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

  title={Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder},
  author={Morihiro Fujimura and Naoki Izumimoto and Shinobu Momen and Satoru Yoshikawa and Ryosuke Kobayashi and Sayoko Kanie and Mikito Hirakata and Toshikazu Komagata and Satoshi Okanishi and Tadatoshi Hashimoto and Naoki Yoshimura and Koji Kawai},
  journal={The Journal of Pharmacology and Experimental Therapeutics},
  pages={543 - 551}
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… 

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