Synthesis and biological activity of new melatonin dimeric derivatives.

Article Details

Citation

Di Giacomo B, Bedini A, Spadoni G, Tarzia G, Fraschini F, Pannacci M, Lucini V

Synthesis and biological activity of new melatonin dimeric derivatives.

Bioorg Med Chem. 2007 Jul 1;15(13):4643-50. Epub 2007 Mar 30.

PubMed ID
17481904 [ View in PubMed
]
Abstract

A new series of melatonin (MLT) dimers were obtained by linking together two melatonin units with a linear alkyl chain through the MLT acetamido group or through a C-2 carboxyalkyl function. The binding properties of these ligands were evaluated in in vivo experiments on cloned human MT(1) and MT(2) receptors expressed in NIH3T3 rat fibroblast cells. The class of 2-carboxyalkyl dimers was the most interesting one with compounds having good MT(1)/MT(2) nanomolar affinity. The data obtained suggest that the spacer length is crucial for optimal interaction at both receptor subtypes as well as to determine functional activity of the resulting dimers.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MelatoninMelatonin receptor type 1AKi (nM)0.2N/AN/ADetails
MelatoninMelatonin receptor type 1BKi (nM)0.3N/AN/ADetails