2. Academic Validation
  3. Synthesis of resveratrol derivatives as new analgesic drugs through desensitization of the TRPA1 receptor

Synthesis of resveratrol derivatives as new analgesic drugs through desensitization of the TRPA1 receptor

  • Bioorg Med Chem Lett. 2017 Jul 15;27(14):3167-3172. doi: 10.1016/j.bmcl.2017.05.025.
Syuhei Nakao 1,  Miyuki Mabuchi 2,  Shenglan Wang 3,  Yoko Kogure 4,  Tadashi Shimizu 1,  Koichi Noguchi 5,  Akito Tanaka 6,  Yi Dai 7
Affiliations

Affiliations

  • 1 Advanced Medical Research Center, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan; School of Pharmacy, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan.
  • 2 Advanced Medical Research Center, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan.
  • 3 School of Pharmacy, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan; Traditional Medicine Research Center, Chinese Medicine Confucius Institute at Hyogo College of Medicine, Kobe 650-8530, Japan.
  • 4 School of Pharmacy, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan.
  • 5 Department of Anatomy and Neuroscience, Hyogo College of Medicine, Nishinomiya, Hyogo 663-8501, Japan.
  • 6 Advanced Medical Research Center, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan; School of Pharmacy, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan. Electronic address: tanaka-a@huhs.ac.jp.
  • 7 School of Pharmacy, Hyogo University of Health Sciences, 1-3-6 Minatojima, Kobe 650-8530, Japan; Traditional Medicine Research Center, Chinese Medicine Confucius Institute at Hyogo College of Medicine, Kobe 650-8530, Japan; Department of Anatomy and Neuroscience, Hyogo College of Medicine, Nishinomiya, Hyogo 663-8501, Japan. Electronic address: ydai@huhs.ac.jp.
PMID: 28576617 DOI: 10.1016/j.bmcl.2017.05.025
Abstract

A series of 31 resveratrol derivatives was designed, synthesized and evaluated for activation and inhibition of the TRPA1 channel. Most acted as activators and desensitizers of TRPA1 channels like resveratrol or allyl isothiocyanate (AITC). Compound 4z (HUHS029) exhibited higher inhibitory activity than resveratrol with an IC50 value of 16.1μM. The activity of 4z on TRPA1 was confirmed in TRPA1-expressing HEK293 cells, as well as in rat dorsal root ganglia neurons by a whole cell patch clamp recording. Furthermore, pretreatment with 4z exhibited an analgesic effect on AITC-evoked TRPA1-related pain behavior in vivo.

Keywords

Analgesic drug; HUHS029; Resveratrol; TRPA1.

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