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PF-063782865 (likely a typographical error for PF-06372865) is an investigational small molecule developed by Pfizer. It acts as a subtype-selective positive allosteric modulator (PAM) of the GABA-A receptor, specifically targeting the α2, α3, and α5 subunits while sparing the α1 subunit. This selectivity is intended to provide analgesic, anxiolytic, and anticonvulsant effects without the sedative and cognitive side effects typically associated with non-selective GABA-A modulators like benzodiazepines. The compound has been evaluated in clinical trials for conditions including chronic low back pain, photosensitive epilepsy, and generalized anxiety disorder. In pain studies, it has been compared against placebo and active controls such as naproxen and pregabalin. Development for chronic pain was discontinued following Phase 2 results.
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