, Li MY
?1-Adrenergic receptors (?1-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, ?1-ARs have been divided into at least three subtypes, ?1A, ?1B, and ?1D, which distribute in various tissues and organs. In this research, we designed and synthesized several napthalimide-based small-molecule fluorescent probes for ?1-ARs, which mainly contained two parts: the pharmacophore (quinazoline and phenylpiperazine) that binds to ?1-ARs and the fluorophore (naphthalimide) that labels the receptors with fluorescent properties. Moreover, some of these compounds demonstrated potent affinity to ?1-ARs and cell imaging potential.
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