Augmentation of glycine receptor alpha3 currents suggests a mechanism for glucose-mediated analgesia

作者：Breitinger Ulrike; Breitinger Hans Georg

来源：Neuroscience Letters, 2016, 612: 110-115.

DOI：10.1016/j.neulet.2015.11.051

• Ligand-gated ion channels
• Glycine receptors alpha
• 3 subunit
• Allosteric modulation
• Glucose as channel modulator
• Pain pathways
• Gain-of-function mutant alpha
• 3(P185L)

The inhibitory glycine receptor (GlyR) mediates rapid synaptic inhibition in the mammalian central nervous system. Recently, glucose was identified as a positive modulator of alpha 1 GlyRs. Here, recombinant human alpha 3GlyRs with and without glucose treatment were studied using patch clamp methods. Similar to alpha 1GlyRs, receptor variants alpha 3L and alpha 3K were potentiated by sugar. Glucose treatment reduced EC50 values of GlyR alpha 3L and alpha 3K by a factor of 4.5 and 3.3, respectively, without affecting maximum currents or desensitization. The high-activity mutant alpha 3L(P185L) was not further potentiated by glucose. Potentiation of glycinergic signalling may underlie some of the analgetic effects of glucose.

• 出版日期2016-1-26