Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). The rate of onset of inhibition by low concentrations of ifenprodil acting at NR1A/NR2B receptors was considerably slower than the onset of inhibition seen with high concentrations of ifenprodil acting at NR1A/NR2A receptors. The degree of inhibition seen with 100 microM ifenprodil at NR1A/NR2A receptors was not altered by changes in the concentration of extracellular glycine. However, the inhibitory effect of 1 microM ifenprodil at NR1A/NR2B receptors was reduced by increasing the concentration of glycine[3]. Moreover, ifenprodil decreased NMDA receptor equilibrium open probability by raising an energetic barrier to activation and also by biasing the receptor toward low open probability gating modes[4]. A single injection of ifenprodil (3 mg/kg, intraperitoneally (i.p.)) was sufficient to provoke rapid antidepressant-like effects in chronic unpredictable mild stress (CUMS) rats. Moreover, ifenprodil activated mTOR signaling and reversed the CUMS-induced elevation of interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) in the hippocampus after acute administration[5]. In the basolateral amygdala, ifenprodil dose dependently blocks excitatory transmission to principal neurons by a presynaptic mechanism. Ifenprodil reduces synaptic transmission in the basolateral amygdala by partially blocking P-type voltage-dependent calcium channels[6].
Japan
... 展开 >> Department of Psychiatry, Chiba University School of Medicine Chiba, Chuo-ku, Japan 260-8670
Recruiting
Chiba, Chuo-ku, Japan, 260-8670
Contact: Tsuyoshi Sasaki, MD +81-43-222-7171 sasaki@faculty.chiba-u.jp
Contact: Kenji Hashimoto, PhD +81-43-222-7171 hashimoto@faculty.chiba-u.jp
Principal Investigator: Masaomi Iyo, MD,PhD 收起 <<
Japan
... 展开 >> Department of Psychiatry, Chiba University School of Medicine Chiba, Chuo-ku, Japan 260-8670
Recruiting
Chiba, Chuo-ku, Japan, 260-8670
Contact: Tsuyoshi Sasaki, MD +81-43-222-7171 sasaki@faculty.chiba-u.jp
Contact: Kenji Hashimoto, PhD +81-43-222-7171 hashimoto@faculty.chiba-u.jp
Principal Investigator: Masaomi Iyo, MD,PhD 收起 <<
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