Author/Authors :
Ronald J. Mattson، نويسنده , , John D. Catt، نويسنده , , Daniel Keavy، نويسنده , , Charles P. Sloan، نويسنده , , James Epperson، نويسنده , , Qi Gao، نويسنده , , Donald B. Hodges، نويسنده , , Lawrence Iben، نويسنده , , Cathy D. Mahle، نويسنده , , Elaine Ryan، نويسنده , , Frank D. Yocca، نويسنده ,
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 only weak contractile effects in rat tail artery.
