Deekonda2016 Explained

Deekonda2016 is a piperidine-based opioid analgesic compound, developed through modification of the fentanyl scaffold and with similar potency to fentanyl. It was designed as a mixed μ/δ opioid agonist but is much more selective for the μ-opioid receptor, with a binding affinity of 4 nM.[1] [2] [3] [4]

See also

Notes and References

  1. Deekonda S, Wugalter L, Kulkarni V, Rankin D, Largent-Milnes TM, Davis P, Bassirirad NM, Lai J, Vanderah TW, Porreca F, Hruby VJ . Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands . Bioorganic & Medicinal Chemistry . 23 . 18 . 6185–6194 . September 2015 . 10.1016/j.bmc.2015.07.071 . 26299827 . 4642887 .
  2. Deekonda S, Rankin D, Davis P, Lai J, Vanderah TW, Porecca F, Hruby VJ . Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands . Bioorganic & Medicinal Chemistry . 24 . 2 . 85–91 . January 2016 . 10.1016/j.bmc.2015.11.030 . 26712115 . 4873254 .
  3. Lipiński PF, Kosson P, Matalińska J, Roszkowski P, Czarnocki Z, Jarończyk M, Misicka A, Dobrowolski JC, Sadlej J . Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis . Molecules . 24 . 4 . February 2019 . 740 . 10.3390/molecules24040740 . free . 30791394 . 6412969 .
  4. Wu Z, Hruby VJ . Toward a Universal μ-Agonist Template for Template-Based Alignment Modeling of Opioid Ligands . ACS Omega . 4 . 17 . 17457–17476 . October 2019 . 10.1021/acsomega.9b02244 . 31656918 . 6812133 .