Add time:08/21/2019         Source:sciencedirect.com

We report the synthesis, binding properties and intrinsic activity at MT1 and MT2 melatonin receptors of new dimeric melatonin receptor ligands in which two units of the monomeric agonist N-{2-[(3-methoxyphenyl)methylamino]ethyl}acetamide (1) are linked together through different anchor points. Dimerization of compound 1 through the methoxy substituent leads to a substantial improvement in selectivity for the MT1 receptor, and to a partial agonist behavior. Compound 3a, with a trimethylene linker, was the most selective for the MT1 subtype (112-fold selectivity) and compound 3d, characterized by a hexamethylene spacer, had the highest MT1 binding affinity (pKiMT1 = 8.47) and 54-fold MT1-selectivity. Dimerization through the aniline nitrogen of 1 abolished MT1 selectivity, leading to compounds with either a full agonist or an antagonist behavior depending on the nature of the linker.

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