Premium
Investigation of the NMDA receptor complex: Radiolabeling, regional distribution and initial characterization of 123 I‐dextrorphan binding sites in rat brain
Author(s) -
Gildehaus F. J.,
Li H. F.,
Linke R.,
Dresel S.,
Hahn K.,
Tatsch K.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.25804401102
Subject(s) - dextrorphan , nmda receptor , chemistry , ionotropic effect , forebrain , dextromethorphan , pharmacology , receptor , antagonist , distribution (mathematics) , glutamate receptor , binding site , central nervous system , neuroscience , biochemistry , psychology , biology , mathematical analysis , mathematics
The NMDA receptor is involved in a variety of neurological and psychiatric disorders. Dextrorphan is a selective noncompetitive antagonist of the activated NMDA sub‐family of ionotropic glutamate receptors. The distribution of 3 H‐dextrorphan binding sites appears qualitatively similar to the distribution of NMDA receptors. In biodistri‐bution studies with n.c.a. 123 I radiolabeled dextrorphan the initial uptake in brain was moderate (0.36% I.D./g, 15 min. p.i.) but after 2 hrs 50% of the initial activity still remained in the brain. The regional binding sites are heterogeneously distributed throughout the rat forebrain. After treatment with MK‐801 a reduction up to 25% in the regional uptake of 123 I‐dextrorphan was observed.