- 生物活性
Flesinoxan 是一种降压剂，是一种有效的，高亲和力的选择性的 5-羟色胺 1A (5-HT1A) 受体激动剂，EC50 值为 24 nM。Flesinoxan 还具有有效的抗焦虑/抗抑郁作用。
- 靶点
5-HT
1A
Receptor
24 nM (EC
50
)
- 体内研究
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).
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 [
3
H]Flesinoxan and [
3
H]8-OH-DPAT are determined. Nine minutes after intravenous administration, [
3
H]8-OH-DPAT reached significantly greater brain concentration than [
3
H]Flesinoxan.
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.
