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7-Azaindole derivatives as potential partial nicotinic agonists. 2008
Axel R Stoit, and
Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
Solvay Pharmaceuticals, Research Laboratories, C.J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands. axel.stoit@solvay.com
We have investigated a series of 7-azaindoles as potential partial agonists of the alpha4beta2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (Ki = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation.
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Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
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Hiskias Keizer, and
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Sjoerd van Schaik, and
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October 2023,
European journal of medicinal chemistry,
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Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
April 2009,
The Journal of pharmacology and experimental therapeutics,
Axel R Stoit, and
Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
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Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
May 1963,
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Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
January 2008,
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Axel R Stoit, and
Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
February 2007,
Biochemical pharmacology,
Axel R Stoit, and
Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
March 2007,
Bioorganic & medicinal chemistry letters,
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Arnold P den Hartog, and
Harry Mons, and
Sjoerd van Schaik, and
Nynke Barkhuijsen, and
Cees Stroomer, and
Hein K A C Coolen, and
Jan Hendrik Reinders, and
Tiny J P Adolfs, and
Martina van der Neut, and
Hiskias Keizer, and
Chris G Kruse
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