iveFunctional NR2B-containing NMDA receptors are formed by their coassembly with the obligatory NR1 subunit.Although NR1 subunits are ubiquitously expressed in the CNS,the localization of NR2B subunits are more restri...iveFunctional NR2B-containing NMDA receptors are formed by their coassembly with the obligatory NR1 subunit.Although NR1 subunits are ubiquitously expressed in the CNS,the localization of NR2B subunits are more restricted.NR2B subunits are found in the spinal cord,and localized predominantly in the forebrain.The more discrete distribution of NR2B subunits in the CNS gives hope that antagonists selective for this receptor subtype would retain the known analgesic properties of other NMDA receptor antagonists without the profound side-effect profile.Indeed,NR2B-slective compounds are antinociceptive in a variety of preclinical pain models and have a much lower side-effect profile compared with other NMDA receptor antagonists.Therefore,NR2B subunit in the CNS could serve as a new target site for controlling persistent pain in humans.展开更多
文摘iveFunctional NR2B-containing NMDA receptors are formed by their coassembly with the obligatory NR1 subunit.Although NR1 subunits are ubiquitously expressed in the CNS,the localization of NR2B subunits are more restricted.NR2B subunits are found in the spinal cord,and localized predominantly in the forebrain.The more discrete distribution of NR2B subunits in the CNS gives hope that antagonists selective for this receptor subtype would retain the known analgesic properties of other NMDA receptor antagonists without the profound side-effect profile.Indeed,NR2B-slective compounds are antinociceptive in a variety of preclinical pain models and have a much lower side-effect profile compared with other NMDA receptor antagonists.Therefore,NR2B subunit in the CNS could serve as a new target site for controlling persistent pain in humans.
