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Naltalimide
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Naltalimide : ウィキペディア英語版
Naltalimide

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.〔http://business.highbeam.com/436989/article-1G1-131689504/trk-130-takeda-toray-licensing-agreement〕 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%).〔 Notably, naltalimide somehow appears to lack certain undesirable side effects such as constipation seen with other μ-opioid receptor agonists such as morphine.〔 It enhances bladder storage via suppression of the afferent limb of the micturition reflex pathway.〔
==References==



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