(−)6-n-Propylnicotine antagonizes the antinociceptive effects of (−)Nicotine
2002; Elsevier BV; Volume: 12; Issue: 20 Linguagem: Inglês
10.1016/s0960-894x(02)00614-5
ISSN1464-3405
AutoresMałgorzata Dukat, Mohamed Ayman El‐Zahabi, Giovanni Ferretti, M. Imad Damaj, Billy R. Martin, Richard Young, Richard A. Glennon,
Tópico(s)Synthesis and Biological Evaluation
ResumoSeveral 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, (−)4 antagonized 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.
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