Syntheses and Biological Activities of Joro Spider Toxin Analogs to Spidamine and Joramine
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概要
- 論文の詳細を見る
In order to study the structure-activity relationships of spidamine and joramine found in the venom of Joro spider, Nephila clavata, we attempted to synthesize various analogs. Six analogs were convergently synthesized according to our previous method for the synthesis of spidamine, N-(3-aminopropyl-β-alanyl)-N'-(2,4-dihydroxy-phenylacetyl-L-asparaginyl)-1,5-pentanediamine and joramine, N-(3-aminopropyl-β-alanyl)-N'-(4-hydroxyphenyl-acetyl-L-asparaginyl)-1,5-pentanediamine. The biological activities of the analogs and four intermediates were compared with those of synthetic spidamine and joramine in three bioassay systems, lobster neuromuscular synapse, cockroaches and mosquito larvae. The glutamate receptors in these systems were inhibited by some analogs, and the D-asparagine- or indoleacetyl-containing analogs were found to be strong inhibitors. These compounds have potential application as insecticides.
- 公益社団法人日本薬学会の論文
- 1997-01-15
著者
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Yoshioka Masanori
Faculty of Pharmaceutical Sciences, Setsunan University
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Chiba T
Faculty Of Pharmaceutical Sciences Setsunan University
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KAWAI Nobufumi
Department of Physiology,Jichi Medical School
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AKIZAWA Toshifumi
Faculty of Pharmaceutical Sciences, Setsunan University
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Kono Y
National Institute Of Health
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Kawai N
Department Of Physiology Jichi Ika University
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Kawai Nobufumi
Department Of Neurobiology Tokyo Metropolitan Institute For Neurosciences
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Kawai Nobufumi
Physiology Jichi Medical School
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Yoshioka M
Faculty Of Pharmaceutical Sciences Setsunan University
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Yoshioka Masanori
Faculty Of Pharmaceutical Sciences Setsunan University
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CHIBA Tadashige
Faculty of Pharmaceutical Sciences, Setsunan University
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MATSUKAWA Motomi
Faculty of Pharmaceutical Sciences, Setsunan University
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KONO Yoshiaki
National Institute of Health
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Yoshioka Masanori
Department Of Analytical Chemistry Faculty Of Pharmaceutical Sciences Setsunan University
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Matsukawa M
Setsunan Univ. Osaka Jpn
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Akizawa Toshifumi
Faculty Of Pharmaceutical Sciences Setsunan University
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