Pseudoallosteric modulation by (+)-MK801 of NMDA-coupled phencyclidine binding sites.
A A Reid, J A Monn, A E Jacobson, K C Rice, Richard B Rothman
Life Sciences 1990 DOI: 10.1016/0024-3205(90)90531-u (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Peer reviewed |
|---|---|
| Population | Guinea pig brain tissue |
| Key points | PCP enhanced dissociation of [3H]TCP from both the NMDA-coupled site (site 1) and the dopamine-reuptake-carrier-associated site (site 2), while (+)-MK801 enhanced dissociation only from site 1. The authors conclude that PCP's interactions with both sites are more complex than previously appreciated and that further studies are needed to determine the mechanisms. |
Abstract
Two high affinity phencyclidine (PCP) binding sites, labelled by [3H] 1-[1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP), have been identified in guinea pig brain, with one site coupled to the N-methyl-D-aspartate (NMDA) receptor (site 1) and the other site associated with the dopamine reuptake carrier complex (site 2). In this study, PCP enhanced the dissociation of [3H]TCP from PCP site 1 and site 2, while (+)-MK801 only enhanced dissociation of [3H]TCP from PCP site 1. Although additional studies will be required to determine the exact mechanism(s) of these effects, these data demonstrate that the interactions of PCP with both site 1 and site 2 are more complex than previously appreciated.