Nuclear benzodiazepine binding : possible interaction with thyroid hormone receptors

The biochemical and pharmacological properties of nuclear [3H]flunitrazepam in brain tissues were studied. Nuclear [3H]flunitrazepam binding is saturable for both central and peripheral binding sites. Inosine and hypoxanthine displace nuclear [3H]flunitrazepam binding with greater potency than the m...

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Veröffentlicht in:Neurochemical research 1993-03, Vol.18 (3), p.305-311
Hauptverfasser: DALEZIOS, Y, MATSOKIS, N
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description The biochemical and pharmacological properties of nuclear [3H]flunitrazepam in brain tissues were studied. Nuclear [3H]flunitrazepam binding is saturable for both central and peripheral binding sites. Inosine and hypoxanthine displace nuclear [3H]flunitrazepam binding with greater potency than the membrane [3H]flunitrazepam binding. Triiodothyronine (T3) increases the maximum number of binding sites (Bmax) of nuclear [3H]flunitrazepam binding in vitro while thyroxine (T4) does not have any effect. Diazepam reduces the affinity of nuclear 125I-T3 binding in vitro, while the Bmax is not affected significantly. Mild digestion of chromatin, using micrococcal nuclease, reveals that a major portion of nuclear [3H]flunitrazepam binding sites are located on chromatin. These data suggest a functional role for nuclear benzodiazepine binding and a possible modulatory effect of benzodiazepines on T3 binding with its nuclear receptors.
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subjects Animals
Benzodiazepines - metabolism
Biological and medical sciences
Brain - metabolism
Cell Nucleus - metabolism
Central nervous system
Central neurotransmission. Neuromudulation. Pathways and receptors
DNA - metabolism
Flunitrazepam - metabolism
Fundamental and applied biological sciences. Psychology
Hypoxanthine
Hypoxanthines - metabolism
Inosine - metabolism
Rats
Rats, Wistar
Receptors, Thyroid Hormone - metabolism
Thyroxine - pharmacology
Triiodothyronine - metabolism
Triiodothyronine - pharmacology
Vertebrates: nervous system and sense organs
title Nuclear benzodiazepine binding : possible interaction with thyroid hormone receptors
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