CBD3063 is a first-in-class modulator of the Cav2.2 channel that disrupts Cav2.2 interaction with the cytosolic auxiliary subunit collapsing response mediator protein 2 (CRMP2). CBD3063 antagonizes Cav2.2 function and blocks neuropathic and inflammatory pain in mouse models. In contrast to gabapentin (a clinically useful Cav2.2 blocker), CBD3063 did not affect somatosensation and did not compromise the protective role of pain in mice. CBD3063 did not induce sedative, affective, or cognitive effects in mice. It also induced anxiolytic-like effects suggesting partial blood-brain barrier penetration. CDB3063 represents a potential new and superior therapeutic agent for chronic pain.
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