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IBNtxA

IBNtxA
IBNtxA structure.png
Clinical data
ATC code
  • none
Identifiers
PubChem CID
ChemSpider
Chemical and physical data
FormulaC27H29IN2O4
Molar mass572.434 g/mol g·mol−1
3D model (JSmol)

IBNtxA, or 3-iodobenzoyl naltrexamine, is an atypical opioid analgesic drug derived from naltrexone. In animal studies it produces potent analgesic effects that are blocked by levallorphan and so appear to be μ-opioid mediated, but it fails to produce constipation or respiratory depression, and is neither rewarding or aversive in conditioned place preference protocols. These unusual properties are thought to result from agonist action at a splice variant or heterodimer of the μ-opioid receptor, rather than at the classical full length form targeted by conventional opioid drugs.[1][2][3][4][5]

References

  1. ^ Majumdar S, Grinnell S, Le Rouzic V, Burgman M, Polikar L, Ansonoff M, Pintar J, Pan YX, Pasternak GW. Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects. Proceedings of the National Academy of Sciences USA. 2011 Dec 6;108(49):19778-83. PMID 22106286
  2. ^ Majumdar S, Subrath J, Le Rouzic V, Polikar L, Burgman M, Nagakura K, Ocampo J, Haselton N, Pasternak AR, Grinnell S, Pan YX, Pasternak GW (2012). "Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associated μ opioid receptor (MOR-1) splice variants". J. Med. Chem. 55 (14): 6352–62. doi:10.1021/jm300305c. PMC 3412067. PMID 22734622.
  3. ^ Wieskopf JS, Pan YX, Marcovitz J, Tuttle AH, Majumdar S, Pidakala J, Pasternak GW, Mogil JS (2014). "Broad-spectrum analgesic efficacy of IBNtxA is mediated by exon 11-associated splice variants of the mu-opioid receptor gene". Pain. 155 (10): 2063–70. doi:10.1016/j.pain.2014.07.014. PMC 4372857. PMID 25093831.
  4. ^ Grinnell SG, Majumdar S, Narayan A, Le Rouzic V, Ansonoff M, Pintar JE, Pasternak GW (2014). "Pharmacologic characterization in the rat of a potent analgesic lacking respiratory depression, IBNtxA". J. Pharmacol. Exp. Ther. 350 (3): 710–8. doi:10.1124/jpet.114.213199. PMC 4152881. PMID 24970924.
  5. ^ Keck TM, Uddin MM, Babenko E, Wu C, Moura-Letts G. Abuse Liability and Anti-Addiction Potential of the Atypical Mu Opioid Receptor Agonist IBNtxA. The FASEB Journal 31 (1 Supplement), 985.4-985.4, 2017