Article

Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted-3'-phenyl-5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel nicotinic antagonist.

Chemistry and Life Sciences, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA.
Journal of Medicinal Chemistry (impact factor: 5.25). 12/2001; 44(24):4039-41. pp.4039-41
Source: PubMed

ABSTRACT A series of 2'-substituted-3'-phenyl epibatidine analogues were synthesized and evaluated for inhibition of binding at nicotine acetylcholine receptors and for antinociceptive properties in mice. The introduction of a bulky phenyl group at the 3'-position exerted a profound influence on both receptor binding and antinociceptive effects. Substitution of different groups at the 2'-position distinguished between agonist and antagonist properties. These results demonstrate that structural requirements for receptor activities and recognition are distinctively different.

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Keywords

2'-substituted-3'-phenyl epibatidine analogues
 
agonist
 
antagonist properties
 
antinociceptive effects
 
bulky phenyl group
 
different groups
 
mice
 
nicotine acetylcholine receptors
 
profound influence
 
receptor activities
 
receptor binding
 

F I Carroll