2,3-Dihydrobenzo-dioxine piperidine derivatives as potent and selective α2c antagonists. 2022

Shouming Wang, and Anssi Haikarainen, and Antti Pohjakallio, and Julius Sipilä, and Janne Kaskinoro, and Satu Juhila, and Niina Jalava, and Mikko Koskinen, and Marja Vesajoki, and Esa Kumpulainen, and Jarmo Pystynen, and Tuula Koskelainen, and Patrik Holm, and David Din Belle
Department of Medicinal Chemistry, Orion Corporation Orion Pharma, Orionintie 1, PL 65, FI-02101, Finland. Electronic address: shouming.wang@orionpharma.com.

In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule.

UI MeSH Term Description Entries
D010880 Piperidines A family of hexahydropyridines.
D004147 Dioxins A family of compounds that contain the 1,4-dioxin structure. Many specific dioxin derivatives are listed as CARCINOGENS; TERATOGENS; or MUTAGENS. Dioxin
D018341 Receptors, Adrenergic, alpha-2 A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release. Adrenergic alpha-2 Receptors,Receptors, alpha-2 Adrenergic,alpha-2 Adrenergic Receptors,Adrenergic Receptor alpha(2C),Adrenergic Receptor alpha(2d),Adrenergic Receptor alpha-2C,Adrenergic Receptor alpha-2b,Adrenergic Receptor, alpha-2,Adrenergic alpha-2A Receptors,Adrenergic alpha-2B Receptors,Adrenergic alpha-2C Receptors,Adrenergic alpha-2D Receptors,Receptor, Adrenergic, alpha-2,Receptor, Adrenergic, alpha-2A,Receptor, Adrenergic, alpha-2B,Receptor, Adrenergic, alpha-2C,Receptor, Adrenergic, alpha-2D,Receptors, Adrenergic, alpha-2A,Receptors, Adrenergic, alpha-2B,Receptors, Adrenergic, alpha-2D,alpha 2 Adrenergic Receptors,alpha-2A Adrenergic Receptor,alpha-2B Adrenergic Receptor,alpha-2C Adrenergic Receptor,alpha-2D Adrenergic Receptor,Adrenergic Receptor alpha 2C,Adrenergic Receptor alpha 2b,Adrenergic Receptor, alpha 2,Adrenergic Receptor, alpha-2A,Adrenergic Receptor, alpha-2B,Adrenergic Receptor, alpha-2C,Adrenergic Receptor, alpha-2D,Adrenergic Receptors, alpha-2,Adrenergic alpha 2 Receptors,Adrenergic alpha 2A Receptors,Adrenergic alpha 2B Receptors,Adrenergic alpha 2C Receptors,Adrenergic alpha 2D Receptors,Receptor alpha-2C, Adrenergic,Receptor alpha-2b, Adrenergic,Receptor, alpha-2 Adrenergic,Receptor, alpha-2A Adrenergic,Receptor, alpha-2B Adrenergic,Receptor, alpha-2C Adrenergic,Receptor, alpha-2D Adrenergic,Receptors, Adrenergic alpha-2,Receptors, Adrenergic alpha-2A,Receptors, Adrenergic alpha-2B,Receptors, Adrenergic alpha-2C,Receptors, Adrenergic alpha-2D,Receptors, alpha 2 Adrenergic,alpha 2A Adrenergic Receptor,alpha 2B Adrenergic Receptor,alpha 2C Adrenergic Receptor,alpha 2D Adrenergic Receptor,alpha-2 Adrenergic Receptor,alpha-2 Receptors, Adrenergic,alpha-2A Receptors, Adrenergic,alpha-2B Receptors, Adrenergic,alpha-2C Receptors, Adrenergic,alpha-2C, Adrenergic Receptor,alpha-2D Receptors, Adrenergic,alpha-2b, Adrenergic Receptor

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