• Bioorg. Med. Chem. Lett. · Jul 2014

    DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.

    • Parthasarathi Rajagopalan, Heather Tracey, Zhoumou Chen, Acintya Bandyopadhyaya, Sridhar Veeraraghavan, Desikan R Rajagopalan, Daniela Salvemini, Ian McPhee, Srikant Viswanadha, and Raghavan Rajagopalan.
    • Daya Drug Discoveries, Inc., University of Missouri, St. Louis, One University Blvd., St. Louis, MO 63121, USA.
    • Bioorg. Med. Chem. Lett. 2014 Jul 15;24(14):3088-91.

    AbstractDDD-028 (4), a novel pentacyclic pyridoindolobenzazepine derivative was evaluated in vitro for receptor binding affinity and in vivo for analgesic activity using rodent models of neuropathic and inflammatory pain. DDD-028 does not bind to opioid, cannabinoid, dopamine, or histamine receptors. DDD-028 is very active even at the low oral dose of 1-5 mg/kg in both neuropathic, (spinal nerve ligation and chronic constriction injury) and inflammatory (Complete Freund's Adjuvant Induced) models of pain. DDD-028 appears to be about 6-fold more potent than pregabalin and indomethacin. Visual observation of all the animals used in these studies indicated that DDD-028 is well tolerated without any sedation. Thus, DDD-028 seems to be a promising candidate for the treatment of neuropathic and inflammatory pain without the possible side effects or abuse potential associated with opioid or cannabinoid activities.Copyright © 2014 Elsevier Ltd. All rights reserved.

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