Ifenprodil, a Novel NMDA Receptor Antagonist : Site and Mechanism of Action

Author(s): Keith Williams

Journal Name: Current Drug Targets

Volume 2 , Issue 3 , 2001

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Ifenprodil is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit. As such, it has become widely used as a tool to study subtypes of NMDA receptors both in vitro and in vivo, and as a tool for molecular studies of the properties and regulation of NMDA receptors. Ifenprodil has an unusual form of activity-dependence and its mechanism of action may involve an increase in proton inhibition of NMDA receptors. These properties are shared by analogs or derivatives of ifenprodil, some of which may be lead compounds for therapeutically useful NMDA antagonists. Such antagonists have potential as neuroprotectants, anticonvulsants, analgesics, and for the treatment of Parkinsons disease and other disorders of the nervous system. The location of the ifenprodil binding site on NMDA receptors and the structural and mechanistic basis of its effects are still unknown. Recent work suggests that at least part of the ifenprodil binding site is located in the R1 / R2 domain of the NR1 subunit. This region, like the S1 / S2 agonist binding domain, shares homology with bacterial periplasmic binding proteins.

Keywords: NMDA Receptor Antagonist, ifenprodil binding site, MK-801, NR1/NR2 receptors, Proton Inhibition, glycine-independent stimulation, leucine isoleucine valine binding protein (LIVBP)

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Article Details

Year: 2001
Published on: 01 March, 2012
Page: [285 - 298]
Pages: 14
DOI: 10.2174/1389450013348489
Price: $65

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