Benzodiazepines are weak inhibitors of [3H]nitrobenzylthioinosine binding to adenosine uptake sites in brain

J. Patel; P. J. Marangos; P. Skolnick; S. M. Paul; A. M. Martino

doi:10.1016/0304-3940(82)90368-8

Benzodiazepines are weak inhibitors of [³H]nitrobenzylthioinosine binding to adenosine uptake sites in brain

J. Patel, P. J. Marangos, P. Skolnick, S. M. Paul, A. M. Martino

Washington University School of Medicine

Research output: Contribution to journal › Article › peer-review

28 Scopus citations

Abstract

Saturable, specific, high affinity binding of the potent adenosine uptake inhibitor [³H]nitrobenzylthioinosine ([³H]NBI) to brain membranes has been demonstrated. In an effort to test the hypothesis that benzodiazepine action may be due to the inhibition of adenosine uptake, the inhibition of [³H]NBI binding by diazepam, clonazepam and chlordiazepoxide was tested. The benzodiazepines are very weak inhibitors of [³H]NBI binding, having IC₅₀ values several orders of magnitude above their therapeutic levels.

Original language	English
Pages (from-to)	79-82
Number of pages	4
Journal	Neuroscience Letters
Volume	29
Issue number	1
DOIs	https://doi.org/10.1016/0304-3940(82)90368-8
State	Published - Mar 17 1982

Keywords

adenosine uptake
benzodiazepine
binding sites
nitrobenzylthioinosine

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title = "Benzodiazepines are weak inhibitors of [3H]nitrobenzylthioinosine binding to adenosine uptake sites in brain",

abstract = "Saturable, specific, high affinity binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membranes has been demonstrated. In an effort to test the hypothesis that benzodiazepine action may be due to the inhibition of adenosine uptake, the inhibition of [3H]NBI binding by diazepam, clonazepam and chlordiazepoxide was tested. The benzodiazepines are very weak inhibitors of [3H]NBI binding, having IC50 values several orders of magnitude above their therapeutic levels.",

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AU - Paul, S. M.

AU - Martino, A. M.

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N2 - Saturable, specific, high affinity binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membranes has been demonstrated. In an effort to test the hypothesis that benzodiazepine action may be due to the inhibition of adenosine uptake, the inhibition of [3H]NBI binding by diazepam, clonazepam and chlordiazepoxide was tested. The benzodiazepines are very weak inhibitors of [3H]NBI binding, having IC50 values several orders of magnitude above their therapeutic levels.

AB - Saturable, specific, high affinity binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membranes has been demonstrated. In an effort to test the hypothesis that benzodiazepine action may be due to the inhibition of adenosine uptake, the inhibition of [3H]NBI binding by diazepam, clonazepam and chlordiazepoxide was tested. The benzodiazepines are very weak inhibitors of [3H]NBI binding, having IC50 values several orders of magnitude above their therapeutic levels.

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Benzodiazepines are weak inhibitors of [³H]nitrobenzylthioinosine binding to adenosine uptake sites in brain

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