Traxoprodil (CP101606) is a selective NMDA antagonist and protects hippocampal neurons (IC50: 10 nM).

NMDAR:10 nM

Traxoprodil在阻断haloperidol引起的僵直中表现出强效，ED50小于1 mg/kg。1 mg/kg剂量下，Traxoprodil能有效阻断小鼠NMDA（i.p.）刺激的c-fos诱导[1]。Traxoprodil以20和40 mg/kg的剂量，在强迫游泳测试中显示出抗抑郁活性，并且这与动物的运动活动变化无关[2]。Traxoprodil（20 nM i.c.v.）能延长PTZ（70 mg/kg; i.p.）诱发的广泛强直-阵挛性发作的潜伏期。Traxoprodil（60 mg/kg, p.o.）能增加阵挛性和广泛性发作的潜伏期，并减少发作总时长[3]。

The effect of traxoprodil and SPD on PTZ-induced seizures is investigated by injecting the Adult (90-100 days-old) male Wistar rats (250-300 g) with traxoprodil (0.2, 2 or 20 nM/site), SPD (0.02, 0.2 or 2 nM/site), or with vehicle (0.9% NaCl, 1 μL) 15 min before the administration of PTZ (35 or 70 mg/kg, i.p.) [3]. The Forced swim test is done on male Albino Swiss mice (25-30 g). Traxoprodil (5, 10, 20, 40 mg/kg), imipramine and saline are administered i.p. 60 min before the test. The antidepressant activity is measured [2].