1202647-54-8
Chemical Structure
PF-04455242
- CAS No.: 1202647-54-8
- Formula:C21H28N2O2S
- Molecular Weight:372.52
IUPAC Name: 2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)propan-1-amine
InChIKey: OWVIKBRKPCTDEP-UHFFFAOYSA-N
SMILES: O=S(C1=CC=CC=C1C2=CC=C(CNCC(C)C)C=C2)(N3CCCC3)=O
Biological Activity: PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal[1][2][3][4].
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PF-04455242 | PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal. | |||||||||||||||||||||
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References
- [1]. Naganawa M, et al. Evaluation of the agonist PET radioligand [¹¹C]GR103545 to image kappa opioid receptor in humans: kinetic model selection, test-retest reproducibility and receptor occupancy by the antagonist PF-04455242. Neuroimage. 2014;99:69-79. [Content Brief]
- [2]. Margolis EB, et al. Differential effects of novel kappa opioid receptor antagonists on dopamine neurons using acute brain slice electrophysiology. PLoS One. 2020;15(12):e0232864. Published 2020 Dec 29. [Content Brief]
- [3]. Romero-Picó A, et al. Kappa-Opioid Receptor Blockade Ameliorates Obesity Caused by Estrogen Withdrawal via Promotion of Energy Expenditure through mTOR Pathway. Int J Mol Sci. 2022;23(6):3118. Published 2022 Mar 14. [Content Brief]
- [4]. Grimwood S, et al. Pharmacological characterization of 2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a high-affinity antagonist selective for κ-opioid receptors. J Pharmacol Exp Ther. 2011;339(2):555-566. [Content Brief]
