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Discovery of Quinazoline-Based Fluorescent Probes to ?1-Adrenergic Receptors.

ABSTRACT: ?1-Adrenergic receptors (?1-ARs), as the essential members of G protein-coupled receptors (GPCRs), can mediate numerous physiological responses in the sympathetic nervous system. In the current research, a series of quinazoline-based small-molecule fluorescent probes to ?1-ARs (1a-1e), including two parts, a pharmacophore for ?1-AR recognition and a fluorophore for visualization, were well designed and synthesized. The biological evaluation results displayed that these probes held reasonable fluorescent properties, high affinity, accepted cell toxicity, and excellent subcellular localization imaging potential for ?1-ARs.

SUBMITTER: Zhang W

PROVIDER: S-EPMC4434465 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature

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Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.

Zhang Wei W Ma Zhao Z Li Wenhua W Li Geng G Chen Laizhong L Liu Zhenzhen Z Du Lupei L Li Minyong M

ACS medicinal chemistry letters 20150330 5

α1-Adrenergic receptors (α1-ARs), as the essential members of G protein-coupled receptors (GPCRs), can mediate numerous physiological responses in the sympathetic nervous system. In the current research, a series of quinazoline-based small-molecule fluorescent probes to α1-ARs (1a-1e), including two parts, a pharmacophore for α1-AR recognition and a fluorophore for visualization, were well designed and synthesized. The biological evaluation results displayed that these probes held reasonable flu ...[more]

PMID: 26005522

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