CRA-024781 is a potent and selective inhibitor of the neuronal K⁺-Cl^- cotransporter isoform 2 (KCC2), a key regulator of chloride homeostasis in neurons. It is primarily used in research settings to study GABAergic signaling and neuronal excitability in the central nervous system. By inhibiting KCC2, CRA-024781 shifts the intracellular chloride concentration, reducing inhibitory GABAergic tone and increasing neuronal activity. This makes it a valuable tool for investigating potential treatments for neurological disorders such as epilepsy, neuropathic pain, anxiety, depression, and schizophrenia. Researchers also explore its effects on neuroplasticity, synaptic function, and inflammation-related pathways in the brain. Its applications remain experimental, with ongoing studies to assess efficacy, safety, and therapeutic potential.