ChemInform Abstract: Essential Structure of Opioid ϰ Receptor Agonist Nalfurafine for Binding to ϰ Receptor 1: Synthesis of Decahydroisoquinoline Derivatives and Their Pharmacologies.

DOI DOI Web Site Web Site PubMed 被引用文献8件 参考文献30件 オープンアクセス

書誌事項

タイトル別名
  • Essential Structure of Opioid κ Receptor Agonist Nalfurafine for Binding to κ Receptor 1: Synthesis of Decahydroisoquinoline Derivatives and Their Pharmacologies
公開日
2012
資源種別
journal article
DOI
  • 10.1248/cpb.c12-00336
  • 10.1002/chin.201303181
公開者
公益社団法人 日本薬学会

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説明

On the basis of the three-dimensional pharmacophore model of opioid κ agonists, we simplified the structure of nalfurafine (selective κ agonist) to find the essential structural moieties for binding the opioid receptors, especially κ receptor type. As a result, we found that the trans-fused decahydroisoquinoline derivatives without a phenol ring bound the opioid receptor in micromolar order and that both the amide side chain and the nitrogen substituted by the cyclopropylmethyl group were indispensable moieties for eliciting the κ selectivity. The simple decahydroisoquinoline without amide side chain also bound the opioid receptor without receptor type selectivity, suggesting that the message-address concept would be applicable to even these simple derivatives. These findings that the simple decahydroisoquinoline derivatives showed the affinities for the opioid receptors, especially some of the compounds showed κ selectivity, are the first example in the opioid field.

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