Synthesis and receptor??affinity profile of N??hydroxytryptamine derivatives for serotonin and tryptamine receptors. A molecular??modeling study

…, PHH Hermkens, JH van Maarseveen…

Index: Dijkstra, Gerard D. H.; Tulp, Martin Th. M.; Hermkens, Pedro H. H.; Maarseveen, Jan H. van; Scheeren, Hans W.; Kruse, Chris G. Recueil des Travaux Chimiques des Pays-Bas, 1993 , vol. 112, # 2 p. 131 - 136

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Citation Number: 6

Abstract

Abstract The synthesis and the affinities for serotonin and tryptamine receptors of a series of N-oxy derivatives of tryptamine (6–8, 13–14) are reported. It was found that N- hydroxytryptamine (6) is a relatively selective ligand for the 5-HT 1C receptor. The receptor- binding data are interpreted by a molecular modeling study in which the binding sites of the 5-HT 1A and 5-HT 1C receptors are compared. An asparagine residue present in helix 7 ...