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  • 标题:Development of κ Opioid Receptor Agonists by Focusing on Phenyl Substituents of 4-Dimethylamino-3-phenylpiperidine Derivatives: Structure–Activity Relationship Study of Matrine Type Alkaloids
  • 本地全文:下载
  • 作者:Hiroyoshi Teramoto ; Takayasu Yamauchi ; Shigeru Sasaki
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2016
  • 卷号:64
  • 期号:5
  • 页码:420-431
  • DOI:10.1248/cpb.c15-00963
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:A series of new κ opioid receptor (KOR) agonists were developed from the lead compound 4-dimethylamino-1-pentanoylpiperidine ( 3 ), a matrine-type alkaloid. Derivatives of 3 were synthesized with a variety of phenyl substituents and evaluated for their antinociceptive effects. Additionally, their selectivity for an opioid receptor was investigated for cis - 4c and d , and trans - 4g , all of which had high activity exerted through the KOR.
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