Identification of a [3H]muscimol photoaffinity substrate in the bovine gamma-aminobutyric acidA receptor alpha subunit.
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چکیده
منابع مشابه
Mapping the benzodiazepine photoaffinity-labelling site with sequence-specific gamma-aminobutyric acidA-receptor antibodies.
The gamma-aminobutyric acidA (GABAA) receptor purified from adult bovine cerebral cortex was photoaffinity-labelled with the agonist benzodiazepine [3H]flunitrazepam and the radioactivity shown to be coincident with a band with Mr 53,000 that was recognized by three anti-(GABAA receptor alpha 1 subunit sequence)-specific antibodies. Complete and limited CNBr cleavage of the purified photoaffini...
متن کاملIdentification of Benzodiazepine Binding Site Residues in the g2 Subunit of the g-Aminobutyric AcidA Receptor
g-Aminobutyric acidA receptor g-subunits are important for benzodiazepine (BZD) binding and modulation of the g-aminobutyric acid-mediated Cl current. Previously, by using g2/a1 chimeric subunits, we identified two domains of the g2-subunit, Lys-41-Trp-82 and Arg-114-Asp-161, that are, in conjunction, necessary and sufficient for high-affinity BZD binding. In this study, we generated additional...
متن کاملCloning of genomic and cDNA sequences encoding an invertebrate gamma-aminobutyric acidA receptor subunit.
11. Shivers, B. D., Killisch, I., Sprengel, R., Sontheimer, H., Kohler, M., Schofield, P. R. & Seeburg, P. H. (1989) Neuron 3,327-337 Sieghart, W. ( I 989) Trends Pharmacol. Sci. 10,407-41 1 Wisden, W., Morris, B. J., Darlison, M. G., Hunt, S. P. & Barnard, E. A. (1 988) Neuron I , 937-947 Wisden, W., Morris, B. J., Darlison, M. G., Hunt, S. P. & Barnard, E. A. ( 1989) Mol. Brain Res. 5,305-3 1...
متن کاملModifications of gamma-aminobutyric acidA receptor subunit expression in rat neocortex during tolerance to diazepam.
We evaluated whether tolerance to the antagonism of bicuculine-induced seizures by diazepam is associated with changes (i) in the content of mRNAs encoding for gamma-aminobutyric acidA (GABAA) receptor subunits, (ii) in the expression density of these subunits, and (iii) in the 1,4-benzodiazepine binding site characteristics in discrete neocortical structures. We found that in diazepam-tolerant...
متن کاملTwo tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allosteric modulation of gamma-aminobutyric acidA receptors.
Benzodiazepines (BZs) exert their therapeutic effects in the mammalian central nervous system at least in part by modulating the activation of gamma-aminobutyric acid (GABA)-activated chloride channels. To gain further insight into the mechanism of action of BZs on GABA receptors, we have been investigating structural determinants required for the actions of the BZ diazepam (dzp) on recombinant...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1994
ISSN: 0021-9258
DOI: 10.1016/s0021-9258(17)32003-3