Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4374-7. doi: 10.1016/j.bmcl.2007.03.043. Epub 2007 Mar 16.

Abstract

A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.

MeSH terms

  • Animals
  • Blood-Brain Barrier
  • Histamine H1 Antagonists / chemistry
  • Histamine H1 Antagonists / pharmacology*
  • Mice
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology*
  • Receptors, Histamine H3 / drug effects*
  • Serotonin Plasma Membrane Transport Proteins / drug effects*
  • Structure-Activity Relationship
  • Tetrahydroisoquinolines / chemistry
  • Tetrahydroisoquinolines / pharmacology*

Substances

  • Histamine H1 Antagonists
  • Pyrrolidines
  • Receptors, Histamine H3
  • Serotonin Plasma Membrane Transport Proteins
  • Tetrahydroisoquinolines