A potential 5-HT1A receptor antagonist: p-MPPI

Hank F. Kung, Mei Ping Kung, William Clarke, Saul Maayani, Zhi Ping Zhuang

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Abstract

A potential 5-HT1A receptor antagonist, p-MPPI, 4-(2'-methoxy-)phenyl-1-[2'-(n-2"-pyridinyl)-p-iodobenzamido-] ethyl-piperazine, was developed. The [125I]p-MPPI demonstrated high affinity and selectivity toward 5-HT1A receptors: Kd = 0.36 nM and Bmax = 264 fmol/mg of protein in rat hippocampal membrane homogenates. The binding is not sensitive to GTP (300μM) or Gpp(NH)p (100 μM). In forskolin-stimulated adenylyl cyclase assay using rat hippocampus, p-MPPI (up to 10 μM) showed no agonist activity as compared to that of (±)-8-OH-DPAT. At 100 nM it completely antagonized the inhibition of forskolin-stimulated adenylyl cyclase activity produced by 100 nM of (±)-8-OH-DPAT. This potential 5-HT1A antagonist may provide a powerful tool for studies of the pharmacology of the 5-HT1A receptor system.

Original languageEnglish (US)
Pages (from-to)1459-1462
Number of pages4
JournalLife Sciences
Volume55
Issue number19
DOIs
StatePublished - 1994
Externally publishedYes

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ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Kung, H. F., Kung, M. P., Clarke, W., Maayani, S., & Zhuang, Z. P. (1994). A potential 5-HT1A receptor antagonist: p-MPPI. Life Sciences, 55(19), 1459-1462. https://doi.org/10.1016/0024-3205(94)00686-5