Subunit arrangement and phenylethanolamine binding in GluN1/GluN2B NMDA receptors.

ABSTRACT: Since it was discovered that the anti-hypertensive agent ifenprodil has neuroprotective activity through its effects on NMDA (N-methyl-D-aspartate) receptors, a determined effort has been made to understand the mechanism of action and to develop improved therapeutic compounds on the basis of this knowledge. Neurotransmission mediated by NMDA receptors is essential for basic brain development and function. These receptors form heteromeric ion channels and become activated after concurrent binding of glycine and glutamate to the GluN1 and GluN2 subunits, respectively. A functional hallmark of NMDA receptors is that their ion-channel activity is allosterically regulated by binding of small compounds to the amino-terminal domain (ATD) in a subtype-specific manner. Ifenprodil and related phenyl

SUBMITTER: Karakas E 

PROVIDER: S-EPMC3171209 | biostudies-literature | 2011 Jun

REPOSITORIES: biostudies-literature