PF04455242盐酸盐，PF-04455242 hydrochloride；≥98% (HPLC)

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.

 

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.

 

This compound was developed by Pfizer for Neuroscience research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.
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