Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3567-70. doi: 10.1016/s0960-894x(98)00646-5.

Abstract

Four 7-[3-(4-phenyl-1-piperazinyl)propoxy]coumarins were synthesized. The affinities of these compounds for DA (D2A, D3) and 5HT1A receptors were evaluated for their ability to displace [3H]-raclopride and [3H]-8-OH-DPAT respectively from their specific binding sites. The affinities of the target compounds were all in the nanomolar range and followed the order 5-HT1A > D2 > D3.

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Humans
  • Mice
  • Piperazines / chemistry*
  • Piperazines / metabolism
  • Piperazines / pharmacology*
  • Radioligand Assay
  • Receptors, Dopamine D2 / drug effects*
  • Receptors, Dopamine D2 / metabolism
  • Receptors, Dopamine D3
  • Receptors, Serotonin / drug effects*
  • Receptors, Serotonin / metabolism
  • Receptors, Serotonin, 5-HT1

Substances

  • DRD3 protein, human
  • Drd3 protein, mouse
  • Piperazines
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • phenylpiperazine