Diazepam receptor: specific nuclear binding of [3H]flunitrazepam. | Zendy

H B Bosmann | Zendy; David P. Penney | Zendy; Kenneth R. Case | Zendy; Kathleen Averill | Zendy

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Diazepam receptor: specific nuclear binding of [3H]flunitrazepam.

Author(s) -

H B Bosmann,

David P. Penney,

Kenneth R. Case,

Kathleen Averill

Publication year - 1980

Publication title -

proceedings of the national academy of sciences

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.011

H-Index - 771

eISSN - 1091-6490

pISSN - 0027-8424

DOI - 10.1073/pnas.77.2.1195

Subject(s) - flunitrazepam , binding site , inosine , chemistry , hypoxanthine , cortex (anatomy) , ligand (biochemistry) , membrane , nuclear membrane , biophysics , cell nucleus , biochemistry , nucleus , receptor , biology , microbiology and biotechnology , gabaa receptor , enzyme , neuroscience , gene

Autoradiographic localization of [3H]flunitrazepam in nuclei of the rat cerebral cortex was further confirmed by biochemical analysis of specific nuclear binding. Highly purified rat cerebral cortex nuclei were shown to bind [3H]flunitrazepam specifically. The Kd(app) for nuclear binding was 28 nM for the nuclei compared with a Kd(app) of 1.1 nM for binding of [3H] flunitrazepam to synaptosomal membrane fractions of the same tissue. Inhibition of the nuclear binding with inosine and hypoxanthine was greater than inhibition of the synaptic membrane fractions. These results lead to to conclude that specific binding may occur at both the synaptic membrane and the nuclear levels and that different endogenous ligands may compete at each site for binding. Furthermore, the possibility exists for translocation and alteration of the bound ligand complex from membrane site to nuclear site.

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