Indanyl piperazines as melatonergic MT2 selective agents.

Article Details

Citation

Copy to clipboard

Mattson RJ, Catt JD, Keavy D, Sloan CP, Epperson J, Gao Q, Hodges DB, Iben L, Mahle CD, Ryan E, Yocca FD

Indanyl piperazines as melatonergic MT2 selective agents.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1199-202.

PubMed ID

12643943 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Melatonin receptor type 1A	IC 50 (nM)	0.6	N/A	N/A	Details
Melatonin	Melatonin receptor type 1B	IC 50 (nM)	0.3	N/A	N/A	Details