Activation of the NPFF(2) receptor reduces the inhibitory effect of opioids on the N-type Ca(2+) channel. Although this anti-opioid effect is specific for opioid receptors in neurons and tissues, it also affects NPY Y2 and alpha(2)-adrenoreceptors in undifferentiated SH-SY5Y cells stably expressing the NPFF(2) receptor. To test whether this difference could be due to the immaturity of these cells, they were differentiated to a noradrenergic neuronal phenotype with staurosporine. The differentiated cells ceased to divide and grew long, thin neurites. The inhibition of the depolarization-triggered Ca(2+) transient by activation of G(i)-coupled receptors was either unaffected (micro-opioid), increased (NPY), reduced (NPFF(2)) or lost (alpha(2)-adrenoreceptors). Following a 20 min incubation with 1DMe, the effect of DAMGO was reduced, as in undifferentiated cells, but the effect of NPY was no longer affected. Staurosporine differentiation did not modify the coupling of the micro-opioid and NPFF(2) receptors to the G(i/o) proteins. We suggest that the specificity of the effect of NPFF may not reside in the molecular mechanism of its anti-opioid activity itself but in the organization of receptors within the membrane.

译文

:激活NPFF(2)受体减少阿片类药物对N型Ca(2)通道的抑制作用。尽管这种抗阿片类药物作用对神经元和组织中的阿片类药物受体而言是特异性的,但它也影响稳定表达NPFF(2)受体的未分化SH-SY5Y细胞中的NPY Y2和α(2)-肾上腺素受体。为了测试这种差异是否可能是由于这些细胞的不成熟,将它们分化为带有星形孢菌素的去甲肾上腺素能神经元表型。分化的细胞停止分裂并长出细长的神经突。通过激活G(i)耦合受体抑制去极化触发的Ca(2)瞬变不受影响(微阿片类药物),增加(NPY),减少(NPFF(2))或丢失(alpha(2) -肾上腺素受体)。与1DMe孵育20分钟后,与未分化细胞一样,DAMGO的作用降低了,但NPY的作用不再受到影响。 Staurosporine分化不会修改微阿片类药物和NPFF(2)受体到G(i / o)蛋白质的耦合。我们建议,NPFF作用的特异性可能不在于其自身抗阿片类药物活性的分子机制,而在于膜内受体的组织。

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