N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3325-8. doi: 10.1016/s0960-894x(99)00607-1.

Abstract

A series of N-phenylalkyl-substituted tropane analogs of boat conformation was synthesized, and these tropanes were evaluated for their ability to inhibit high affinity uptake of dopamine (DA) and serotonin (5-HT) into striatal nerve endings (synaptosomes). Some of these compounds exhibit high affinity for the DA transporter with a 5-HT/DA transporter selectivity ratio of >50.

Publication types

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

MeSH terms

  • Carrier Proteins / metabolism*
  • Dopamine / metabolism
  • Dopamine Plasma Membrane Transport Proteins
  • In Vitro Techniques
  • Membrane Glycoproteins / metabolism*
  • Membrane Transport Proteins*
  • Nerve Tissue Proteins*
  • Serotonin / metabolism
  • Serotonin Plasma Membrane Transport Proteins
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism
  • Tropanes / chemistry
  • Tropanes / metabolism*
  • Tropanes / pharmacology

Substances

  • Carrier Proteins
  • Dopamine Plasma Membrane Transport Proteins
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Serotonin Plasma Membrane Transport Proteins
  • Tropanes
  • Serotonin
  • Dopamine