Phenylethanolamine-based NMDA receptor antagonists. United States Patent 8648198

Hiro Furukawa (February 2014) Phenylethanolamine-based NMDA receptor antagonists. United States Patent 8648198. .



Described herein are enhanced N-methyl-D-aspartate (NMDA) receptor antagonists, pharmaceutical compositions thereof, and their methods of use and treatment, e.g., of Formula (I):wherein one or more of R1, R2, R3, R4, R5, or the ring formed by the joining of R1 and R2, is a hydrophobic moiety which confers enhanced antagonist activity as compared to existing NMDA receptor antagonists, e.g., ifenprodil. Compounds described herein are designed based on the discovery that ifenprodil binds within the allosteric domain of the GluN1/GluN2B NMDA receptor, particularly at the interface between GluN1 and GluN2B subunits. In silico methods are further described herein.

Item Type: Patent
Subjects: patents
CSHL Authors:
Communities: CSHL labs > Furukawa lab
Depositing User: Matt Covey
Date: 11 February 2014
Date Deposited: 04 Feb 2015 21:40
Last Modified: 04 Feb 2015 21:40

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