(R)-CPPene(SDZ EAA 494)

Midafotel (SDZ-EAA 494) is a potent and comprtitive NMDA antagonist with an ED50 value of 39 nM. Midafotel causes intense stereotyped behaviors. Midafotel shows neuroprotective effects[1][2][3].

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

NMDA Receptor:39 nM ()

Midafotel (15 mg/kg；腹腔注射) 在大鼠中引起强烈的刻板行为[2]。 Midafotel (1.5、4.5、15 mg/kg；静脉注射；在 MCA 阻塞前 15 分钟开始 (随后以 1、3 或 10 mg/kg/h 持续输注)) 产生剂量依赖性体积减少梗死; 4.5 mg/kg剂量对大鼠局灶性脑缺血最有效[3]。 Animal Model: Adult female Wistar rats[2] Dosage: 15 mg/kg Administration: I.p. Result: Induced the typical PCP-like behavioral syndrome with ataxia, hyperlocomotion and stereotyped behaviors, i.e., head weaving, stereotyped sniffing, face washing and grooming, significantly increased extracellular levels of HVA and 5-HIAA in the striatum.

[1]. Lowe DA, et al. D-CPP-ene (SDZ EAA 494), a potent and competitive N-methyl-D-aspartate (NMDA) antagonist: effect on spontaneous activity and NMDA-induced depolarizations in the rat neocortical slice preparation, compared with other CPP derivatives and MK-801. Neurosci Lett. 1990 Jun 8;113(3):315-21.  

[2]. Potschka H, et al. Effects of the NMDA receptor antagonist D-CPPene on extracellular levels of dopamine and dopamine and serotonin metabolites in striatum of kindled and non-kindled rats. Eur J Pharmacol. 1999 Jun 18;374(2):175-87.  

[3]. Park CK, McCulloch J, Kang JK, Choi CR. Efficacy of D-CPPene, a competitive N-methyl-D-aspartate antagonist in focal cerebral ischemia in the rat. Neurosci Lett. 1992 Nov 23;147(1):41-4.