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Recent advances in the development of melatonin MT(1) and MT(2) receptor agonists. 2010

Marco Mor, and Silvia Rivara, and Daniele Pala, and Annalida Bedini, and Gilberto Spadoni, and Giorgio Tarzia
Dipartimento Farmaceutico, UniversitĂ  degli Studi di Parma, Italy. marco.mor@unipr.it

BACKGROUND Increasing clinical evidences suggest that melatonin receptor agonists can represent a novel therapeutic approach for the treatment of sleep disturbances and depression. A variety of studies also revealed a role of melatonin and its receptors in different patho-physiological conditions. Due to the multiple effects of this hormone, the design of new agents able to interact selectively with melatonin receptors has become an area of great interest during the last decade. METHODS An extensive inspection of patents and scientific literature about MT(1) and MT(2) melatonin receptor agonists reported from 1999 to early 2010. RESULTS A comprehensive review of structures recently claimed as melatonin receptor agonists and a broad overview of structure-activity relationships for these ligands. CONCLUSIONS After 5 decades of research, the field of melatonin receptor agonists comprises a variety of chemical entities, belonging to structurally different classes. Patents filed since 1999 claim new melatonin receptor agonists, characterized either by improved pharmacokinetic or pharmacodynamic properties, compared to those of melatonin receptor agonists already approved for clinical uses. The results of preclinical studies on animal models show that melatonin receptor agonists can be considered promising agents for the treatment of CNS-related pathologies.

UI MeSH Term Description Entries
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D010330 Patents as Topic Works about exclusive legal rights or privileges applied to inventions, plants, etc. Trademarks,Patents as Topics,Trademark
D002491 Central Nervous System Agents A class of drugs producing both physiological and psychological effects through a variety of mechanisms. They can be divided into "specific" agents, e.g., affecting an identifiable molecular mechanism unique to target cells bearing receptors for that agent, and "nonspecific" agents, those producing effects on different target cells and acting by diverse molecular mechanisms. Those with nonspecific mechanisms are generally further classed according to whether they produce behavioral depression or stimulation. Those with specific mechanisms are classed by locus of action or specific therapeutic use. (From Gilman AG, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p252) Central Nervous System Drugs
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D044122 Receptor, Melatonin, MT1 A melatonin receptor subtype that is primarily found in the HYPOTHALAMUS and in the KIDNEY. Melatonin MT1 Receptor,MT1 Receptor,Mel(1a)-Melatonin Receptor,MT1 Receptor, Melatonin,Receptor, MT1,Receptor, Melatonin MT1
D044123 Receptor, Melatonin, MT2 A melatonin receptor subtype primarily found expressed in the BRAIN and RETINA. Melatonin MT2 Receptor,MT2 Receptor,Mel 1b Receptor,Melatonin 1b Receptor,MT2 Receptor, Melatonin,Receptor, MT2,Receptor, Melatonin 1b,Receptor, Melatonin MT2

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