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Key Publications

AEAr Agonists

Review Articles

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
  • Lu, Z. (2018). Truncated μ-Opioid Receptors With 6 Transmembrane Domains Are Essential for Opioid Analgesia. Anesthesia & Analgesia, 126(3), 1050–1057. https://doi.org/10.1213/ane.0000000000002538
  • ​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. (2015). Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target. Methods in Molecular Biology, 241–249. https://doi.org/10.1007/978-1-4939-2914-6_16
  • 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 Partial Agonist / DOR Antagonists

  • 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

Sigma Antagonist / DAT Inhibitor

  • Katz, J. L., Hiranita, T., Hong, W. C., Job, M. O., & McCurdy, C. R. (2017). A role for sigma receptors in stimulant self-administration and addiction. Handbook of Experimental Pharmacology, 177–218. https://doi.org/10.1007/978-3-319-55765-9_8
  • Matsumoto, R. R., Nguyen, L., Kaushal, N., & Robson, M. J. (2014). Sigma (σ) receptors as potential therapeutic targets to mitigate psychostimulant effects. Advances in Pharmacology, 69, 323–386. https://doi.org/10.1016/B978-0-12-420118-7.00009-3
  • Hiranita, T., Soto, P. L., Kohut, S. J., Kopajtic, T., Cao, J., Newman, A. H., Tanda, G., & Katz, J. L. (2011). Decreases in cocaine self-administration with dual inhibition of the dopamine transporter and σ receptors. Journal of Pharmacology and Experimental Therapeutics, 339(2), 662–677. https://doi.org/10.1124/jpet.111.185025
  • Martin-Fardon, R., Maurice, T., Aujla, H., Bowen, W. D., & Weiss, F. (2007). Differential effects of sigma1 receptor blockade on self-administration and conditioned reinstatement motivated by cocaine vs natural reward. Neuropsychopharmacology, 32(9), 1967–1973. https://doi.org/10.1038/sj.npp.1301323
  • Katz, J. L., Hiranita, T., Kopajtic, T. A., Rice, K. C., Mesangeau, C., Narayanan, S., Abdelazeem, A. H., & McCurdy, C. R. (2016). Blockade of cocaine or σ receptor agonist self-administration by subtype-selective σ receptor antagonists. Journal of Pharmacology and Experimental Therapeutics, 358(1), 109–124. https://doi.org/10.1124/jpet.116.232728
  • Ritz, M. C., Lamb, R. J., Goldberg, S. R., & Kuhar, M. J. (1987). Cocaine receptors on dopamine transporters are related to self-administration of cocaine. Science, 237(4819), 1219–1223. https://doi.org/10.1126/science.2820058
  • Gilmore, D. L., Liu, Y., & Matsumoto, R. R. (2004). Review of the pharmacological and clinical profile of rimcazole. CNS Drug Reviews, 10(1), 1–22. https://doi.org/10.1111/j.1527-3458.2004.tb00001.x
  • Katz, J. L., Libby, T. A., Kopajtic, T., Husbands, S. M., & Newman, A. H. (2003). Behavioral effects of rimcazole analogues alone and in combination with cocaine. European Journal of Pharmacology, 468(2), 109–119. https://doi.org/10.1016/s0014-2999(03)01638-8
  • Pontieri, F. E., Tanda, G., & Di Chiara, G. (1995). Intravenous cocaine, morphine, and amphetamine preferentially increase extracellular dopamine in the ‘shell’ as compared with the ‘core’ of the rat nucleus accumbens. Proceedings of the National Academy of Sciences, 92(26), 12304–12308. https://doi.org/10.1073/pnas.92.26.12304
  • Mereu, M., et al. (2012). Rimcazole attenuates the cocaine-induced stimulation of mesolimbic dopamine related to its abuse and dependence. FASEB Journal, 26, 659.4. [Unpublished Meeting Abstract].
  • Loland, C. J., Desai, R. I., Zou, M. F., Cao, J., Grundt, P., Gerstbrein, K., Sitte, H. H., Newman, A. H., Katz, J. L., & Gether, U. (2008). Relationship between conformational changes in the dopamine transporter and cocaine-like subjective effects of uptake inhibitors. Molecular Pharmacology, 73(3), 813–823. https://doi.org/10.1124/mol.107.039800
  • Katz, J. L., Su, T. P., Hiranita, T., Hayashi, T., Tanda, G., Kopajtic, T., & Tsai, S. Y. (2011). A role for sigma receptors in stimulant self-administration and addiction. Pharmaceuticals (Basel), 4(6), 880–914. https://doi.org/10.3390/ph4060880
  • Hiranita, T., Kohut, S. J., Soto, P. L., Tanda, G., Kopajtic, T. A., & Katz, J. L. (2014). Preclinical efficacy of N-substituted benztropine analogs as antagonists of methamphetamine self-administration in rats. Journal of Pharmacology and Experimental Therapeutics, 348(1), 174–191. https://doi.org/10.1124/jpet.113.208264
  • Xu, Y. T., Kaushal, N., Shaikh, J., Wilson, L. L., Mésangeau, C., McCurdy, C. R., & Matsumoto, R. R. (2010). A novel substituted piperazine, CM156, attenuates the stimulant and toxic effects of cocaine in mice. Journal of Pharmacology and Experimental Therapeutics, 333(2), 491–500. https://doi.org/10.1124/jpet.109.161398
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