Key Publications

AEAr Agonists

Key Review Articles 

Key Scientific  Articles

  • Grinnell, S. G. (2014). Pharmacologic Characterization in the Rat of a Potent Analgesic Lacking Respiratory Depression, IBNtxA. Journal of Pharmacology and Experimental Therapeutics, 350(3), 710–718. https://doi.org/10.1124/jpet.114.213199

  • Lu, Z. (2015). Mediation of opioid analgesia by a truncated 6-transmembrane GPCR. Journal of Clinical Investigation, 125(7), 2626–2630. https://doi.org/10.1172/jci81070

  • Majumdar, S. (2011). 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, 108(49), 19778–19783.https://doi.org/10.1073/pnas.1115231108

  • Majumdar, S., & Pasternak, A. R. (2011). Generation of novel radiolabeled opiates through site-selective iodination. Bioorganic & Medicinal Chemistry Letters, 21(13), 4001–4004. https://doi.org/10.1016/j.bmcl.2011.05.008

  • Majumdar, S., & Pasternak, A. R. (2012). Synthesis and Evaluation of Aryl-Naloxamide Opiate Analgesics Targeting Truncated Exon 11-Associated μ Opioid Receptor (MOR-1) Splice Variants. Journal of Medicinal Chemistry, 55(14), 6352–6362. https://doi.org/10.1021/jm300305c

  • Marrone, G. F. (2016a). Tetrapeptide Endomorphin Analogs Require Both Full Length and Truncated Splice Variants of the Mu Opioid Receptor Gene Oprm1 for Analgesia. ACS Chemical Neuroscience, 7(12), 1717–1727. https://doi.org/10.1021/acschemneuro.6b00240

  • Marrone, G. F. (2016b). Truncated mu opioid GPCR variant involvement in opioid-dependent and opioid-independent pain modulatory systems within the CNS. Proceedings of the National Academy of Sciences, 113(13), 3663–3668. https://doi.org/10.1073/pnas.1523894113

  • Wieskopf, J. S. (2014). Broad-spectrum analgesic efficacy of IBNtxA is mediated by exon 11-associated splice variants of the mu-opioid receptor gene. Pain, 155(10), 2063–2070.https://doi.org/10.1016/j.pain.2014.07.014

MOR / DOR Modulators

  • Váradi, A., et al.  (2016). Mitragynine /Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. Journal of Medicinal Chemistry, 59(18), 8381–8397. https://doi.org/10.1021/acs.jmedchem.6b00748

  • Wilson, L. L. et al. (2021). Kratom Alkaloids, Natural and Semi-Synthetic, Show Less Physical Dependence and Ameliorate Opioid Withdrawal. Cellular and Molecular Neurobiology, 992–1001. https://doi.org/10.1007/s10571-020-01034-7

  • Kruegel, A. C. et al. (2019). 7-Hydroxymitragynine Is an Active Metabolite of Mitragynine and a Key Mediator of Its Analgesic Effects. ACS Central Science, 5(6), 992–1001. https://doi.org/10.1021/acscentsci.9b00141

Irreversible MOR Antagonists

  • Dong, J. (2014b). Sulfur(VI) Fluoride Exchange (SuFEx): Another Good Reaction for Click Chemistry. Angewandte Chemie International Edition, 53(36), 9430–9448. https://doi.org/10.1002/anie.201309399

  • Leen, J. L. S. (2019). Carfentanil: a narrative review of its pharmacology and public health concerns. Canadian Journal of Anesthesia/Journal Canadien d’anesthésie, 66(4), 414–421. https://doi.org/10.1007/s12630-019-01294-y

  • Liu, Z. (2018). SuFEx Click Chemistry Enabled Late-Stage Drug Functionalization. Journal of the American Chemical Society, 140(8), 2919–2925. https://doi.org/10.1021/jacs.7b12788

Peripheral DOR Bitopic Agonists