Strategies leading to MT2 selective melatonin receptor antagonists.
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.
Spadoni
Gilberto
G
Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino, Piazza Rinascimento 6, I-61029 Urbino, Italy. gilberto@uniurb.it
Bedini
Annalida
A
Piersanti
Giovanni
G
Mor
Marco
M
Rivara
Silvia
S
Tarzia
Giorgio
G
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
C426685:5-hydroxyethoxy-N-acetyltryptamine; D007211:Indoles; D008024:Ligands; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D011994:Recombinant Proteins; D008550:Melatonin