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 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},
  year={2014},
  volume={350},
  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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Discovery of highly selective κ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.
Mechanisms of inhibitory action of TRK-130 (Naltalimide), a μ-opioid receptor partial agonist, on the micturition reflex
TLDR
It is suggested that TRK-130 enhances the bladder storage function by modulating the afferent limb of the micturition reflex through µ-opioid receptors in the spinal cord with a different fashion from antimuscarinics and conventional opioids for overactive bladder.
β3-Adrenoceptor agonists for overactive bladder syndrome: Role of translational pharmacology in a repositioning clinical drug development project.
The phthalimide analogues N-3-hydroxypropylphthalimide and N-carboxymethyl-3-nitrophthalimide exhibit activity in experimental models of inflammatory and neuropathic pain.
Endogenous opiates and behavior: 2014
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Emerging drugs for overactive bladder
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Long-term data for mirabegron has shown that it is more effective in severe OAB, and combinations of antimuscarinics, β3-agonists and antidiuretics may prove to be more effective with less adverse effects.
Astragalus polysaccharides and astragaloside IV ameliorates cyclophosphamide-induced mouse model of overactive bladder.
Efficacy of Frankincense and Myrrha in Treatment of Acute Interstitial Cystitis/Painful Bladder Syndrome
TLDR
Frankincense and myrrha modulate urothelial wound healing, which ameliorates typical features of acute IC/PBS in rats, and increased cell proliferation and migration in HUCs compared with control.
Platelet-Rich Plasma Ameliorates Cyclophosphamide-Induced Acute Interstitial Cystitis/Painful Bladder Syndrome in a Rat Model
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It is suggested that PRP modulate urothelial repair, which ameliorate the increase in urination frequency in rats treated with CYP and may confer potential benefits by acting as urobaric repair modulators.
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