Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-Aminoethoxy)pyridine as novel nicotinic receptor ligands
摘要:
Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy)pyridine substituted at the 5' and 6'-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [H-3](-)cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited K-i values ranging from 0.076 to 319 nM compared to a K-i value of 26 nM for compound 1. Among the compounds tested, 5'-vinyl-6'-chloro substituted I was the most potent. (C) 2002 Elsevier Science Ltd. All rights reserved.
SUBSTITUTED PYRIDINE COMPOUNDS USEFUL FOR CONTROLLING CHEMICAL SYNAPTIC TRANSMISSION
申请人:ABBOTT LABORATORIES
公开号:EP1257535A1
公开(公告)日:2002-11-20
[EN] SUBSTITUTED PYRIDINE COMPOUNDS USEFUL FOR CONTROLLING CHEMICAL SYNAPTIC TRANSMISSION<br/>[FR] COMPOSES PYRIDINE SUBSTITUES UTILES DANS LA REGULATION DE LA TRANSMISSION SYNAPTIQUE CHIMIQUE
申请人:ABBOTT LAB
公开号:WO2001056991A1
公开(公告)日:2001-08-09
The present invention is directed to a series of substituted pyridine compounds (I), a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3'-(5'- and/or 6'-substituted) pyridyl ethers. n = 1-4, R1-R6 as in the claims.
Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-Aminoethoxy)pyridine as novel nicotinic receptor ligands
作者:Nan-Horng Lin、Liming Dong、William H Bunnelle、David J Anderson、Michael D Meyer
DOI:10.1016/s0960-894x(02)00740-0
日期:2002.11
Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy)pyridine substituted at the 5' and 6'-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [H-3](-)cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited K-i values ranging from 0.076 to 319 nM compared to a K-i value of 26 nM for compound 1. Among the compounds tested, 5'-vinyl-6'-chloro substituted I was the most potent. (C) 2002 Elsevier Science Ltd. All rights reserved.