Naltalimide
 | |
| Systematic (IUPAC) name | |
|---|---|
| 2-[(5α,6β)-17-(Cyclopropylmethyl)-3,14-dihydroxy-4,5-epoxymorphinan-6-yl]-1H-isoindole-1,3(2H)-dione | |
| Clinical data | |
| Identifiers | |
| 160359-68-2 | |
| None | |
| PubChem | CID 16066809 |
| ChemSpider | 17226389 |
| Chemical data | |
| Formula | C28H28N2O5 |
| 472.532 g/mol | |
|
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Naltalimide (INN) (code name TRK-130, formerly TAK 363) is a novel, centrally-acting opioid drug which is under development by Takeda and Toray for the treatment of overactive bladder/urinary incontinence.[1][2] It acts as a potent and selective partial agonist of the μ-opioid receptor (Ki = 0.268 nM, EC50 = 2.39 nM, Emax = 66.1%) over the δ-opioid (Ki = 121 nM, EC50 = 26.1 nM, Emax = 71.0%) and κ-opioid receptors (Ki = 8.97 nM, EC50 = 9.51 nM, Emax = 62.6%).[1] Notably, naltalimide somehow appears to lack certain undesirable side effects such as constipation seen with other μ-opioid receptor agonists such as morphine.[1] It enhances bladder storage via suppression of the afferent limb of the micturition reflex pathway.[1]
References
- ↑ 1.0 1.1 1.2 1.3 Fujimura, M.; Izumimoto, N.; Momen, S.; Yoshikawa, S.; Kobayashi, R.; Kanie, S.; Hirakata, M.; Komagata, T.; Okanishi, S.; Hashimoto, T.; Yoshimura, N.; Kawai, K. (2014). "Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder". Journal of Pharmacology and Experimental Therapeutics 350 (3): 543–551. doi:10.1124/jpet.114.214031. ISSN 1521-0103.
- ↑ http://business.highbeam.com/436989/article-1G1-131689504/trk-130-takeda-toray-licensing-agreement