Neuronal voltage-gated calcium channels play a pivotal role in the conversion of electrical signals into calcium entry into nerve endings that is required for the release of neurotransmitters. They are under the control of a number of cellular signaling pathways that serve to fine tune synaptic activities, including G-protein coupled receptors (GPCRs) and the opioid system. Besides modulating channel activity via activation of second messengers, GPCRs also physically associate with calcium channels to regulate their function and expression at the plasma membrane. In this mini review, we discuss the mechanisms by which calcium channels are regulated by classical opioid and nociceptin receptors. We highlight the importance of this regulation in the control of neuronal functions and their implication in the development of disease conditions. Finally, we present recent literature concerning the use of novel μ-opioid receptor/nociceptin receptor modulators and discuss their use as potential drug candidates for the treatment of pain.

神经元电压门控钙通道在将电信号转换为钙进入神经末梢的过程中发挥着关键作用，这是释放神经递质所需的。它们受到许多细胞信号通路的控制，这些信号通路可微调突触活动，包括 G 蛋白偶联受体 (GPCR) 和阿片类药物系统。除了通过激活第二信使调节通道活性外，GPCR 还与钙通道物理结合，以调节其在质膜上的功能和表达。在这篇小综述中，我们讨论了经典阿片类药物和伤害感受素受体调节钙通道的机制。我们强调这种调节在控制神经元功能中的重要性及其对疾病发展的影响。最后，我们介绍了有关新型μ阿片受体/伤害感受素受体调节剂的使用的最新文献，并讨论了它们作为治疗疼痛的潜在候选药物的用途。