Marc J C Scanio
Affiliation: Abbott Laboratories
- Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligandsMarc J C Scanio
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL, USA
J Med Chem 54:7678-92. 2011..3.0]octane)-substituted pyridines or 2-(diazabicyclo[3.3.0]octane)-substituted pyrazines were found to have the desired binding and activity profile. The structure-activity relationship of these compounds is presented...
- Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic painMarc J C Scanio
Global Pharmaceutical Research and Development, Abbott Laboratories, Dept R4PM, Bldg AP9A, 100 Abbott Park Road, Abbott Park, IL 60064 6117, United States
Bioorg Med Chem 18:7816-25. 2010..2. We further demonstrate that an example from this series is orally bioavailable and produces antinociceptive activity in vivo in a rodent model of neuropathic pain following oral administration...
- Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory painMichael E Kort
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6100, USA
J Med Chem 51:407-16. 2008..2, Nav1.5, Nav1.7) and human ether-a-go-go (hERG) channels. Following systemic administration, compounds 7 and 27 dose-dependently reduced neuropathic and inflammatory pain in experimental rodent models...
- Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic painIrene Drizin
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem 16:6379-86. 2008....
- Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivativesMichael E Kort
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6100, USA
Bioorg Med Chem Lett 20:6812-5. 2010..Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain...
- Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivityWilliam H Bunnelle
Department R47W, Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064 6117, USA
J Med Chem 52:4126-41. 2009..The effects of substitution on subtype selectivity provide some insight into the differences in the ligand binding domains of the alpha4beta2 and alpha7 receptors, especially in regions removed from the cation binding pocket...
- Voltage-gated sodium channel blockers for the treatment of chronic painMark A Matulenko
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6100, USA
Curr Top Med Chem 9:362-76. 2009..This review will focus on the latest advances in the development of small molecule sodium channel blockers and their application to the treatment of chronic pain...
- A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic ratsSteve McGaraughty
Neuroscience Research, Abbott Laboratories, R4PM, AP9 1, 100 Abbott Park Rd, Abbott Park, IL 60064 6118, USA
J Pharmacol Exp Ther 324:1204-11. 2008..However, Na(v)1.8 sodium channels on central terminals seem to be key to the modulation of spontaneous firing in SNL rats...