1-(Benzofuran-2-yl)-2-(3,3,3-trifluoropropyl)aminopentane HCl, 3-F-BPAP, antagonizes the enhancer effect of (-)-BPAP in the shuttle box and leaves the effect of (-)-deprenyl unchanged

Joseph Knoll, Ildikó Miklya, Berta Knoll, Takuya Yasusa, Seiichiro Shimazu, Fumio Yoneda

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9 Citations (Scopus)

Abstract

The subcutaneous administration of 1 mg/kg tetrabenazine, once daily for 5 days, which depletes the catecholamine stores in the brain, significantly inhibits in rats the acquisition of a two-way conditioned avoidance reflex in the shuttle box. Enhancer substances, the tryptamine-derived selective and highly potent enhancer, R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane HCl [(-)-BPAP] (0.05-10 mg/kg), the β-phenylethylamine (PEA)-derived enhancer, (-)-deprenyl (1-5 mg/kg) and the (-)-deprenyl analogue, free of MAO-B inhibitory potency, (-)-1-phenyl-2-propylaminopentane HCl [(-)-PPAP], (1-5 mg/kg), antagonize in a dose-dependent manner the inhibition of learning caused by tetrabenazine. 1-(Benzofuran 2 yl)-2-(3,3,3-trifluoropropyl)aminopentane HCl [3 F BPAP], a newly synthetized analogue of (-)-BPAP with low specific activity, significantly antagonized the enhancer effect of (-)-BPAP but left the effect of (-)-deprenyl and (-)-PPAP unchanged. This is the first proof for a difference in the mechanism of action between a PEA-derived enhancer substance and its tryptamine-derived peer.

Original languageEnglish
Pages (from-to)1975-1984
Number of pages10
JournalLife Sciences
Volume71
Issue number17
DOIs
Publication statusPublished - Sep 13 2002

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Keywords

  • (-)-1-phenyl-2-propylaminopentane HCl [(-)-PPAP]
  • (-)-deprenyl
  • 1-(benzofuran-2-yl)-2-(3,3,3-trifluoropropyl)-aminopentane HCl [3-F-BPAP]
  • Enhancer substances
  • Enhancer-sensitive neurons
  • R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane HCl [(-)-BPAP]

ASJC Scopus subject areas

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

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