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PubMed · 12643943

Indanyl piperazines as melatonergic MT2 selective agents.

Ronald J Mattson·John D Catt·Daniel Keavy·Charles P Sloan·James Epperson·Qi Gao·Donald B Hodges·Lawrence Iben·Cathy D Mahle·Elaine Ryan·Frank D Yocca
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Abstract

Optimization of a benzyl piperazine pharmacophore produced N-acyl-4-indanyl-piperazines that bind with high affinity to melatonergic MT(2) receptors. (R)-4-(2,3-dihydro-6-methoxy-1H-inden-1-yl)-N-ethyl-1-piperazine-carboxamide fumarate (13) is a water soluble, selective MT(2) 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.

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3T3 CellsAdenylyl CyclasesAnimalsCircadian RhythmHumansIn Vitro TechniquesIndicators and ReagentsMaleMiceMuscle ContractionMuscle, Smooth, VascularPiperazinesRatsRats, Long-EvansReceptors, Cell SurfaceReceptors, Cytoplasmic and NuclearReceptors, MelatoninJournal Article

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Ronald J Mattson, John D Catt, Daniel Keavy, Charles P Sloan, James Epperson, Qi Gao, Donald B Hodges, Lawrence Iben, Cathy D Mahle, Elaine Ryan, Frank D Yocca. 2003-03-24. Indanyl piperazines as melatonergic MT2 selective agents.. https://doi.org/10.1016/s0960-894x(03)00090-8

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