Eltoprazine is a partial agonist at SR-1 and SR-2C. Also, it is a 5-HT1A/1B receptor agonist.
5-HT 1 and 5-HT 2C receptor partial agonist (K i values are 40, 52 and 81 nM for 5-HT 1A , 5-HT 1B and 5-HT 2C receptors respectively). Reduces 5-HIAA levels in the striatum and exhibits antiaggressive behavior in vivo .
Rats are chronically treated with Mianserin (10 mg/kg i.p.) or Eltoprazine (1 mg/kg i.p.) and are tested in the elevated plus-maze test for anxiety. Mianserin and Eltoprazine display opposite effects in the elevated plus-maze: Mianserin induces anxiolytic-like effects, while Eltoprazine shows anxiogenic-like ones[2].
5-HT1A Receptor; 5-HT1B Receptor; 5-HT2C Receptor