New 5-HT1A receptor antagonist: [3H]p-MPPF

Synapse. 1996 Aug;23(4):344-6. doi: 10.1002/(SICI)1098-2396(199608)23:4<344::AID-SYN13>3.0.CO;2-X.


A new 5-HT1A receptor antagonist ligand, [3H]p-MPPF, 4-(2'-methoxy-)-phenyl-1-[2'-(N-2"-pyridyl)-p-fluorobenzamido] ethyl-piperazine, was prepared and characterized. It demonstrated high affinity and selectivity toward 5-HT1A receptors (Kd = 0.34 +/- 0.12 nM and Bmax = 145 +/- 35 fmol/mg protein in rat hippocampal membrane homogenates). The binding is not sensitive to 100 microM Gpp(NH)p. Initial autoradiography studies of rat brain sections exhibit regional localization consistent with the known 5-HT1A receptor distribution. This potential 5-HT1A antagonist ligand may provide a powerful tool for 5-HT1A receptor pharmacology studies in the central nervous system.

Publication types

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

MeSH terms

  • Aminopyridines / metabolism*
  • Animals
  • Binding, Competitive
  • Hippocampus / metabolism*
  • Piperazines / metabolism*
  • Radioligand Assay
  • Rats
  • Serotonin Antagonists / metabolism*
  • Tritium


  • Aminopyridines
  • Piperazines
  • Serotonin Antagonists
  • Tritium
  • 4-(2' methoxyphenyl)-1-(2'-(N-(2''-pyridinyl)-4-fluorobenzamido)ethyl)piperazine