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Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in
Compound 14 is a potent and selective alpha7 nAChR agonist with an excellent in vitro profile and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition. Expand
Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists.
A two-pronged approach was taken to improve the potential hERG liability of previously disclosed alpha7 nAChR agonist, PNU-282,987, while maintaining the compound's other desirable pharmacological properties. Expand
Continuous administration decreases and pulsatile administration increases behavioral sensitivity to a novel dopamine D2 agonist (U-91356A) in MPTP-exposed monkeys.
It is confirmed that the mode of administration of dopaminergic agents may result in a markedly different clinical outcome, and a tendency toward upregulation of putaminal D1 receptors was observed in the levodopa-treated, dyskinetic animals. Expand
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.
A novel alpha7 nAChR agonist, N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (3a, PHA-709829), has been identified for the potential treatment of cognitive deficits inExpand
Optimization of protein immobilization on 1,1′-carbonyldiimidazole-activated diol-bonded silica
Abstract The activation of diol-bonded silica with 1,1′-carbonyldiimidazole and the coupling of protein ligands was examined as a function of activation conditions, coupling time, buffer, and pH. ItExpand
Affinity chromatographic examination of a retention model for macromolecules.
Plots of log k' vs. log (1/[mobile phase modifier]) were made for a monovalent and a divalent solute using affinity chromatography and all exhibited slopes (Z values) of less than the theoretical integer values. Expand
Protein diffusion coefficient measurements by laminar flow analysis: method and applications.
The translational diffusion coefficient of a solute can be calculated from the band dispersion, tube length, and flow rate, and the amount of protein needed was approximately 25 micrograms. Expand
Peak-decay method for the measurement of dissociation rate constants by high-performance affinity chromatography
Abstract A new method was described for the measurement of dissociation rate constants of biological complexes by affinity chromatography. Theory and computer modeling were used to establishExpand
Improved enantioselective method for the determination of the enantiomers of reboxetine in plasma by solid-phase extraction, chiral derivatization, and column-switching high-performance liquid
A rapid enantioselective method is described for the quantitation of the reboxetine (R,R)- and (S,S)-enantiomers in plasma utilizing solid-phase extraction, derivatization, normal-phaseExpand
Progress toward the development of a safe and effective agent for treating reentrant cardiac arrhythmias: synthesis and evaluation of ibutilide analogues with enhanced metabolic stability and
A series of ibutilide analogues with fluorine substituents on the heptyl side chain was prepared and evaluated and one compound had excellent antiarrhythmic activity and metabolic stability and was devoid of proarrhythmmic activity in the rabbit model and was chosen for further development. Expand