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

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

  • Bioorg Med Chem Lett. 2014 Jul 15;24(14):3088-91. doi: 10.1016/j.bmcl.2014.05.016.
Parthasarathi Rajagopalan 1,  Heather Tracey 2,  Zhoumou Chen 3,  Acintya Bandyopadhyaya 1,  Sridhar Veeraraghavan 4,  Desikan R Rajagopalan 1,  Daniela Salvemini 3,  Ian McPhee 2,  Srikant Viswanadha 4,  Raghavan Rajagopalan 5
Affiliations

Affiliations

  • 1 Daya Drug Discoveries, Inc., University of Missouri, St. Louis, One University Blvd., St. Louis, MO 63121, USA.
  • 2 SB Drug Discovery, Ltd, Todd Campus, West of Scotland Science Park, Glasgow, Scotland G20 0XA, UK.
  • 3 Department of Pharmacological and Physiological Sciences, St. Louis University School of Medicine, 1402 South Grand Blvd., St. Louis, MO 63104, USA.
  • 4 Incozen Therapeutics, Ltd, 450 Alexandria Knowledge Park, Hyderabad 500078, Andhra Pradesh, India.
  • 5 Daya Drug Discoveries, Inc., University of Missouri, St. Louis, One University Blvd., St. Louis, MO 63121, USA. Electronic address: raghavanr@daya-dd.com.
PMID: 24863744 DOI: 10.1016/j.bmcl.2014.05.016
Abstract

DDD-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.

Keywords

CCI model; Inflammatory pain; Neuropathic pain; Pyridoinolobenzazepine; SNL model.

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