Ryanodine receptors (RyR), as intracellular Ca²⁺ release channels, mediate Ca²⁺ release from intracellular stores in the sarcoplasmic reticulum and play essential roles in some excitable cells such as cardiac and skeletal cells. Cyclic adenosine diphosphate ribose (cADPR) and FK 506 binding proteins(FKBP) are tightly associated with RyR in these cells. A summary on latest research progress in RyR and some channel modulators for RyR2 was given based on authors′ research.