title: Strategies leading to MT2 selective melatonin receptor antagonists.
abstract: Studies of the physiological actions of melatonin have been hindered by the lack of specific, potent and subtype selective agonists and antagonists. This paper reviews our progress in developing subtype selective melatonin antagonists. Evidence is presented suggesting the structural features conferring MT2 selective antagonism.
authors.affiliation: Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino, Piazza Rinascimento 6, I-61029 Urbino, Italy. gilberto@uniurb.it
authors.forename: Gilberto
authors.initials: G
authors.lastname: Spadoni
authors.forename: Annalida
authors.initials: A
authors.lastname: Bedini
authors.forename: Giovanni
authors.initials: G
authors.lastname: Piersanti
authors.forename: Marco
authors.initials: M
authors.lastname: Mor
authors.forename: Silvia
authors.initials: S
authors.lastname: Rivara
authors.forename: Giorgio
authors.initials: G
authors.lastname: Tarzia
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D008024:Ligands; D008550:Melatonin / Q000819:agonists / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology; D051379:Mice; D041681:NIH 3T3 Cells; D044122:Receptor, Melatonin, MT1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D044123:Receptor, Melatonin, MT2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: C426685:5-hydroxyethoxy-N-acetyltryptamine; D007211:Indoles; D008024:Ligands; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D011994:Recombinant Proteins; D008550:Melatonin