Indanyl piperazines as melatonergic MT 2 selective agents

…, JD Catt, D Keavy, CP Sloan, J Epperson…

Index: Mattson, Ronald J.; Catt, John D.; Keavy, Daniel; Sloan, Charles P.; Epperson, James; Gao, Qi; Hodges, Donald B.; Iben, Lawrence; Mahle, Cathy D.; Ryan, Elaine; Yocca, Frank D. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 6 p. 1199 - 1202

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Citation Number: 31

Abstract

Optimization of a benzyl piperazine pharmacophore produced N-acyl-4-indanyl-piperazines that bind with high affinity to melatonergic MT2 receptors.(R)-4-(2, 3-dihydro-6-methoxy-1H- inden-1-yl)-N-ethyl-1-piperazine-carboxamide fumarate (13) is a water soluble, selective MT2 agonist, which produces advances in circadian phase in rats at doses of 1–56 mg/kg that are no different from those of melatonin at 1 mg/kg. Unlike melatonin, 13 produced ...