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Your search keyword '"Haga, Yoshihiro"' showing total 3 results
Start Over Author "Haga, Yoshihiro" Publisher elsevier b.v.
3 results on '"Haga, Yoshihiro"'

3. Discovery of NR2B-selective antagonists via scaffold hopping and pharmacokinetic profile optimization.

Author

Anan, Kosuke, Masui, Moriyasu, Tazawa, Aya, Tomida, Minoru, Haga, Yoshihiro, Kume, Masaharu, Yamamoto, Shoichi, Shinohara, Shunji, Tsuji, Hiroki, Shimada, Shinji, Yagi, Shigenori, Hasebe, Nobuyoshi, and Kai, Hiroyuki

Subjects
*ISOXAZOLES, *CAUSATION (Philosophy), *HOPS, *METHYL aspartate receptors
Abstract

Graphical abstract Abstract Selective N -methyl- d -aspartate receptor subunit 2B (NR2B) antagonists show potential as analgesic drugs, and do not cause side effects associated with non-selective N -methyl- d -aspartate (NMDA) antagonists. Using a scaffold-hopping approach, we previously identified isoxazole derivative 4 as a potent selective NR2B antagonist. In this study, further scaffold hopping of isoxazole derivative 4 and optimization of its pharmacokinetic profile led to the discovery of the orally bioavailable compound 6v. In a rat study of analgesia, 6v demonstrated analgesic effects against neuropathic pain. [ABSTRACT FROM AUTHOR]

Published
2019
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