Jiangsu Key Laboratory of TCM Evaluation and Translational Research, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, 211198, China.
State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
Exp Mol Med. 2021 Feb;53(2):235-249. doi: 10.1038/s12276-021-00563-5. Epub 2021 Feb 9.
Dopamine D1 receptor (D1DR) and D2 receptor (D2DR) are closely associated with pain modulation, but their exact effects on neuropathic pain and the underlying mechanisms remain to be identified. Our research revealed that intrathecal administration of D1DR and D2DR antagonists inhibited D1-D2DR complex formation and ameliorated mechanical and thermal hypersensitivity in chronic constriction injury (CCI) rats. The D1-D2DR complex was formed in the rat spinal cord, and the antinociceptive effects of D1DR and D2DR antagonists could be reversed by D1DR, D2DR, and D1-D2DR agonists. Gαq, PLC, and IP3 inhibitors also alleviated CCI-induced neuropathic pain. D1DR, D2DR, and D1-D2DR complex agonists all increased the intracellular calcium concentration in primary cultured spinal neurons, and this increase could be reversed by D1DR, D2DR antagonists and Gαq, IP3, PLC inhibitors. D1DR and D2DR antagonists significantly reduced the expression of p-PKC γ, p-CaMKII, p-CREB, and p-MAPKs. Levo-corydalmine (l-CDL), a monomeric compound in Corydalis yanhusuo W.T. Wang, was found to obviously suppress the formation of the spinal D1-D2DR complex to alleviate neuropathic pain in CCI rats and to decrease the intracellular calcium concentration in spinal neurons. l-CDL-induced inhibition of p-PKC γ, p-MAPKs, p-CREB, and p-CaMKII was also reversed by D1DR, D2DR, and D1-D2DR complex agonists. In conclusion, these results indicate that D1DR and D2DR form a complex and in turn couple with the Gαq protein to increase neuronal excitability via PKC γ, CaMKII, MAPK, and CREB signaling in the spinal cords of CCI rats; thus, they may serve as potential drug targets for neuropathic pain therapy.
多巴胺 D1 受体(D1DR)和 D2 受体(D2DR)与疼痛调节密切相关,但它们对神经病理性疼痛的确切影响及其潜在机制仍有待确定。我们的研究表明,鞘内给予 D1DR 和 D2DR 拮抗剂可抑制 D1-D2DR 复合物的形成,并改善慢性缩窄性损伤(CCI)大鼠的机械和热敏性。D1-D2DR 复合物在大鼠脊髓中形成,D1DR 和 D2DR 拮抗剂的抗伤害作用可被 D1DR、D2DR 和 D1-D2DR 激动剂逆转。Gαq、PLC 和 IP3 抑制剂也可减轻 CCI 诱导的神经病理性疼痛。D1DR、D2DR 和 D1-D2DR 复合物激动剂均增加原代培养脊髓神经元的细胞内钙浓度,而这种增加可被 D1DR、D2DR 拮抗剂和 Gαq、IP3、PLC 抑制剂逆转。D1DR 和 D2DR 拮抗剂显著降低了 p-PKCγ、p-CaMKII、p-CREB 和 p-MAPKs 的表达。左旋延胡索乙素(l-CDL),一种来自于延胡索的单体化合物,明显抑制脊髓 D1-D2DR 复合物的形成,减轻 CCI 大鼠的神经病理性疼痛,并降低脊髓神经元的细胞内钙浓度。l-CDL 诱导的 p-PKCγ、p-MAPKs、p-CREB 和 p-CaMKII 的抑制作用也可被 D1DR、D2DR 和 D1-D2DR 复合物激动剂逆转。总之,这些结果表明,D1DR 和 D2DR 形成复合物,进而与 Gαq 蛋白偶联,通过 PKCγ、CaMKII、MAPK 和 CREB 信号通路增加 CCI 大鼠脊髓神经元的兴奋性;因此,它们可能成为治疗神经病理性疼痛的潜在药物靶点。