Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder

@article{Fujimura2014CharacteristicsOT,
  title={Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder},
  author={Morihiro Fujimura and N. Izumimoto and Shinobu Momen and Satoru Yoshikawa and R. Kobayashi and S. Kanie and Mikito Hirakata and Toshikazu Komagata and S. Okanishi and Tadatoshi Hashimoto and N. Yoshimura and K. Kawai},
  journal={The Journal of Pharmacology and Experimental Therapeutics},
  year={2014},
  volume={350},
  pages={543 - 551}
}
  • Morihiro Fujimura, N. Izumimoto, +9 authors K. Kawai
  • Published 2014
  • Chemistry, Medicine
  • The Journal of Pharmacology and Experimental Therapeutics
  • We characterized TRK-130 (N-[(5R,6R,14S)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]phthalimide; naltalimide), an opioid ligand, to clarify the therapeutic potential for overactive bladder (OAB). In radioligand-binding assays with cells expressing human µ-opioid receptors (MORs), δ-opioid receptors (DORs), or κ-opioid receptors (KORs), TRK-130 showed high selectivity for MORs (Ki for MORs, DORs, and KORs = 0.268, 121, and 8.97 nM, respectively). In a functional assay (cAMP… CONTINUE READING
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