Ward S J, Portoghese P S, Takemori A E
Eur J Pharmacol. 1982 Jun 4;80(4):377-84. doi: 10.1016/0014-2999(82)90083-8.
The profiles of action of beta-funaltrexamine (beta-FNA) and beta-chlornaltrexamine (beta-CNA) have been assessed in the mouse vas deferens preparation. beta-FNA, but not beta-CNA, demonstrated a reversible agonist action that appeared to be mediated via kappa-receptor interaction. beta-CNA produced an irreversible antagonism of mu-, kappa- and delta-mediated agonist actions, whereas beta-FNA irreversibly antagonized mu-mediated agonist effects only. This selective action of beta-FNA could also be seen following administration in vivo. beta-CNA and particularly beta-FNA should prove valuable in the elucidation of multiple opioid receptors.
已在小鼠输精管制备物中评估了β-氟纳曲胺(β-FNA)和β-氯纳曲胺(β-CNA)的作用概况。β-FNA表现出可逆的激动剂作用,而β-CNA则没有,这种作用似乎是通过κ受体相互作用介导的。β-CNA对μ、κ和δ介导的激动剂作用产生不可逆的拮抗作用,而β-FNA仅不可逆地拮抗μ介导的激动剂作用。β-FNA的这种选择性作用在体内给药后也可见。β-CNA,尤其是β-FNA,在阐明多种阿片受体方面应具有重要价值。