RGD Reference Report - Indanyl piperazines as melatonergic MT2 selective agents. - Rat Genome Database

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Indanyl piperazines as melatonergic MT2 selective agents.

Authors: Mattson, RJ  Catt, JD  Keavy, D  Sloan, CP  Epperson, J  Gao, Q  Hodges, DB  Iben, L  Mahle, CD  Ryan, E  Yocca, FD 
Citation: Mattson RJ, etal., Bioorg Med Chem Lett. 2003 Mar 24;13(6):1199-202.
RGD ID: 9588678
Pubmed: (View Article at PubMed) PMID:12643943

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.

Gene Ontology Annotations    

Biological Process

Objects Annotated

Genes (Rattus norvegicus)
Mtnr1b  (melatonin receptor 1B)

Additional Information