Mapping of GABAA receptor sites that are photoaffinity-labelled by [3H]flunitrazepam and [3H]Ro 15-4513

European Journal of Pharmacology

Volumn 298, Issue 3, 1996, Pages 313-319

  Duncalfe, Lori L ^a   Dunn, Susan M J ^a  

^a UNIVERSITY OF ALBERTA   (Canada)

Author keywords

Benzodiazepine; Flunitrazepam; GABAA receptor; Hydroxylamine; Ro 15 4513

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 8 AZIDO 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPINE 3 CARBOXYLIC ACID ETHYL ESTER; BENZODIAZEPINE RECEPTOR INVERSE STIMULATING AGENT; BENZODIAZEPINE RECEPTOR STIMULATING AGENT; DIAZEPAM; FLUNITRAZEPAM; HYDROXYLAMINE; PARTIAL AGONIST; REAGENT; RECEPTOR SUBUNIT; AZIDE; BENZODIAZEPINE DERIVATIVE; DIAGNOSTIC AGENT;

AMINO ACID SEQUENCE; ANIMAL TISSUE; ARTICLE; BINDING SITE; BRAIN CORTEX; BRAIN MEMBRANE; CATTLE; CEREBELLUM; CONTROLLED STUDY; LIGAND BINDING; NONHUMAN; PH; PHOTOAFFINITY LABELING; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROTEIN DOMAIN; AFFINITY LABELING; ANIMAL; BRAIN LEVEL; BRAIN MAPPING; IN VITRO STUDY; METABOLISM; MOLECULAR WEIGHT; PHYSIOLOGY; RADIOASSAY;

AFFINITY LABELS; ANIMALS; AZIDES; BENZODIAZEPINES; BRAIN CHEMISTRY; BRAIN MAPPING; CATTLE; CEREBELLUM; CEREBRAL CORTEX; ELECTROPHORESIS, POLYACRYLAMIDE GEL; FLUNITRAZEPAM; HYDROGEN-ION CONCENTRATION; HYDROXYLAMINES; MOLECULAR WEIGHT; RADIOLIGAND ASSAY; RECEPTORS, GABA-A;

EID: 0029670010     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/0014-2999(95)00811-X     Document Type: Article

References (32)

1. Barnard, E.A., 1992, Receptor classes and the transmitter-gated ion channels, Trends Biochem. Sci. 17, 368.
2. Binkley, P. and M.K. Ticku, 1991, Histidine residue is crucial for the binding of ligands to the benzodiazepine site except Ro15-4513, Eur. J. Pharmacol. Mol. Pharmacol. 208, 269.
3. Bornstein, P. and G. Balian, 1977, Cleavage at Asn-Gly bonds with hydroxylamine, Methods Enzymol. 47, 132.
4. Czajkowski, C. and D.H. Farb, 1986, Transmembrane topology and subcellular distribution of the benzodiazepine receptor, J. Neurosci. 6, 2857.
5. A receptor iso-oligomers, J. Biol. Chem. 265, 3831.
6. A receptors: differential effects of sulfhydryl modification, Eur. J. Pharmacol. Mol. Pharmacol. 246, 141.
7. A receptor from solubilized components, Biochemistry 28, 2545.
8. Ellis, K.J. and J.F. Morrison, 1982, Buffers of constant ionic strength for studying pH-dependent processes, Methods Enzymol. 87, 405.
9. A-benzodiazepine receptor complex, Neurosci. Lett. 90, 314.
10. Lambolez, B. and J. Rossier, 1987, Benzodiazepine agonists protect a histidine residue from modification by diethyl pyrocarbonate whereas propyl β-carboline does not, FEBS Lett. 219, 301.
11. Lambolez, B., C.-M. Deschamps and J. Rossier, 1989, Interactions of benzodiazepines and β-carbolines with a histidine residue of the benzodiazepine receptor, Neurochem. Int. 15, 145.
12. A receptor selective for a behavioural alcohol antagonist, Nature 346, 648.
13. Maksay, G., 1992, Modification of benzodiazepine receptors supports the distinctive role of histidine residues, Eur. J. Pharmacol. Mol. Pharmacol. 227, 57.
14. 3H]Ro15-4513 binding in intact cultured cerebellar granule cells, Eur. J. Pharmacol. 169, 53.
15. A receptor structure: analysis of ligand binding domains, Can. J. Physiol. Pharmacol. 72, S-28.
16. A receptor family in the mammalian brain, Neurochem. Res. 16, 317.
17. Otero de Bengtsson, M.S., H.D. Lacorazza, M.J. Biscoglio de Jiménex Bonino and J.H. Medina, 1993, Involvement of a disulfide bond in the binding of flunitrazepam to the benzodiazepine receptor from bovine cerebral cortex, J. Neurochem. 60, 536.
18. Pritchett, D.B. and P.H. Seeburg, 1991, γ-aminobutyric acid type A receptor point mutation increases the affinity of compounds for the benzodiazepine site, Proc. Natl. Acad. Sci. USA. 88, 1421.
19. Schägger, H. and G. Von Jagow, 1987, Tricine-sodium dodecyl sulfate-polyacrylamide gel electrophoresis for the separation of proteins in the range from 1 to 100 kDa, Anal. Biochem. 166, 368.
20. Schmitz, E., R. Reichelt, H. Möhler and J. Hebebrand, 1989, Photolabelled tryptic degradation products of benzodiazepine binding proteins are glycopeptides, FEBS Lett. 244, 433.
21. A receptor shows a ligand-gated superfamily, Nature 328, 221.
22. Sieghart, W., 1988, Comparison of two different benzodiazepine binding proteins by peptide mapping after limited proteolysis, Brain Res. 450, 387.
23. - ion channels modulated by multiple drug-binding sites, Trends Pharmacol. Sci. 13, 446.
24. 3H]Ro15-4513, J. Neurochem. 48, 1109.
25. 3H]Ro15-4513: a biochemical and autoradiographic study, J. Neurochem. 48, 46.
26. A receptors, Trends Pharmacol. Sci. 16, 162.
27. Stephenson, F.A. and M.J. Duggan, 1989, Mapping the benzodiazepine photoaffinity labelling site with sequence specific γ-aminobutyric acid A receptor antibodies, Biochem. J. 264, 199.
28. 1 polypeptide is the principle site of the agonist benzodiazepine photoaffinity labelling reaction, J. Biol. Chem. 265, 21160.
29. A receptor subtype that is insensitive to diazepam, J. Pharmacol. Exp. Ther. 257, 1236.
30. 3H]Ro15-4513 binding, J. Neurochem. 59, 560.
31. 3H]Ro15-4513, J. Neurochem. 59, 568.
32. A receptors is essential for benzodiazepine agonist binding, J. Biol. Chem. 267, 1426.