PMID: 7086410Jul 1, 1982Paper

3H]nitrobenzylthioinosine binding as a probe for the study of adenosine uptake sites in brain

Journal of Neurochemistry
P J MarangosA M Martino

Abstract

The binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membrane fractions was investigated. Reversible, saturable, specific, high-affinity binding was demonstrated in both rat and human brain. The KD in both was 0.15 nM with Bmax values of 140-200 fmol/mg protein. Linear Scatchard plots were routinely obtained, indicating a homogeneous population of binding sites in brain. The highest density of binding sites was found in the caudate and hypothalamus in both species. The binding site was heat labile and trypsin sensitive. Binding was also decreased by incubation of the membranes in 0.05% Triton X-100 and by treatment with dithiothreitol and iodoacetamide. Of the numerous salt and metal ions tested, only copper and zinc had significant effects on [3H]NBI binding. The inhibitory potencies of copper and zinc were IC50 = 160 microM and 6 mM, respectively. Subcellular distribution studies revealed a high percentage of the [3H]NBI binding sites on synaptosomes, indicating that these sites were present in the synaptic region. A study of the tissue distribution of the [3H]NBI sites revealed very high densities of binding in erythrocyte, lung, and testis, with much lower binding densities in b...Continue Reading

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Citations

Jun 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·J DeckertP J Marangos
Jan 1, 1986·Pflügers Archiv : European journal of physiology·G Sanderson, C N Scholfield
Feb 1, 1985·Pflügers Archiv : European journal of physiology·J McCabe, C N Scholfield
Dec 3, 1982·European Journal of Pharmacology·P J MarangosJ Patel
Sep 30, 1983·European Journal of Pharmacology·P J MarangosS Weiss
Nov 19, 1985·European Journal of Pharmacology·P J MarangosP Montgomery
Jul 11, 1985·European Journal of Pharmacology·H MoritokiM Takei
Jul 6, 1993·European Journal of Pharmacology·J DeckertP Riederer
Jan 1, 1982·The International Journal of Biochemistry·P H Wu, J W Phillis
Jan 21, 1985·Life Sciences·A Verma, P J Marangos
Aug 25, 1986·Life Sciences·J Deckert, P J Marangos
Apr 1, 1987·Pharmacology, Biochemistry, and Behavior·S M AndersonG J Kant
Jan 1, 1985·Neuroscience and Biobehavioral Reviews·P J Marangos, J P Boulenger
Jan 1, 1984·Progress in Neuro-psychopharmacology & Biological Psychiatry·J W Phillis
Apr 11, 1983·Neuroscience Letters·J N CrawleyP J Marangos
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Jul 3, 2018·Frontiers in Pharmacology·Marçal Pastor-Anglada, Sandra Pérez-Torras

Related Concepts

4-nitrobenzylthioinosine
Adenocard
Brain
Caudate Nucleus Structure
Plasma Membrane
Heart
Organum Vasculosum Laminae Terminalis
Inosine
August Rats
Synaptosomes

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