Synthesis and evaluation of phenylcarbamate derivatives as ligands for nicotinic acetylcholine receptors
- 作者：G脙脙ndisch ; Daniela ; Andr脙脙 ; Matthias ; Munoz ; Lenka ; Cristina Tilotta ; Maria
- 关键词：Phenylcarbamate ; Nicotinic acetylcholine receptor ; Epibatidine ; MLA (methyllycaconitine)
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2004
- 期刊代码：9_09680896
- 类别：ch
- 出版时间：September 15, 2004
- 卷：12
- 期：18
- 页码：4953-4962
- 文件大小：344 K
摘要
Phenylcarbamate derivatives were synthesized and evaluated in radioligand binding assays for different nicotinic acetylcholine receptor (nAChR) subtypes. Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8芒芒芒20 exhibited much lower affinity for 芒芒7芒芒芒 nAChR than the analogues in the quinuclidine series 21芒芒芒25, although the same structural elements are present. Furthermore, in contrast to the quinuclidine analogues 21芒芒芒25, all (S)-pyrrolidine derivatives 8芒芒芒12 and the piperidine analogues 15 and 16 exhibited higher affinities for 芒芒4芒芒2芒芒芒 nAChR.