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CNS-5161 is a selective, high-affinity, noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor ion channel. It preferentially binds to the activated form of the NMDA receptor and blocks glutamate-mediated neurotransmission. The compound was developed as a novel treatment for neuropathic pain and has also been investigated for use in migraine, cluster headaches, diabetic neuropathy, and acute or chronic pain. Preclinical studies demonstrated neuroprotective, anticonvulsant, and analgesic effects. In addition to its therapeutic potential, radiolabeled forms of CNS-5161 have been used as PET imaging agents to study NMDA receptor function in vivo[1][2][3][4][5].
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