| Autor: |
Bunnelle WH; Department R47W, Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064-6117, USA. William.h.bunnelle@abbott.com, Tietje KR, Frost JM, Peters D, Ji J, Li T, Scanio MJ, Shi L, Anderson DJ, Dyhring T, Grønlien JH, Ween H, Thorin-Hagene K, Meyer MD |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2009 Jul 23; Vol. 52 (14), pp. 4126-41. |
| DOI: |
10.1021/jm900249k |
| Abstrakt: |
A series of 5-(pyridine-3-yl)octahydropyrrolo[3,4-c]pyrroles have been prepared that exhibit high affinity to alpha4beta2 and/or alpha7 nicotinic acetylcholine receptors (nAChRs). Simple substitution patterns have been identified that allow construction of ligands that are highly selective for either nAChR subtype. 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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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