Data di Pubblicazione:
2006
Citazione:
Towards the development of mixed MT(1)-agonist/MT(2)-antagonist melatonin receptor ligands / G. Spadoni, A. Bedini, T. Guidi, G. Tarzia, V. Lucini, M. Pannacci, F. Fraschini. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 1:10(2006 Oct), pp. 1099-1105.
Abstract:
Herein we report attempts to optimize the pharmacological properties of 5-(2-hydroxyethoxy)-N-acetyltryptamine (5-HEAT), a melatonin receptor ligand previously described by us. Several 5-substituted
and 2,5-disubstituted N-acyltryptamines were synthesized and evaluated in vitro for the human cloned MT1 and MT2 receptors.
Fromthis series of N-acyltryptamines the 2-bromo derivative (5c) retains the interesting efficacy profile of 5-HEAT and shows increased melatonin receptor affinities; it represents one of the
first examples of a high-affinity MT1 agonist/MT2 antagonist.
Some other full agonists for both melatonin receptors which exhibit similar or increased affinity relative to that of melatonin
were obtained.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Biological activity; Drug design; Melatonin; N-acyltryptamines; Receptors
Elenco autori:
G. Spadoni, A. Bedini, T. Guidi, G. Tarzia, V. Lucini, M. Pannacci, F. Fraschini
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