Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2565-8. doi: 10.1016/s0960-894x(03)00504-3.

Abstract

The synthesis and 5-HT(2A) receptor affinities of 2-substituted-5-aminomethyl-10,11-dihydrodibenzo[a,d]cycloheptene (AMDH) derivatives are described. Comparison of the effects of substitution on affinities allowed assignment of potential binding modes in comparison with DOB-like agonists/antagonists and 3-substituted 1-(aminomethyl)-9,10-dihydroanthracene structures.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Cyclopentanes / chemical synthesis
  • Cyclopentanes / pharmacology*
  • Indicators and Reagents
  • Kinetics
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Conformation
  • Radioligand Assay
  • Receptor, Serotonin, 5-HT2A / drug effects
  • Receptor, Serotonin, 5-HT2A / metabolism*
  • Serotonin Agents / chemical synthesis*
  • Serotonin Agents / pharmacology*
  • Structure-Activity Relationship

Substances

  • 5-aminomethyl-10,11-dihydro-dibenzo(a,d)cycloheptene
  • Cyclopentanes
  • Indicators and Reagents
  • Ligands
  • Receptor, Serotonin, 5-HT2A
  • Serotonin Agents