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首页> 外文期刊>Life sciences >Analysis of the effect of (-)-BPAP, a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain.
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Analysis of the effect of (-)-BPAP, a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain.

机译：分析（-）-BPAP的作用，这是脉冲传播介导的儿茶酚胺和5-羟色胺在大脑中释放的选择性增强剂。

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Endogenous and synthetic enhancer substances enhance in low concentration the impulse propagation mediated release of transmitters from the catecholaminergic and serotonergic neurons in the brain. The purpose of this study was to see whether uptake or MAO inhibition or agonists have similar enhancing prospectives as the enhancer substances. We measured the electrical stimulation induced release of [3H]-norepinephrine or [3H]-dopamine or [3H]-serotonin from the isolated brain stem of rats. (-)-1-Benzofuran-2-yl)-2-propylaminopentane HCl [(-)-BPAP] was used as a prototype of the enhancer compounds. 50 ng/ml (-)-BPAP was the most effective concentration in enhancing the nerve stimulation induced release of [3H]-norepinephrine and [3H]-dopamine, 10 ng/ml (-)-BPAP was highly effective in enhancing the release of [3H]-serotonin. In contrast, 250 ng/ml desmethylimipramine (DMI), a selective inhibitor of the uptake of norepinephrine, did not change significantly the nerve stimulation induced release of [3H]-norepinephrine and 50 ng/ml fluoxetine, a selective inhibitor of the uptake of serotonin, did not change the release of [3H]-serotonin. Neither 250 ng/ml clorgyline, a selective inhibitor of MAO-A, nor 250 ng/ml lazabemide, a selective inhibitor MAO-B, was capable to significantly increase the nerve stimulation induced release of either [3H]-serotonin or [3H]-norepinephrine. The potent dopamine receptor agonists, pergolide and bromocriptine did not change significantly the release of [3H]-dopamine in 50 ng/ml concentration, which is sufficient to stimulate the dopamine receptors. The results prove that stimulation of catecholaminergic and serotonergic neurons in the brain via the enhancing mechanism is clearly different from influencing uptake or MAO.
机译：内源性和合成的增强剂物质在低浓度时会增强冲动传播介导的脑儿茶酚胺能和血清素能神经元的递质释放。这项研究的目的是了解摄取或抑制MAO或激动剂是否具有与增强物质相似的增强前景。我们测量了电刺激诱导的大鼠离体脑干释放的[3H]-去甲肾上腺素或[3H]-多巴胺或[3H] -5-羟色胺的释放。 （-）-1-苯并呋喃-2-基）-2-丙基氨基戊烷HCl [（-）-BPAP]被用作增强剂化合物的原型。 50 ng / ml（-）-BPAP是增强神经刺激诱导的[3H]-去甲肾上腺素和[3H]-多巴胺释放的最有效浓度，10 ng / ml（-）-BPAP是增强神经刺激诱导的释放的最有效浓度。 [3H] -5-羟色胺。相比之下，选择性去甲肾上腺素吸收的抑制剂250 ng / ml去甲基丙米拉明（DMI）并没有显着改变神经刺激诱导的[3H]-去甲肾上腺素和50 ng / ml氟西汀的神经刺激释放。血清素，并没有改变[3H]-血清素的释放。 250 ng / ml的MAO-A选择性抑制剂clorgyline或250 ng / ml的MAO-B选择性抑制剂lazabemide均不能显着增加神经刺激诱导的[3H] -5-羟色胺或[3H]的释放。 -去甲肾上腺素。强效的多巴胺受体激动剂，培高利特和溴隐亭没有明显改变浓度为50 ng / ml的[3H]-多巴胺的释放，足以刺激多巴胺受体。结果证明，通过增强机制刺激大脑中的儿茶酚胺能和血清素能神经元明显不同于影响摄取或MAO。

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