Background　G protein-coupled inwardly rectifying potassium （GIRK） channel is one of the seven groups that constitute the family of inwardly rectifying K+ channels （Kir）. Based on their genetic structure， conductibility and widely distribution， GIRK channel takes an important role in neuronal conduction and membrane excitability.　Objective　The expression of GIRK channels exists in both the ascending conduction of pain signal system and endogenous descending inhibitory system. This review will focus on the mechanism of the GIRK channel and pain signal transmission.　Content　This article is aimed to review the important role of GIRK channel in regulating resting potential， neuron excitement and the releasing of neurotransmitter. Various neurotransmitters receptors occurring in numerous different subtypes are capable of coupling to GIRK channels. The opening of GIRK channel result in the efflux of K+ ions， then hyperpolarize the cell membrane in postsynaptic neurons as well as inhibiting the release of neurotransmitters presynaptically， thus control the excitability of neurons and inhibit the transduction of pain signal.　Trend　Further study on the relationship between GIRK channel and pain will make for understanding the mechanism of pain generation.