Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333
2012
Beinat, Corinne | Banister, Samuel D. | van Prehn, Saundra | Doddareddy, Munikumar Reddy | Hibbs, David | Sako, Michael | Chebib, Mary | Tran, Thao | Al-Muhtasib, Nour | Xiao, Yingxian | Kassiou, Michael
A series of ligands based on SEN12333, containing either contracted or elongated alkyl chains, were synthesized and evaluated in molecular docking studies against a homology model of the α7 nicotinic acetylcholine receptor (nAChR) subtype. The predicted binding of all ligands was highly similar, with the exception of the analog containing a 5 methylene unit spacer. However, in vitro competition binding assays revealed that the ligands possessed dissimilar binding affinities, with a Kᵢ range of more than an order of magnitude (Kᵢ=0.50 to >10μM), and only SEN12333 itself exhibited functional activity at the α7 nAChR.
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