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| Formula | C28H28N2O5 |
| Molar mass | 472.541 g·mol−1 |
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Naltalimide (INN; development codeTRK-130, formerlyTAK 363) is a novel,centrally-actingopioiddrug which is under development byTakeda andToray for the treatment ofoveractive bladder/urinary incontinence.[1][2] It acts as a potent and selectivepartial agonist of theμ-opioid receptor (Ki = 0.268 nM,EC50 = 2.39 nM,Emax = 66.1%) over theδ-opioid (Ki = 121 nM,EC50 = 26.1 nM,Emax = 71.0%) andκ-opioid receptors (Ki = 8.97 nM,EC50 = 9.51 nM,Emax = 62.6%).[1] Notably, naltalimide somehow appears to lack certain undesirableside effects such asconstipation seen with other μ-opioid receptor agonists such asmorphine.[1] It enhancesbladder storage via suppression of the afferent limb of themicturition reflex pathway.[1]
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