Figure 1.

Proposed mechanism of neuronal depolarization by kisspeptin binding to its receptor, Kiss1r. Kisspeptin binding to its GPCR, Kiss1r, activates the G protein, Gα_q, and PLC to cleave phosphatidylinositol 4,5-bisphosphate (PIP₂) into IP₃ and DAG. DAG activates a signal cascade by activating PKC, whereas IP₃ mobilizes calcium ions (Ca²⁺), which participate in the cascade by activating other proteins. Membrane depolarization is caused by activation (+) of nonselective TRPC cation channels and inhibition (−) of inwardly rectifying potassium channels (K_ir), possibly through involvement of DAG.