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Pharmacological profile of a potential anxiolytic: AP159, a new benzothieno-pyridine derivative

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Abstract

AP159 ([N-cyclohexyl-1,2,3,4-tetrahydrobenzo(b)thieno(2,3c)pyridine]-3-carboamide,hydrochloride) showed clear anti-conflict activity in rats in the absence of effects on muscle relaxation, potentiation of anesthesia (in mice) or anticonvulsant activity (in mice). This anticonflict effect was antagonized by treatment with Ro15-1788. By contrast with the deficits produced by diazepam, AP159 did not impair passive avoidance. The latter drug also improved scopolamine-induced amnesia in the same task. AP159 did not inhibit3H-flunitrazepam binding, but potently inhibited3H-8OH-DPAT binding. This compound increased serotonin and 5HIAA content of the midbrain raphe nuclei and of the amygdala centralis. AP159 has been shown to be a novel non-BZP anxiolytic agent with no side effects in laboratory animals; it could be a clinically effective anxiolytic agent.

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Correspondence to Tadashi Nagatani.

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Nagatani, T., Yamamoto, T., Takao, K. et al. Pharmacological profile of a potential anxiolytic: AP159, a new benzothieno-pyridine derivative. Psychopharmacology 104, 432–438 (1991). https://doi.org/10.1007/BF02245645

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Key words

  • AP159
  • Anxiolytic
  • 5HT1A receptor
  • Anti-amnesia
  • Rat
  • Mouse