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 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},
  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
    11 Citations
    Discovery of highly selective κ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.
    • 2
    Mechanisms of inhibitory action of TRK-130 (Naltalimide), a μ-opioid receptor partial agonist, on the micturition reflex
    • 3
    Endogenous opiates and behavior: 2014
    • 108
    A promising protein responsible for overactive bladder in ovariectomized mice.
    • 5
    Emerging drugs for overactive bladder
    • 6
    Efficacy of Frankincense and Myrrha in Treatment of Acute Interstitial Cystitis/Painful Bladder Syndrome


    Effects of WAY100635, a selective 5-HT1A-receptor antagonist on the micturition-reflex pathway in the rat.
    • 61
    • Highly Influential
    • PDF
    Effects of TAK-637, a tachykinin receptor antagonist, on the micturition reflex in guinea pigs.
    • 20
    Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist.
    • 277
    • Highly Influential
    • PDF
    Pharmacological actions of AH-9700 on micturition reflex in anesthetized rats.
    • 5
    Role of dopamine D1 and D2 receptors in the micturition reflex in conscious rats
    • 108
    Opioid receptor subtypes involved in the central inhibition of urinary bladder motility.
    • 60
    Signal transduction correlates of mu opioid agonist intrinsic efficacy: receptor-stimulated [35S]GTP gamma S binding in mMOR-CHO cells and rat thalamus.
    • 150
    • Highly Influential
    • PDF
    Actions of tramadol on micturition in awake, freely moving rats
    • 46
    • Highly Influential
    Pharmacological evaluation of JO 1870: relation to the potential treatment of urinary bladder incontinence.
    • 7
    • Highly Influential