6-Chloromelatonin is a Melatonin (sc-207848) derivative and a potent agonist of the MEL-1 (melatonin receptors) with affinity comparable to Melatonin. Along with the Melatonin analogs 2-Iodomelatonin (sc-203463) and 2-Phenylmelatonin (sc-203466), 6-Chloromelatonin is used as part of a panel of agonists and antagonists in binding studies to probe the behavior of melatonin receptors. During characterization studies of a rabbit retinal melatonin receptor, Melatonin and 6-Chloromelatonin demonstrated similar agonist potency at inhibiting calcium-dependent dopamine release from the retina (IC50 = 40 pM for both compounds). Melatonin (at 0.1-2.0 mM) and 6-Chloromelatonin (at 0.1-0.5 mM) both depressed evoked hippocampal potentials similarly, and this action was perturbed by the MEL-1B-R partial antagonist Luzindole (sc-202700), elucidating the mechanism for Melatonin- and 6-Chloromelatonin-induced modulation of neuron potentials. 6-Chloromelatonin is an activator of MEL-1A-R and MEL-1B-R.
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