fenprodil is an atypical, selective, noncompetitive, voltage-independent partial antagonist of N-methyl-D-aspartate (NMDA) receptors. Its maximal inhibition is approximately at 90%. Ifenprodil inhibits GluN2B-containing receptors with high affinity and is more potent for GluN1/GluN2B receptors. Ifenprodil action is pH-dependent and may cause an increase in tonic proton inhibition. There is evidence that ifenprodil binds outside the ion channel pore to the large interlobe cleft of the NR2B N-terminal domain and acts at a discrete sites with an allosteric interaction. Mutations at distinct residues in the R domain of NR1 and NR2B greatly influence ifenprodil inhibition, thus it seems that this region may form part of the ifenprodil binding site. IC50 values of ifenprodil are 0.15 μM for NR2B subunit, 39 μM for NR2A, 29 μM for NR2C and 76 μM for NR2D.
产品描述
An Antagonist of NMDA Receptors
产品形式
fenprodil is an atypical, selective, noncompetitive, voltage-independent partial antagonist of N-methyl-D-aspartate (NMDA) receptors. Its maximal inhibition is approximately at 90%. Ifenprodil inhibits GluN2B-containing receptors with high affinity and is more potent for GluN1/GluN2B receptors. Ifenprodil action is pH-dependent and may cause an increase in tonic proton inhibition. There is evidence that ifenprodil binds outside the ion channel pore to the large interlobe cleft of the NR2B N-terminal domain and acts at a discrete sites with an allosteric interaction. Mutations at distinct residues in the R domain of NR1 and NR2B greatly influence ifenprodil inhibition, thus it seems that this region may form part of the ifenprodil binding site. IC50 values of ifenprodil are 0.15 μM for NR2B subunit, 39 μM for NR2A, 29 μM for NR2C and 76 μM for NR2D.
保存建议
艾美捷为您提供的Alonmone Labs原装进口的Ifenprodil (+)-tartrate salt (hemitartrate salt) (50 mg)产品可室温运输,建议您在收到产品后将其置于合适的温度下保存。