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Management Team

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Sparian

Biosciences

Key Publications

AEAr Agonists

Key Review Articles

Pasternak, G. W. (2018). Mu Opioid Pharmacology: 40 Years to the Promised Land. Advances in Pharmacology, 261–291.https://doi.org/10.1016/bs.apha.2017.09.006

Pasternak, G. W. (2014). Opiate Pharmacology and Relief of Pain. Journal of Clinical Oncology, 32(16), 1655–1661. https://doi.org/10.1200/jco.2013.53.1079

Pasternak, G. W. (2014b). Opioids and their receptors: Are we there yet? Neuropharmacology, 76, 198–203. https://doi.org/10.1016/j.neuropharm.2013.03.039

Pasternak, G. W. (2013). Mu Opioids and Their Receptors: Evolution of a Concept. Pharmacological Reviews, 65(4), 1257–1317. https://doi.org/10.1124/pr.112.007138

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

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 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

Dong, J. (2014a). SuFEx-Based Synthesis of Polysulfates. Angewandte Chemie International Edition, 53(36), 9466–9470. https://doi.org/10.1002/anie.201403758

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

Katritch, V. (2011). Ligand-Guided Receptor Optimization. Methods in Molecular Biology, 189–205. https://doi.org/10.1007/978-1-61779-588-6_8

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

Moss, R. B. (2019). Higher doses of naloxone are needed in the synthetic opioid era. Substance Abuse Treatment, Prevention, and Policy, 14(1), x. https://doi.org/10.1186/s13011-019-0195-4

Rzasa Lynn, R. (2017). Naloxone dosage for opioid reversal: current evidence and clinical implications. Therapeutic Advances in Drug Safety, 9(1), 63–88. https://doi.org/10.1177/2042098617744161

Suffoletto, B. (2020). Risk and protective factors for repeated overdose after opioid overdose survival. Drug and Alcohol Dependence, 209, 107890. https://doi.org/10.1016/j.drugalcdep.2020.107890

Sutter, M. E. (2016). Fatal Fentanyl: One Pill Can Kill. Academic Emergency Medicine, 24(1), 106–113. https://doi.org/10.1111/acem.13034

Weiner, S. G. (2020). One-Year Mortality of Patients After Emergency Department Treatment for Nonfatal Opioid Overdose. Annals of Emergency Medicine, 75(1), 13–17. https://doi.org/10.1016/j.annemergmed.2019.04.020

Peripheral DOR Bitopic Agonists

Benbouzid, M. (2008). Delta-Opioid Receptors Are Critical for Tricyclic Antidepressant Treatment of Neuropathic Allodynia. Biological Psychiatry, 63(6), 633–636. https://doi.org/10.1016/j.biopsych.2007.06.016

Fenalti, G. (2014). Molecular control of δ-opioid receptor signalling. Nature, 506(7487), 191–196. https://doi.org/10.1038/nature12944

Saloman, J. L. (2011). Activation of peripheral delta-opioid receptors leads to anti-hyperalgesic responses in the masseter muscle of male and female rats. Neuroscience, 190, 379–385. https://doi.org/10.1016/j.neuroscience.2011.05.062

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