Interaction of chiral MS-245 analogs at h5-HT6 receptors

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3510-3. doi: 10.1016/j.bmcl.2005.05.092.

Abstract

Optically active pyrrolidinylmethylindole analogs related in structure to the benzenesulfonyltryptamine 5-HT(6) receptor antagonist MS-245 were evaluated and their R-isomers were found to bind with affinity higher than their S-enantiomers.

Publication types

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

MeSH terms

  • Binding Sites
  • Drug Interactions
  • Humans
  • Indoles / chemistry
  • Pyrrolidines / chemistry
  • Receptors, Serotonin / chemistry
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / chemistry
  • Serotonin Antagonists / pharmacology*
  • Structure-Activity Relationship
  • Tryptamines / chemistry*

Substances

  • Indoles
  • N1-benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine
  • Pyrrolidines
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Tryptamines
  • serotonin 6 receptor