Mahmoud Saifeldin, Farrag Mohamed, Ruiz-Velasco Victor
Department of Anesthesiology and Perioperative Medicine, Penn State College of Medicine, Hershey, PA, 17033, USA.
Department of Anesthesiology and Perioperative Medicine, Penn State College of Medicine, Hershey, PA, 17033, USA.
Neurosci Lett. 2016 Aug 3;627:77-83. doi: 10.1016/j.neulet.2016.05.055. Epub 2016 May 26.
The nociceptin/orphanin FQ peptide (NOP) opioid receptors regulate neurotransmitter release via inhibition of voltage-gated Ca(2+) channels (CaV2.2) in sympathetic and sensory neurons. Stimulation of NOP receptors by its endogenous agonist, nociception (Noc), leads to membrane-delimited, voltage-dependent (VD) block of CaV2.2 channel currents mediated by Gβγ protein subunits. Previously we reported that the pertussis toxin-sensitive Gαi1 and Gβ2/β4 isoforms mediate the functional coupling of NOP opioid receptors with CaV channels in rat stellate ganglion (SG) sympathetic neurons. In the present report we extended our studies by identifying the Gγ subunit that forms the heterotrimer within this signaling pathway. Small interference RNA (or siRNA) was employed to silence the expression of the natively expressed Gγ subunits. Initial PCR assays indicated that SG neurons expressed seven Gγ subunits. Silencing Gγ3 subunits did not alter signaling between NOP receptors and Ca(2+) channels. However, after Gγ7 isoforms were silenced, the Noc-mediated inhibition of CaV channels was significantly decreased when compared to SG neurons transfected with scrambled siRNA. We observed that Gγ10 and Gγ11 mRNA levels increased 2.5- and 2.7-fold, respectively, after Gγ7 subunits were silenced. However, this compensatory increase in mRNA expression did not appear to fully rescue the NOP receptor coupling efficiency. Additionally, both Gγ2 and Gγ5 levels increased 50 and 75%, respectively, while Gγ3 and Gγ4 expression levels remained relatively unchanged. Taken together, our findings suggest that the Gαi1/Gβ2(β4)/Gγ7 heterotrimeric G protein complex determines the NOP receptor-mediated modulation of CaV channels in SG neurons.
痛敏肽/孤啡肽FQ肽(NOP)阿片受体通过抑制交感神经和感觉神经元中的电压门控Ca(2+)通道(CaV2.2)来调节神经递质释放。内源性激动剂痛敏肽(Noc)刺激NOP受体,导致由Gβγ蛋白亚基介导的CaV2.2通道电流的膜限定性、电压依赖性(VD)阻断。此前我们报道,百日咳毒素敏感的Gαi1和Gβ2/β4亚型介导NOP阿片受体与大鼠星状神经节(SG)交感神经元中CaV通道的功能偶联。在本报告中,我们通过鉴定在该信号通路中形成异源三聚体的Gγ亚基来扩展我们的研究。使用小干扰RNA(或siRNA)来沉默天然表达的Gγ亚基的表达。初始PCR分析表明,SG神经元表达7种Gγ亚基。沉默Gγ3亚基不会改变NOP受体与Ca(2+)通道之间的信号传导。然而,在沉默Gγ7亚型后,与用乱序siRNA转染的SG神经元相比,Noc介导的CaV通道抑制作用显著降低。我们观察到,在沉默Gγ7亚基后,Gγ10和Gγ11的mRNA水平分别增加了2.5倍和2.7倍。然而,这种mRNA表达的代偿性增加似乎并未完全挽救NOP受体的偶联效率。此外,Gγ2和Gγ5的水平分别增加了50%和75%,而Gγ3和Gγ4的表达水平保持相对不变。综上所述,我们的研究结果表明,Gαi1/Gβ2(β4)/Gγ7异源三聚体G蛋白复合物决定了SG神经元中NOP受体介导的CaV通道调节。