The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzoadiazephine binding site

Neuroscience Letters

Volumn 245, Issue 2, 1998, Pages 85-88

  Sigel, Erwin ^a   Baur, Roland ^a   Netzer, Rainer ^b   Rundfeldt, Chris ^c  

^a UNIVERSITY OF BERN   (Switzerland)

^b GENION   (Germany)

^c ASTA MEDICA AG   (Germany)

Author keywords

Allosteric modulation; AWD 131 138; Benzodiazepine; Chloride ion currents; Diazepam; Ro 15 1788; Aminobutyric acid; Aminobutyric acid A receptor

Indexed keywords

1 (4 CHLOROPHENYL) 4 MORPHOLINO 3 IMIDAZOLIN 2 ONE; 4 AMINOBUTYRIC ACID A RECEPTOR; ANTICONVULSIVE AGENT; DIAZEPAM; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CHLORIDE CURRENT; DRUG EFFECT; DRUG RECEPTOR BINDING; NERVE CELL MEMBRANE POTENTIAL; NERVE CELL STIMULATION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; XENOPUS;

EID: 0032478509     PISSN: 03043940     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0304-3940(98)00186-4     Document Type: Article

References (20)

1. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature. 366:1993;565-569.
2. A receptors alters specificity for ligands of the benzodiazepine binding site. Proc. Natl. Acad. Sci. USA. 94:1997;8824-8829.
3. A receptor affecting modulation of the channel by ligands of the benzodiazepine binding site. Mol. Pharmacol. 49:1996;1080-1084.
4. A receptors drastically alter the affinity for ligands of the benzodiazepine binding site. J. Biol. Chem. 272:1997;11799-11804.
5. A receptors influence affinities for benzodiazepine binding site ligands. Mol. Pharmacol. 52:1997;676-682.
6. A receptor subtypes: from pharmacology to molecular biology. FASEB J. 5:1991;2916-2923.
7. A receptor. Intern. Rev. Neurobiol. 36:1994;51-96.
8. A receptor channels, Annu. Rev. Neurosci. 17:1994;569-602.
9. Mihic S.J., Whiting P.J., Klein R.L., Wafford K.A., Harris R.A. A single amino acid of the human γ-aminobutyric acid type A receptor γ2 subunit determines benzodiazepine efficacy. J. Biol. Chem. 269:1994;32768-32773.
10. A receptor subunit for benzodiazepine pharmacology. Nature. 338:1989;582-585.
11. A receptor research. Synapse. 21:1995;189-274.
12. Rostock, A., Tober, C., Dost, R., Rundfeldt, C., Bartsch, R., Egerland, U., Stark, B., Schupke, H., Kronbach, T., Lankau, H.-J., Unverferth, K. and Engel, J., AWD 131-138, Drugs for the Future, (1998) in press.
13. Schofield P.R., Darlison M.G., Fujita N., Burt D.R., Stephenson F.A., Rodriguez H., Rhee L.M., Ramachandran J., Reale V., Glencorse T.A., Seeburg P.H., Barnard E.A. Sequence and functional expression of the GABA-A receptor shows a ligand-gated receptor superfamily. Nature. 328:1987;221-227.
14. Seen G.A., Wolf H.H., White H.S. AWD 131-138 enhances GABA-evoked whole-cell currents of mouse cortical neurons. Epilepsia. 36(S4):1995;50.
15. A receptor subtypes. Pharmacol. Rev. 47:1995;181-233.
16. A receptors. Trends Pharmacol. Sci. 18:1997;425-429.
17. A receptor channels. EMBO J. 11:1992;2017-2023.
18. A receptors on channel function. Neuron. 5:1990;703-711.
19. Sigel E., Stephenson F.A., Mamalaki C., Barnard E.A. A γ-aminobutyric acid/benzodiazepine receptor complex of bovine cerebral cortex: purification and partial characterization. J. Biol. Chem. 258:1983;6965-6971.
20. A receptor α-subunit. J. Biol. Chem. 269:1994;20380-20387.