2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.
Spadoni G, Balsamini C, Bedini A, Diamantini G, Di Giacomo B, Tontini A, Tarzia G, Mor M, Plazzi PV, Rivara S, Nonno R, Pannacci M, Lucini V, Fraschini F, Stankov BM.
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J Med Chem. 1998 Sep 10;41(19):3624-34. doi: 10.1021/jm970721h.
J Med Chem. 1998.
PMID: 9733487
On the basis of a novel in vitro functional assay (specific binding of [35S]GTPgammaS), which can discriminate agonist from partial agonist, antagonist, and inverse agonist ligands, 5a,g, h,j and 13 were shown to be partial agonists, 5d,e and 8-11 competitive antago …
On the basis of a novel in vitro functional assay (specific binding of [35S]GTPgammaS), which can discriminate agonist from partial agonist, …