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Chemical Compound Review

SureCN1822413     2-[4-[4-(4-chloropyrazol-1...

Synonyms: AC1L1TYZ, AC1Q3AEM, LS-134938, E-4424, E4424, ...
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High impact information on Lesopitron

  • 1. The involvement of presynaptic 5-hydroxytryptamine1A (5-HT1A) autoreceptors in the anxiolytic-like properties of lesopitron (E-4424) (2-(4-[4-(4-chloro-1-pyrazolyl)butyl]-1- piperazinyl)pyrimidine) was studied [1].
  • E-4424 (2-(4-[4-(4-chloro-1-pyrazolyl)butyl]-1-piperazinyl)pyrimidine) was shown to be a 5-hydroxytryptamine1A receptor ligand in radioligand binding assays and in an in vitro guinea pig ileum preparation had both 5-hydroxytryptamine1A antagonist and agonist effects [2].
  • Previous studies have shown that the 5-HT1A receptor ligand, lesopitron (E-4424, 2-[4-[4-(4-chloro-1-pyrazolyl)butyl]-1-piperazinyl]pyrimidine), exerts potent anxiolytic-like effects in rodents and monkeys (Costall et al., 1992, J. Pharmacol. Exp. Ther. 262, 90) [3].


  1. Effect of acute administration of the 5-HT1A receptor ligand, lesopitron, on rat cortical 5-HT and dopamine turnover. Ballarín, M., Carceller, A., Guitart, X. Br. J. Pharmacol. (1994) [Pubmed]
  2. Profile of action of a novel 5-hydroxytryptamine1A receptor ligand E-4424 to inhibit aversive behavior in the mouse, rat and marmoset. Costall, B., Domeney, A.M., Farre, A.J., Kelly, M.E., Martinez, L., Naylor, R.J. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  3. Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat. Haj-Dahmane, S., Jolas, T., Laporte, A.M., Gozlan, H., Farré, A.J., Hamon, M., Lanfumey, L. Eur. J. Pharmacol. (1994) [Pubmed]
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