Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers.

Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Research Abstract Details 

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Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Abstract Text:

Hiromitsu Takayama,Yuichi Yaegashi,Mariko Kitajima,Xia Han,Kazuhiro Nishimura,Shigeru Okuyama,Kazuei Igarashi,

We have developed a new class of N-methyl-d-aspartate (NMDA) channel blockers having a conjugate structure that consists of a nitrogenous heterocyclic head and a tetraamine tail. Among them, dihydrodibenzazepine-homospermine conjugate (8) exhibited potent antagonistic activity at NR1/NR2A or NR1/NR2B NMDA subtype receptors compared with the lead compound, AQ343 (1), or memantine, as well as weak cytotoxicity. Its superior biological profiles compared with known compounds point to its potential use as therapeutic agents for neurological disorders.

Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Publishing Authors By Initials

H Takayama,Y Yaegashi,M Kitajima,X Han,K Nishimura,S Okuyama,K Igarashi,

For similar proteins: membrane proteins: receptors, cell surface: receptors, neurotransmitter: receptors, amino acid: receptors, glutamate: receptors, n-methyl-d-aspartate research abstracts see: proteins: membrane proteins: receptors, cell surface: receptors, neurotransmitter: receptors, amino acid: receptors, glutamate: receptors, n-methyl-d-aspartate research

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Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 4729-32

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 27

MONTH: 06

YEAR: 2007

Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Keywords Mesh Terms:

KEYWORDS: Receptors, N-Methyl-D-Aspartate

MESH TERMS: antagonists & inhibitors

Chemical & Substance for Abstract: Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers. Information

Substance Name: Receptors, N-Methyl-D-Aspartate

Registry Number: 0

Grant and Affiliation Information for Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers.

AFFILIATION: Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan. takayama@p.chiba-u.ac.jp

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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