Abstract:Melatonin (N‐acetyl‐5‐methoxytryptamine) modulates circadian rhythms and sleep‐wake cycles, primarily via activation of the MT1 and MT2 melatonin receptors which exhibit distinct pharmacological profiles. The MT1/MT2 melatonin receptor ligand, luzindole (LUZ), delays re‐entrainment of running wheel activity following an advance of dark onset via the MT1, and exerts antidepressant‐like effects via the MT2 melatonin receptor. Our goal is to design and synthesize novel analogues with at least 50‐fold selectivity … Show more
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