Martin C A, Emonds-Alt X, Advenier C
Laboratoire de Pharmacologie, Faculté de Médecine Paris-Ouest, France.
Eur J Pharmacol. 1993 Oct 26;243(3):309-12. doi: 10.1016/0014-2999(93)90192-k.
SR 48968 (10(-6) to 10(-5) M) inhibited the cholinergic response of the isolated guinea-pig main bronchus to electrical field stimulation. Since this effect was reversed by naloxone 10(-5) M and since SR 48968 had no effect on the contractile response to exogenous acetylcholine, we conclude that SR 48968 acts at a prejunctional level and that opioid receptors are involved. This effect was observed at concentrations approximately 75,000 times higher than those needed for blockade of tachykinin NK2 receptors.
SR 48968(10⁻⁶至10⁻⁵M)可抑制离体豚鼠主支气管对电场刺激的胆碱能反应。由于该效应可被10⁻⁵M的纳洛酮逆转,且SR 48968对外源性乙酰胆碱的收缩反应无影响,我们得出结论:SR 48968作用于神经节前水平,且涉及阿片受体。在比阻断速激肽NK2受体所需浓度高约75000倍的浓度下观察到了这种效应。