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Pseudoallosteric modulation by (+)-MK801 of NMDA-coupled phencyclidine binding sites.

作者信息

Reid A A, Monn J A, Jacobson A E, Rice K C, Rothman R B

机构信息

Unit on Receptor Studies, NIDDK, NIH Bethesda, MD 20892.

出版信息

Life Sci. 1990;47(16):PL77-82. doi: 10.1016/0024-3205(90)90531-u.

DOI:10.1016/0024-3205(90)90531-u
PMID:2174483
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.

摘要

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引用本文的文献

1
An electrophilic affinity ligand based on (+)-MK801 distinguishes PCP site 1 from PCP site 2.一种基于(+)-MK801的亲电亲和配体区分了PCP位点1和PCP位点2。
Neurochem Res. 1994 Apr;19(4):385-9. doi: 10.1007/BF00967314.