AI Article Synopsis
- Researchers have developed new tetrahydronaphthalenic derivatives of melatonin aimed at being selective ligands for melatonin receptors.
- Modifications to the acyl group and phenyl ring have improved selectivity and activity of these ligands, with ten out of seventeen showing similar affinity for MT(2) receptors as melatonin.
- The new compounds exhibit strong selectivity for MT(2) over MT(1) (selectivity >100) but only show partial agonist or antagonist activity rather than being full agonists.
Article Abstract
Following our studies of the melatoninergic receptors, we have developed new tetrahydronaphthalenic derivatives of melatonin that have been tested as selective melatonin receptors ligands. Regarding the role of the phenyl substituent to obtain selective ligands, modulation of selectivity and activity have been achieved by modifications of the acyl group and substitutions on the phenyl ring. Ten of the seventeen evaluated derivatives have MT(2) receptor affinity similar to that of melatonin. Moreover, we have achieved remarkable MT(2) selectivity over MT(1) (selectivity >100) and have been able to further extend the RSA of the tetrahydrophthalenic series. However, the compounds presented here display partial agonist or antagonist behavior instead of full agonist.
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| http://dx.doi.org/10.1016/j.bmc.2009.03.023 | DOI Listing |
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