Antinociceptive and side effects of novel oral active indole alkaloids

2009 Fiscal Year Final Research Report

• Project/Area Number: 20790075
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Biological pharmacy
• Research Institution: Josai International University
• Principal Investigator: MATSUMOTO Kenjiro Josai International University, 薬学部, 助手 (10406770)
• Project Period (FY): 2008 – 2009
• Keywords: オピオイド / インドールアルカロイド / モルヒネ / ミトラガイニン / 痛み

Research Abstract

本研究ではインドール骨格を基本骨格とする7-hydroxymitragynine(7-OHMG)関連化合物の鎮痛活性の評価、副作用の検討、作用機序解析を行った。我々の検討により、強力な鎮痛活性と低い副作用特性を合わせ持つMGM-9やモルヒネより約45倍強力な鎮痛活性を有する化合物MGM-16等が発見された。またMitragynine関連化合物について国内、米国、国際特許出願を行った。

Research Products

• [Journal Article] Localization of TRPV1 and contractile effect of capsaicin in mouse large intestine: high abundance and sensitivity in rectum and distal colon American Journal of Physiology (2009)
  • Author(s): 松本健次郎, 他7名
  • Journal Title: Gastrointestinal and Liver Physiology 54 Pages: G348-360
  • Peer Reviewed
• [Journal Article] MGM-9 [(E)-methyl 2-(3-ethyl-7a,12a-(epoxyethanoxy)-9-fluoro-1,2,3,4,6,7,12,12b-octahydro-8-methoxyindolo[2,3-a]quinolizin-2-yl)-3-methoxyacrylate], a derivative of the indole alkaloid mitragynine: a novel dual-acting mu- and kappa-opioid agonist with potent antinociceptive and weak rewarding effects in mice (2008)
  • Author(s): 松本健次郎, 他11名
  • Journal Title: Neuropharmacology 54 Pages: 154-165
  • Peer Reviewed
• [Presentation] マウス下部消化管におけるTRPV1発現神経と神経ペプチドとの局在に関する免疫組織学的検討 (2009)
  • Author(s): 松本健次郎
  • Organizer: 日本神経消化器病学会
  • Place of Presentation: 仙台
  • Year and Date: 2009-09-21
• [Presentation] Differences in localization of TRPV1 channels and contractile effect of capsaicin in mouse isolated lower gastrointestinal tract: higher abundance and sensitivity of TRPV1 channels in rectum and distal colon than in transverse and proximal colon (2008)
  • Author(s): 松本健次郎
  • Organizer: Digestive Disease Week and the 109th Annual Meeting of the American Gastroenterological Association Institute
  • Place of Presentation: San Diego, U.S.A.
  • Year and Date: 2008-05-21
• [Patent(Industrial Property Rights)] (2008)
  • Inventor(s): 高山廣光、北島満里子、堀江俊治、松本健次郎
  • Industrial Property Rights Holder: 国立大学法人 千葉大学学校法人 城西大学
  • Industrial Property Number: 特許・PCT/JP2008/71689
  • Filing Date: 2008-11-28