PHENYL PYRROLIDINE ANALOGS AS POTENT NICOTINIC ACETYLCHOLINE-RECEPTOR (NACHR) LIGANDS
PHENYL PYRROLIDINE ANALOGS AS POTENT NICOTINIC ACETYLCHOLINE-RECEPTOR (NACHR) LIGANDS
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DOI：
10.1016/0960-894x(95)00154-l
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发表时间：
1995-05-04
影响因子：
2.7
通讯作者：
GARVEY, DS
中科院分区：
文献类型：
--
作者：
ELLIOTT, RL;RYTHER, KB;GARVEY, DS
本文报道了一系列2-苯基吡咯烷类神经元nAChR配体的合成和构效关系。芳基环上的取代对受体结合亲和力具有显著影响，Ki值范围为46 nM至> 10，000 nM。类似物8、9和14是评价的最有效的配体，其Ri值分别为68 nM、75 nM和46 nM。
The synthesis and SAR of a series of 2-phenyl pyrrolidines as neuronal nAChR ligands are described. Substitution on the aryl ring had a dramatic effect on receptor binding affinity, with K-i values ranging from 46 nM to >10,000 nM. Analogues 8, 9, and 14 were the most potent ligands evaluated, having Ri values of 68 nM, 75 nM, and 46 nM; respectively.