A novel class of central nicotinic acetylcholine receptor ligands, 3-(5-alkylamino-4- isoxazolyl)-1, 2, 5, 6-tetrahydropyridine 4a–f, was synthesized. Several of the compounds showed high affinity for central nicotinic receptors (4c: IC50= 50nM), with more than a 100- fold selectivity for nicotinic over muscarinic receptors. The compounds showed up to a 10- fold selectivity for the central nicotinic subtype combination α4β2 (4c: IC50= 4.6 nM), as ...
