Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.
作者信息
Löber Stefan, Aboul-Fadl Tarek, Hübner Harald, Gmeiner Peter
机构信息
Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052, Erlangen, Germany.
出版信息
Bioorg Med Chem Lett. 2002 Feb 25;12(4):633-6. doi: 10.1016/s0960-894x(01)00814-9.
Abstract
Based on the lead molecule FAUC 113, a series of di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives was synthesized and investigated for their dopamine receptor binding profile. The carbonitrile 11a (FAUC 327) showed excellent pharmacological properties combining high D4 affinity (K(i)=1.5 nM) and selectivity with significant intrinsic activity (31%) in low nanomolar concentrations (EC50=1.5 nM).
摘要
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