Ifenprodil tartrate 是典型的非竞争性NMDA受体拮抗剂，抑制GIRK (Kir3)，通过基底 GIRK 活性减少内向电流，有用做脑血管舒张试剂的潜力。它对 NR1A/NR2B 受体亲和力是 NR1A/NR2A 受体的 400 倍。

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

Ifenprodil抑制NMDA（10 μM）和NMDA（100 μM）诱发的电流,IC 50值分别为0.88 μM和0.17μ。在大鼠皮质神经元中,Ifenprodil（10 μM）抑制大部分的NMDA受体诱发的电流。

In vitro biochemical and pharmacological assaysinhibition studies with recombinant human COX-1 and COX-2: Microsomal preparations of recombinant human COX-1 and COX-2 are prepared from a vaccinia virus-COS-7 cell expression system. Recombinant human COX-1 and COX-2 are expressed in baculovirus-Sf9 cells, and enzymes are purified. Enzymatic activity is monitored continuously by either a fluorescence assay measuring the appearance of the oxidized form of the reducing agent cosubstrate homovanillic acid or by oxygen consumption. The HPLC assay for the assessment of inhibition of purified COX-1 by Rofecoxib with 0.1 μM arachidonic acid substrate concentration, the determination of the stoichiometry of the complex between COX-2 and Rofecoxib, the dissociation rate constant of the enzyme-inhibitor complex by recovery of enzymatic activity, and the recovery of intact Rofecoxib from that complex are all performed as described previously. The solvent system for the HPLC analysis of Rofecoxib is 15:85 MeOH/aqueous potassium phosphate (1 g/liter), with elution by a linear gradient of 15 to 75% MeOH over 25 minutes with detection at 275 nm on a Novapak C18 column.

23210-58-4

C46H60N2O10

800.99

DMSO:88 mg/mL (163.4 mM)
Ethanol:58 mg/mL (107.7 mM)
H2O:9 mg/mL (11.23 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years