Partial agonists and subunit selectivity at NMDA receptors

TY - JOUR

T1 - Partial agonists and subunit selectivity at NMDA receptors

AU - Risgaard, Rune

AU - Hansen, Kasper Bø

AU - Clausen, Rasmus Prætorius

N1 - Keywords: agonists, glutamate, ligand design, receptors, subunit selectivity

PY - 2010/12/17

Y1 - 2010/12/17

N2 - Subunit-selective ligands for glutamate receptors remains an area of interest as glutamate is the major excitatory neurotransmitter in the brain and involved in a number of diseased states in the central nervous system (CNS). Few subtype-selective ligands are known, especially among the N-methyl-D-aspartic acid (NMDA) receptor class. Development of these ligands seems to be a difficult task because of the conserved region in the binding site of the NMDA receptor subunits. A few scaffolds have been developed showing potential to differentiate between the NMDA receptors.

AB - Subunit-selective ligands for glutamate receptors remains an area of interest as glutamate is the major excitatory neurotransmitter in the brain and involved in a number of diseased states in the central nervous system (CNS). Few subtype-selective ligands are known, especially among the N-methyl-D-aspartic acid (NMDA) receptor class. Development of these ligands seems to be a difficult task because of the conserved region in the binding site of the NMDA receptor subunits. A few scaffolds have been developed showing potential to differentiate between the NMDA receptors.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1002/chem.201001366

DO - 10.1002/chem.201001366

M3 - Review

C2 - 20945316

SN - 0947-6539

VL - 16

SP - 13910

EP - 13918

JO - Chemistry: A European Journal

JF - Chemistry: A European Journal

IS - 47

ER -