1.
Bioorg Med Chem Lett
; 14(23): 5881-4, 2004 Dec 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15501061
RESUMO
A series of tetrahydroisoquinolines has yielded potent MT(2) receptor antagonists, which are selective versus the MT(1) receptor.
Assuntos
Receptor MT2 de Melatonina/antagonistas & inibidores , Receptor MT2 de Melatonina/metabolismo , Tetra-Hidroisoquinolinas/química , Tetra-Hidroisoquinolinas/metabolismo , Humanos , Ligação Proteica/fisiologia
2.
Bioorg Med Chem Lett
; 14(4): 1023-6, 2004 Feb 23.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15013015
RESUMO
A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2) binding affinity and MT(2) selectivity of at least 70-fold over the MT(1) receptor. Compound 26 demonstrated full agonism at the MT(2) receptor.