PF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor ( KOR ) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR -independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal.
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