Jean Y. Zhang scite author profile

As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-HT(6) antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.

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Identification of a series of benzoxazoles as potent 5-HT6 ligands

Liu

Comery

et al. 2009

Bioorganic & Medicinal Chemistry Letters

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Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT6 antagonists

Liu

Robichaud

Greenfield

et al. 2011

Bioorganic & Medicinal Chemistry

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Jean Y. Zhang

Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms

Characterization of the 5-HT6 receptor coupled to Ca2+ signaling using an enabling chimeric G-protein

5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists

Identification of a series of benzoxazoles as potent 5-HT6 ligands

Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT6 antagonists

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