Naltalimide

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Naltalimide
Naltalimide.svg
Systematic (IUPAC) name
2-[(5α,6β)-17-(Cyclopropylmethyl)-3,14-dihydroxy-4,5-epoxymorphinan-6-yl]-1H-isoindole-1,3(2H)-dione
Identifiers
CAS Number 160359-68-2
ATC code None
PubChem CID: 16066809
ChemSpider 17226389
Chemical data
Formula C28H28N2O5
Molecular mass 472.532 g/mol
  • c1ccc2c(c1)C(=O)N(C2=O)[C@@H]3CC[C@]4([C@H]5Cc6ccc(c7c6[C@]4([C@H]3O7)CCN5CC8CC8)O)O
  • InChI=1S/C28H28N2O5/c31-20-8-7-16-13-21-28(34)10-9-19(30-25(32)17-3-1-2-4-18(17)26(30)33)24-27(28,22(16)23(20)35-24)11-12-29(21)14-15-5-6-15/h1-4,7-8,15,19,21,24,31,34H,5-6,9-14H2/t19-,21-,24+,27+,28-/m1/s1
  • Key:DHAITNWJDOSRBU-IBHWKQIPSA-N

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. ↑ 1.0 1.1 1.2 1.3 Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ http://business.highbeam.com/436989/article-1G1-131689504/trk-130-takeda-toray-licensing-agreement


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