Research Topics
| William H BunnelleSummaryAffiliation: Abbott Laboratories Country: USA Publications
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Detail Information
Publications
Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing propertiesKarin R Tietje
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
CNS Neurosci Ther 14:65-82. 2008....- Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptorsWilliam H Bunnelle
Neuroscience Research, Abbott Laboratories, Department R47W, Building AP9A, Abbott Park, Illinois 60064 6117, USA
J Med Chem 50:3627-44. 2007.... - Design of ligands for the nicotinic acetylcholine receptors: the quest for selectivityWilliam H Bunnelle
Abbott Laboratories Global Pharmaceutical Research and Development, Department R47W, AP9A 1, Abbott Park, Illinois 60064, USA
Curr Top Med Chem 4:299-334. 2004..This paper provides an overview of the structure-affinity relationships that continue to drive development of new nAChR ligands... - Reagents for stereoselective preparation of N-carbamyl ?-D-glucuronidesWilliam H Bunnelle
Abbott Laboratories, Neuroscience Research, Building AP9A, Department R4MN, 100 Abbott Park Road, Abbott Park, Illinois 60064 6117, United States
J Org Chem 76:5429-32. 2011.... - 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... - In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107John Malysz
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064 6125, USA
J Pharmacol Exp Ther 334:863-74. 2010..In summary, ABT-107 is a selective high affinity alpha7 nAChR agonist suitable for characterizing the roles of this subtype in pharmacological studies... - Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonistsJianguo Ji
Neuroscience Research, R47W, AP9A 1, Abbott, Abbott Park, Illinois 60064, USA
J Med Chem 50:5493-508. 2007..The SAR studies of these novel ligands led to the discovery of several compounds with interesting in vitro pharmacological profiles... - Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligandsTao Li
Neuroscience Research, GPRD, Abbott, Abbott Park, IL 60064 6117, USA
Bioorg Med Chem Lett 20:3636-9. 2010..SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR agonist activity... - Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonistsJennifer M Frost
Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064, USA
J Med Chem 49:7843-53. 2006..e., 24, 25, 28, 30, 32, and 47) exhibit equivalent or greater affinity for the halpha4beta2 receptor relative to epibatidine, and like epibatidine, many exhibit robust analgesic efficacy in the rat formalin model of persistent pain... - In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's diseaseR Scott Bitner
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
J Pharmacol Exp Ther 334:875-86. 2010.... - Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptorsClark A Briggs
Neuroscience Research, Abbott Laboratories, Abbott Park, IL, USA
Br J Pharmacol 158:1486-94. 2009..The possibility that agonists of this receptor actually function in vivo as inhibitors via desensitization has not been finally resolved... - Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent ?4?2 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... - Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptorKathleen H Mortell
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 20:104-7. 2010..A potent and functionally efficacious analog, (3aR,6aS)-2-(6-phenylpyridazin-3-yl)-5-(pyridin-3-ylmethyl)octahydropyrrolo[3,4-c]pyrrole (3a), was identified... - Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptorsKevin B Sippy
Neuroscience Research, Abbott Laboratories, Department R47W, 100 Abbott Park Rd, Building AP9A, Abbott Park, IL 60064 6117, USA
Bioorg Med Chem Lett 19:1682-5. 2009..Nevertheless, some (1a, 1b) possessed (partial) agonist potencies comparable to nicotine at the alpha4beta2 subtype, but with greatly improved selectivity relative to the alpha3beta4* nAChR... - Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptorRamin Faghih
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
J Med Chem 52:3377-84. 2009..In a rodent model of sensory gating, 19 normalized gating deficits. These results suggest that 19 represents a novel class of molecules capable of allosteric modulation of the alpha7 nAChRs... - SAR of ?7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophoreMichael R Schrimpf
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Dept R4DE, Bldg AP9A, 100 Abbott Park Road, Abbott Park, IL 60064 6117, USA
Bioorg Med Chem Lett 22:1633-8. 2012..Analogs in which the fluorenone core is replaced with either dibenzothiophene-5,5-dioxide or xanthenone also retain potent activity... - A-366833: a novel nicotinonitrile-substituted 3,6-diazabicyclo[3.2.0]-heptane alpha4beta2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in animal modelsJianguo Ji
Neuroscience Research, Department R47W, Bldg AP9A, Global Pharmaceutical Research and Development, Abbott, Abbott Park, IL 60064, USA
Biochem Pharmacol 74:1253-62. 2007..These studies indicate that compounds like A-366833 with improved agonist selectivity at alpha4beta2 vs. alpha3beta4 nAChR can elicit a broad spectrum of analgesic efficacy without concurrent adverse effects... - Role of ?7 nicotinic acetylcholine receptors in regulating tumor necrosis factor-? (TNF-?) as revealed by subtype selective agonistsJinhe Li
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, United States
J Neuroimmunol 239:37-43. 2011..These studies collectively demonstrate that selectively targeting ?7 nAChRs could offer a novel therapeutic modality to treat acute and chronic inflammatory disease states... - Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-aminoethoxy)pyridine as novel nicotinic receptor ligandsNan horng Lin
Neurological and Urological Diseases Research, D 47W, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064 3500, USA
Bioorg Med Chem Lett 12:3321-4. 2002..The substituted analogues exhibited K(i) values ranging from 0.076 to 319 nM compared to a K(i) value of 26 nM for compound 1. Among the compounds tested, 5'-vinyl-6'-chloro substituted 1 was the most potent... - In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profileJohn Malysz
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064 6125, USA
J Pharmacol Exp Ther 330:257-67. 2009..In summary, this study identifies a novel and selective alpha7 PAM showing activity at recombinant and native alpha7 nAChRs exhibiting a unique pharmacological interaction with the receptor... - Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathwaysRobert S Bitner
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
J Neurosci 27:10578-87. 2007.... - Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonistRobert J Altenbach
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6123, USA
J Med Chem 47:3220-35. 2004..However, the data also support a prominent role of the alpha(1A)-AR subtype in the control of MAP... - (L)-Phenylglycine, but not necessarily other alpha2delta subunit voltage-gated calcium channel ligands, attenuates neuropathic pain in ratsJames J Lynch
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
Pain 125:136-42. 2006..These results suggest that additional mechanisms, besides alpha2delta interactions, may contribute to the effects of compounds like gabapentin, pregabalin and (L)-phenylglycine in neuropathic pain... - 6-Chloropyridazin-3-yl derivatives active as nicotinic agents: synthesis, binding, and modeling studiesLucio Toma
Dipartimento di Chimica Organica, , Via Taramelli 10, 27100 Pavia, Italy
J Med Chem 45:4011-7. 2002..Thus, this SAR study gives support to the hypothesis that these longer distances are still compatible with affinity for alpha4beta2 receptors in the nanomolar range...