Author/Authors :
Ma gorzata Dukat، نويسنده , , Mohamed El-Zahabi، نويسنده , , Giovanni Ferretti، نويسنده , , M. Imad Damaj، نويسنده , , Billy R. Martin، نويسنده , , Richard Young، نويسنده , , Richard A. Glennon، نويسنده ,
Abstract :
Several 6-alkyl analogues of nicotine were examined in radioligand binding and in vivo functional assays. Although (−)6-ethylnicotine (3) binds with high affinity at nACh receptors (Ki=5.6 nM) and produces nicotine-like actions, its n-propyl homologue (−)4 (Ki=22 nM) failed to produce such effects. In fact, (−)4antagonized the antinociceptive effects of (−)nicotine in the tail-flick assay in mice, but not the spontaneous activity or discriminative stimulus effects of (−)nicotine. Compound (−)4 appears to selectively antagonize only one of the three effects examined and is an interesting cholinergic agent for subsequent investigation.
