Novel [_D-Arg^2]dermorphin(1-4) Analogs with μ-Opioid Receptor Antagonist Activity
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概要
- 論文の詳細を見る
Ten Tyr-_D-Arg-Phe-βAla-NH_2 (YRFB) analogs in which specific amino acid side chains are shifted to the N^α-position were synthesized, and the binding to these analogs to the μ receptor and their in vitro biological properties were evaluated. Some analogs in which a N, N-bis(p-hydroxybenzyl)-Gly residue was substituted for Tyr^1 exhibited μ receptor antagonist activities (pA_2) between 5.3 and 6.1. Of these analogs, [N, N-bis(p-hydroxybenzyl)-Gly^1]YRFB was found to be the most potent specific antagonist for the μ-opioid receptor.
- 公益社団法人日本薬学会の論文
- 2002-10-01
著者
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AMBO Akihiro
Tohoku Pharmaceutical University
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SASAKI Yusuke
Tohoku Pharmaceutical University
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Sasaki Yusuke
Tohoku College Of Pharmacy
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TERASHIMA Takanori
Tohoku Pharmaceutical University
関連論文
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- Synthesis and Biological Activity of Opioid Peptides Replaced Phenylalanine at Position 3 or 4 by 2, 6-Dimethylphenylalanine
- Biological Properties of Opioid Peptides Replacing Tyr at Position 1 by 2,6-Dimethyl-Tyr
- Synthesis and Bioactivity of Novel Type Pyrazinone Ring-Containing μ-Opioid Ligands
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- Design of Opioidmimetics : Dimerization of 2', 6'-Dimethyl-L-Tyrosine
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