Flesinoxan

Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC₅₀ value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects^[1][2][3]. In Vivo: Flesinoxan acts as a partial agonist at postsynaptic and as a full agonist at presynaptic 5-HT1A receptors. The capacity of Flesinoxan to antagonize the effect of 5-HT on CA3 pyramidal neurons was similar to that of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT)^[1].
The intravenous administration of Flesinoxan suppresses the firing activity of both CA3 pyramidal neurons and dorsal raphe 5-HT neurons. The acute brain penetration of [³H]Flesinoxan and [³H]8-OH-DPAT are determined. Nine minutes after intravenous administration, [³H]8-OH-DPAT reached significantly greater brain concentration than [³H]Flesinoxan^[1].
Subcutaneous administration of Flesinoxan and 8-OH-DPAT produce a dose-dependent hypothermia. The Flesinoxan-induced hypothermia is significantly attenuated by prior administration of the non-selective 5-HT1A antagonist pindolol and the 5-HT1/2 antagonist methysergide. Similar degrees of hypothermia are achieved with 3 mg/kg of Flesinoxan and 0.5 mg/kg of 8-OH-DPAT. The maximal effect of Flesinoxan occurs 30 min later than that of 8-OH-DPAT and fades more slowly^[1].