title: Design, synthesis and biological evaluation of naphthalimide-based 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, 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.
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.forename: Laizhong
authors.initials: L
authors.lastname: Chen
authors.forename: Zhao
authors.initials: Z
authors.lastname: Ma
authors.forename: Lupei
authors.initials: L
authors.lastname: Du
authors.forename: Minyong
authors.initials: M
authors.lastname: Li
mesh_terms: D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000378:metabolism*; D057809:HEK293 Cells; D006801:Humans; D008856:Microscopy, Fluorescence; D015394:Molecular Structure; D053644:Naphthalimides / Q000138:chemical synthesis / Q000378:metabolism*; D010879:Piperazines / Q000138:chemical synthesis / Q000378:metabolism*; D011485:Protein Binding; D011799:Quinazolines / Q000138:chemical synthesis / Q000378:metabolism*; D018340:Receptors, Adrenergic, alpha-1 / Q000235:genetics / Q000378:metabolism*; D014162:Transfection
chemical_list: D005456:Fluorescent Dyes; D053644:Naphthalimides; D010879:Piperazines; D011799:Quinazolines; D018340:Receptors, Adrenergic, alpha-1; C031503:phenylpiperazine