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.

Abstract

2-Methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242) is a novel κ-opioid receptor (KOR) antagonist with high affinity for human (3 nM), rat (21 nM), and mouse (22 nM) KOR, a ∼ 20-fold reduced affinity for human μ-opioid receptors (MORs; K(i) = 64 nM), and negligible affinity for δ-opioid receptors (K(i) > 4 μM). PF… (More)
DOI: 10.1124/jpet.111.185108

Topics

Cite this paper

@article{Grimwood2011PharmacologicalCO, title={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.}, author={Sarah Grimwood and Y. Lu and Anne Schmidt and Michelle A Vanase-Frawley and Aarti Sawant-Basak and Elka Miller and S Mclean and Jeremy Freeman and S. Wong and Jay P. McLaughlin and Patrick R. Verhoest}, journal={The Journal of pharmacology and experimental therapeutics}, year={2011}, volume={339 2}, pages={555-66} }