Neuronal nAChR stereoselectivity to non‐natural epibatidine derivatives

FEBS Letters

Patt, Jörg T²  Schubiger, P.August²  Westera, Gerrit²  Bertrand, Daniel¹  Bertrand, Sonia¹  Spang, Jörg E² 

[1]Département de physiologie, Centre Médical Universitaire (Faculté de Médecine), 1 rue Michel Servet, CH-1211 Geneva 4, Switzerland

[2]Center for Radiopharmaceutical Science, Swiss Federal Institute of Technology Zürich, Paul Scherrer Institute Villigen and Department of Radiology, Clinic of Nuclear Medicine, University Hospital, Zürich, Switzerland

关键词: Nicotinic acetylcholine receptor;    Brain;    Epibatidine;    Pharmacophore;    Imaging;    ACh;    acetylcholine;    nAChR;    nicotinic receptor;    CNS central nervous system;    PNS;    peripheral nervous system;   

DOI  :  10.1016/S0014-5793(99)00473-1

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The frog toxin epibatidine is one of the most powerful ligands of the neuronal nicotinic receptors and derivatives show promising possibilities for labeling in positron emission tomography studies. In an attempt to reduce epibatidine toxicity, new methyl derivatives were synthesized, tested in positron emission tomography imaging and in electrophysiology. labeling as well as physiological experiments highlighted the differences in sensitivity of the neuronal nicotinic acetylcholine receptors between two methyl enantiomers and the reduction in sensitivity caused by introducing the methyl group. At present, epibatidine derivatives seem the most promising compounds for in vivo labeling of neuronal nicotinic acetylcholine receptors.

【 授权许可】

Unknown