PF-4455242 is a selective k opioid receptor (KOR) antagonist with 20-fold selectivity for kappa over mu receptors (k Ki = 3 nM, µ Ki =64 nM). PF-4455242 is orally active, has good brain penetration in rats and was able to block the effects of the kappa agonist U50488. Studies indicate that k blockade has afforded antidepressant activity in several animal models. PF-4455242 has been in phase I clinical trials for trial for bipolar depression.
Features and Benefits
This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Legal Information
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Other Notes
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