Na+-dependent high affinity binding of [3 H] LY515300, a 3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine opioid receptor inverse agonist

…, SL Gackenheimer, PJ Emmerson, SJ Quimby…

Index: Statnick, Michael A.; Suter, Todd M.; Gackenheimer, Susan L.; Emmerson, Paul J.; Quimby, Steve J.; Gehlert, Donald R.; Wheeler, William J.; Mitch, Charles H. European Journal of Pharmacology, 2003 , vol. 482, # 1-3 p. 139 - 150

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Citation Number: 14

Abstract

Analogues of 3, 4-dimethyl-4-(3-hydroxyphenyl) piperidines are high affinity inverse agonists for μ-, δ-and κ-opioid receptors. To characterize inverse agonist binding, we synthesized a high specific activity radioligand from this series,[3H] LY515300 (3-[1-((3- cyclohexyl-[3, 4-3H2])-3 (R, S)-hydroxypropyl)-3 (R), 4 (R)-dimethylpiperidin-4-yl] phenol). In membranes expressing cloned human opioid receptors,[3H] LY515300 binding was ...