[右美沙芬对苯环利定体外血管收缩的拮抗作用]
[Antagonistic effects of dextromethorphan on vasoconstriction of phencyclidine in vitro].
作者信息
Bao W L, Sun F Y, Zheng F C, Zhang A Z
机构信息
Department of Neurobiology, Shanghai Medical University, China.
出版信息
Zhongguo Yao Li Xue Bao. 1991 May;12(3):242-4.
Bioassay and spectrophotofluorometry were used to study the antagonistic effect of dextromethorphan (DM) on phencyclidine (PCP) vasoconstriction in rabbit ear artery. DM (5 mumols.L-1) antagonized enhancement of PCP, N-[1-(2-thienyl) cyclohexyl] piperidine (TCP) and dizocilpine maleate (MK-801) (5 mumols.L-1) on electrical stimulation-induced vasoconstriction by 86 +/- 18%, 84 +/- 17%, and 86 +/- 18%, respectively (n = 6, P less than 0.01), but had no obvious bioactivity itself at the same concentration. DM (1, 2.5, and 5 mumols.L-1) inhibited the PCP effect and reduced the maximal effect of PCP with pD2' = 5.3 +/- 0.3 (n = 4). The contents of norepinephrine (NE) in control, PCP, and DM + PCP groups were 5 +/- 6, 12 +/- 8, and 5 +/- 6 ng.ml-1, respectively (n = 9). PCP (10 mumols.L-1) increased the NE release (P less than 0.05) but DM (10 mumols.L-1) inhibited it (P less than 0.01). The results suggest DM may be a noncompetitive blockader for PCP receptors.
采用生物测定法和分光光度荧光测定法研究右美沙芬（DM）对兔耳动脉中苯环利定（PCP）血管收缩的拮抗作用。DM（5 μmol·L-1）分别拮抗了PCP、N-[1-(2-噻吩基)环己基]哌啶（TCP）和马来酸二氮卓（MK-801）（5 μmol·L-1）对电刺激诱导的血管收缩增强作用的86±18%、84±17%和86±18%（n = 6，P<0.01），但在相同浓度下其本身无明显生物活性。DM（1、2.5和5 μmol·L-1）抑制PCP的作用，并降低PCP的最大效应，pD2' = 5.3±0.3（n = 4）。对照组、PCP组和DM + PCP组中去甲肾上腺素（NE）的含量分别为5±6、12±8和5±6 ng·ml-1（n = 9）。PCP（10 μmol·L-1）增加NE释放（P<0.05），但DM（10 μmol·L-1）抑制NE释放（P<0.01）。结果表明，DM可能是PCP受体的非竞争性阻断剂。
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