Multiple sites of action of (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3PPP) in blood vessels.
Multiple sites of action of (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3PPP) in blood vessels.
复制标题
( )-3-(3-羟基苯基)-N-(1-丙基)哌啶 (( )-3PPP) 在血管中的多个作用位点。
DOI：
10.1016/0014-2999(90)94193-2
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发表时间：
1990
影响因子：
5
通讯作者：
Duckles,SP
中科院分区：
文献类型：
--
作者：
Massamiri,T;Duckles,SP
研究了σ配体(+)-3-（3-羟基苯基）- n -（1-丙基）哌啶（(+)- 3ppp）在体外灌注大鼠尾动脉和兔耳动脉中的功能作用。在大鼠尾动脉中，(+)-3PPP抑制肾上腺素能神经刺激的收缩反应，这种作用被多巴胺d2受体拮抗剂舒必利逆转。然而，在兔耳动脉中，(+)-3PPP增强了对神经刺激的收缩反应，舒必利没有改变这一作用。在大鼠尾动脉中，在沙必利存在的情况下，可卡因和脱氧皮质酮对去甲肾上腺素摄取的阻断揭示了(+)-3PPP的另外两种作用。首先，通过直接测量[3H]去甲肾上腺素积累，证实了对单胺摄取部位的抑制作用。其次，在较高浓度下，抑制肾上腺素能神经刺激的收缩反应的作用在一个尚未确定的部位表现出来。这些研究表明，所观察到的(+)-3PPP的功能效应来自于其对三个单独位点的联合作用，其净效应取决于每种血管中这些不同受体位点的相对密度。
Functional effects of the σ ligand, (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3PPP), were explored in perfused rat tail and rabbit ear arteries in vitro. In the rat tail artery (+)-3PPP inhibited contractile responses to adrenergic nerve stimulation, an effect which was reversed to potentiation by the dopamine D2receptor antagonist sulpiride. In the rabbit ear artery, however, (+)-3PPP potentiated contractile responses to nerve stimulation, an effect which was unchanged by sulpiride. In the rat tail artery, blockade of norepinephrine uptake by cocaine and deoxycorticosterone in the presence of sulpiride revealed two additional actions of (+)-3PPP. First, an inhibitory action on the monoamine uptake site was confirmed by direct measurement of [3H]norepmephrine accumulation. Second, at higher concentrations, an action to inhibit contractile responses to adrenergic nerve stimulation was manifested at a still unidentified site. These studies demonstrate that the observed functional effect of (+)-3PPP results from its combined actions on three individual sites with the net effect dependent on the relative densities of these different receptor sites in each type of vessel.