Binding of indolylalkylamines at 5-HT2 serotonin receptors: examination of a hydrophobic binding region

RA Glennon, C Chaurasia, M Titeler

Index: Glennon, Richard A.; Chaurasia, Chandra; Titeler, Milt Journal of Medicinal Chemistry, 1990 , vol. 33, # 10 p. 2777 - 2784

Full Text: HTML

Citation Number: 25

Abstract

Taking advantage of a proposed hydrophobic region on 5-HTz receptors previously identified by radioligand-binding studies utilizing various phenylisopropylamine derivatives, we prepared and evaluated several N l-and/or Cl-alkyl-substituted derivatives of a- methyltryptamine in order to improve its affinity and selectivity. It was determined that substitution of an n-propyl or amyl group has similar effect on affinity regardless of location ...