Indanyl piperazines as melatonergic MT2 selective agents
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 only weak contractile effects in rat tail artery.
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.
p. 1199 - 1202
(2007/10/03)
MELATONERGIC INDANYL PIPERAZINES
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(2008/06/13)
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