Traxoprodil 是一种有效的和选择性的NMDA拮抗剂，能够保护海马神经元，其 IC50=10 nM。

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

Traxoprodil is potent at blocking haloperidol-induced catalepsy and with an ED50 less than 1 mg/kg. Traxoprodil is effective at 1 mg/kg to block NMDA (i.p.) stimulated c-fos induction in mice [1]. Traxoprodil at a dose of 20 and 40 mg/kg exhibits antidepressant activity in the forced swim test and it is not related to changes in animals’ locomotor activity [2]. Traxoprodil (20 nM i.c.v.) increases the latency to generalized tonic-clonic seizures induced by PTZ (70 mg/kg; i.p.). Traxoprodil (60 mg/kg, p.o.) increases the latency to clonic and generalized seizures and decreases the total time spent in seizures [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].

134234-12-1

C20H25NO3

327.42

曲索罗地;CP101606

H2O:< 0.1 mg/mL (insoluble)
DMSO:62.5 mg/mL (190.89 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years