Ethyl-for-methyl substitution enhances the subtype specificity of mecamylamine analogues.

The synthesis of novel mecamylamine analogues is described in which one, two or three of the methyl groups of mecamylamine have been systematically replaced with ethyl groups. Assessment of the compounds highlights that simple ethyl for methyl changes changes to the parent structure can dramatically enhance activity and selectivity towards either the α4ß2 (at the expense of α3ß4) or the α3ß4 (at the expense of α4ß2) nicotinic acetylcholine receptor sub-type as compared to the parent compound.

A new synthesis and preliminary evaluation of some analogues of mecamylamine - a compound with anti-addiction properties.

A new synthesis of mecamylamine - a known anti-hypertensive drug with anti-addictive properties is described. The new route allowed access to two novel analogues whose activity at two nicotinic acetylcholine receptor subtypes was assessed.