N??Acetyl??5??arylalkoxytryptamine Analogs: Probing the Melatonin Receptors for MT1??Selectivity

…, S Sethi, PA Witt??Enderby, DP Zlotos

Index: Markl, Christian; Clafshenkel, William P.; Attia, Mohamed I.; Sethi, Shalini; Witt-Enderby, Paula A.; Zlotos, Darius P. Archiv der Pharmazie, 2011 , vol. 344, # 10 p. 666 - 674

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Citation Number: 15

Abstract

Abstract A series of melatonin analogs obtained by the replacement of the ether methyl group with larger arylalkyl and aryloxyalkyl substituents was prepared in order to probe the melatonin receptors for MT 1-selectivity. The most MT 1-selective agents 11 and 15 were substituted with a Ph (CH 2) 3 or a PhO (CH 2) 3 group. Compounds 11 and 15 displayed 11.5-fold and 11-fold higher affinity for the MT 1 receptors than for the MT 2 subtype. ...