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

Abstract

We characterized 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 m-opioid receptors (MORs), d-opioid receptors (DORs), or k-opioid receptors (KORs), TRK-130 showed high selectivity for MORs (K i for MORs, DORs, and KORs 5 0.268, 121, and 8.97 nM, respectively). In a functional assay (cAMP accumulation) with cells expressing each human opioid receptor subtype, TRK-130 showed potent but partial agonistic activity for MORs [EC 50 (E max )

Platelet-Rich Plasma Ameliorates Cyclophosphamide-Induced Acute Interstitial Cystitis/Painful Bladder Syndrome in a Rat Model

“…Our study has certain limitations: (1) the pelvic floor structure of the rat, which is a quadruped and has a lax abdominal wall, is different from that of a human female [31]; therefore, the results of this study need to be carefully employed to humans; (2) urodynamic studies were conducted under anesthesia [32]; nevertheless, the preoperative fasting water was not restricted; (3) the effects of PRP on proliferation, maturation, and differentiation of undifferentiated urothelial cells were not observed separately in vitro in the present study; (4) this rat model generated by a single intraperitoneal injection of CYP is an acute IC/PBS model, while human IC/PBS is a chronic disease. It may be the case that several models, each contributing to a piece of the puzzle, are required to recreate a reasonable picture of the pathophysiology and time course of the disease(s) diagnosed as IC/PBS, and thus to identify reasonable targets for treatment [29].…”

Emerging drugs for overactive bladder

“…A Phase II trial on µ-opioid receptor agonist KN203 has ended prematurely. Studies on novel opioid agents with negligible effect on gastrointestinal transit are at the preclinical stage [78].…”