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- W1544591843 abstract "Publisher Summary Molecular characterization of a family of melatonin ( N -acetyl-5-methoxytryptamine) receptors has provided the foundation for new avenues of exploration. While the receptor proteins have been expressed in heterologous expression systems, data regarding precise localization of these receptors throughout the central nervous system (CNS) and periphery and how localization varies with species is limited. Melatonin first isolated from bovine pineal gland extracts is present in all mammalian species. Radio-iodination of melatonin produces [ 125 I]-iodomelatonin, a high affinity, high specific-activity radioligand suitable for discrete localization and pharmacological characterization of the melatonin binding sites. The target of melatonin's actions is thought to be the suprachiasmatic nucleus (SCN), a circadian clock in the suprachiasmatic nucleus of the hypothalamus, as an intact SCN, is necessary for melatonin to exert an effect on rodent circadian rhythms. The large number of melatonin receptor sequences available has prompted efforts to model receptor tertiary structure and to identify amino acid residues involved in ligand binding. All the models are based on the identification of key amino acids that can participate in hydrogen bonding to the methoxy group and to the amide of melatonin, both of which have been identified as critical interaction points for the molecule based upon structure–activity relationship (SAR) studies." @default.
- W1544591843 created "2016-06-24" @default.
- W1544591843 creator A5018449238 @default.
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- W1544591843 date "1997-01-01" @default.
- W1544591843 modified "2023-10-13" @default.
- W1544591843 title "Chapter 4. Melatonin Receptor Ligands and Their Potential Clinical Applications" @default.
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- W1544591843 doi "https://doi.org/10.1016/s0065-7743(08)61462-1" @default.
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