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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Synthesis and biological activity of new melatonin dimeric derivatives.

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.[1]

References

  1. Synthesis and biological activity of new melatonin dimeric derivatives. Di Giacomo, B., Bedini, A., Spadoni, G., Tarzia, G., Fraschini, F., Pannacci, M., Lucini, V. Bioorg. Med. Chem. (2007) [Pubmed]
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