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

NMDAR:10 nM

Traxoprodil exhibits potent activity by effectively blocking haloperidol-induced catalepsy at doses below 1 mg/kg and counteracting NMDA-induced c-fos induction in mice at a 1 mg/kg dosage [1]. Additionally, traxoprodil demonstrates antidepressant properties in the forced swim test at doses of 20 and 40 mg/kg without affecting locomotor activity in animals [2]. Furthermore, at a concentration of 20 nM administered intracerebroventricularly (i.c.v.), traxoprodil prolongs the onset of generalized tonic-clonic seizures triggered by PTZ (70 mg/kg; i.p.). At an oral dose of 60 mg/kg, it not only delays the initiation of clonic and generalized seizures but also reduces the total duration of seizures experienced [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].