- Potent, selective benzenesulfonamide agonists of the human β3 adrenergic receptor
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A cloned human β3 adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR, studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM β3 agonist which shows 30-fold selectivity for β3 agonist activity over β1 and β2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over β1 and β2, respectively.
- Weber, Ann E.,Mathvink, Robert J.,Perkins, Leroy,Hutchins, Jennifer E.,Candelore, Mari R.,Tota, Laurie,Strader, Catherine D.,Wyvratt, Matthew J.,Fisher, Michael H.
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- NMDA RECEPTOR ANTAGONISTS FOR NEUROPROTECTION
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Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurode
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Paragraph 0155
(2021/03/18)
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