Residues at positions 206 and 209 of the α1 subunit of γ-aminobutyric acid(A) receptors influence affinities for benzodiazepine binding site ligands

Molecular Pharmacology

Volumn 52, Issue 4, 1997, Pages 676-682

  Buhr, Andreas ^a   Schaerer, Martin T ^a   Baur, Roland ^a   Sigel, Erwin ^a  

^a UNIVERSITY OF BERN   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

3 METHYL 6 (3 TRIFLUOROMETHYLPHENYL) 1,2,4 TRIAZOLO[4,3 B]PYRIDAZINE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 ETHYL 6,7 DIMETHOXY BETA CARBOLINE 3 CARBOXYLIC ACID METHYL ESTER; BENZODIAZEPINE; DIAZEPAM; FLUMAZENIL; FLUNITRAZEPAM; MUSCIMOL; TRITIUM; ZOLPIDEM;

ARTICLE; BINDING AFFINITY; BINDING SITE; DOSE RESPONSE; DRUG RECEPTOR BINDING; GABAERGIC TRANSMISSION; GENE MUTATION; HUMAN; HUMAN CELL; LIGAND BINDING; NEUROTRANSMISSION; OOCYTE; PRIORITY JOURNAL; XENOPUS LAEVIS;

EID: 0030801390     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.52.4.676     Document Type: Article

References (35)

1. Sigel, E., F. A. Stephenson, C. Mamalaki, and E. A. Barnard. A γ-aminobutyric acid/benzodiazepine receptor complex of bovine cerebral cortex: purification and partial characterization. J. Biol. Chem. 258:6965-6971 (1983).
2. Schofield, P. R., M. G. Darlison, N. Fujita, D. R. Burt, F. A. Stephenson, H. Rodriguez, L. M. Rhee, J. Ramachandran, V. Reale, T. A. Glencorse, P. H. Seeburg, and E. A. Barnard. Sequence and functional expression of the GABA-A receptor shows a ligand-gated receptor superfamily. Nature (Lond.) 328:221-227 (1987).
3. A receptor subunit. Nature (Lond.) 385:820-823 (1997).
4. A receptor subtypes: from pharmacology to molecular biology. FASEB J. 5:2916-2923 (1991).
5. A receptor channels. Annu. Rev. Neurosci. 17:569-602 (1994).
6. A receptor. Int. Rev. Neurobiol. 36:51-96 (1994).
7. A receptor subtypes. Pharmacol. Rev. 47:181-233 (1995).
8. A receptor research. Synapse 21:189-274 (1995).
9. A receptor channels. EMBO J. 11:2017-2023 (1992).
10. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature (Lond.) 366:565-569 (1993).
11. A receptor α-subunit. J. Biol. Chem. 269:20380-20387 (1994).
12. A receptor subunit for benzodiazepine pharmacology. Nature (Lond.) 338:582-585 (1989).
13. A receptors on channel function. Neuron 5:703-711 (1990).
14. Mihic, S. J., P. J. Whiting, R. L. Klein, K. A. Wafford, and R. A. Harris. A single amino acid of the human γ-aminobutyric acid type A receptor γ2 subunit determines benzodiazepine efficacy. J. Biol. Chem. 269:32768-32773 (1994).
15. A receptor affecting modulation of the channel by ligands of the benzodiazepine binding site. Mol. Pharmacol. 49:1080-1084 (1996).
16. A receptors drastically alter the affinity for ligands of the benzodiazepine binding site. J. Biol. Chem. 272:11799-11804 (1997).
17. A receptors alters specificity for ligands of the benzodiazepine binding site. Proc. Natl. Acad. Sci. USA 94:8824-8829 (1997).
18. A receptor. FEBS Lett. 246:145-148 (1989).
19. A-receptor expressed from rat brain α- and β-subunit cDNAs display potentiation by benzodiazepine receptor ligands. Mol. Brain Res. 8:199-208 (1990).
20. A receptor. J. Neurosci. 10:2330-2337 (1990).
21. Chen, C., and H. Okayama. High-efficiency transformation of mammalian cells by plasmid DNA. Mol. Cell. Biol. 7:2745-2752 (1987).
22. 1) and the concentration of inhibitor which causes 50 per cent inhibition (150) of an enzymatic reaction. Biochem. Pharmacol. 22:3099-3108 (1973).
23. A receptor in the rat brain. Neurosci. Lett. 127:125-128 (1991).
24. A receptor in relation to specific GABAergic synapses in the dentate gyrus. Eur. J. Neurosci. 7:630-642 (1995).
25. A-benzodiazepine receptors by immunoaffinity chromatography. FEBS Lett. 284:15-18 (1991).
26. Sigel, E. Properties of single sodium channels translated by Xenopus oocytes after injection with messenger ribonucleic acid. J. Physiol. 386: 73-90 (1987).
27. 35S]t-butylcyclophosphorothionate binding sites modulated by several allosteric ligands of γ-aminobutyric acid type A receptors. Mol. Pharmacol. 48:385-391 (1995).
28. 3H]flunitrazepam binding in human embryonic kidney cell line 293. Eur. J. Pharmacol. 289:87-95 (1995).
29. A receptor form ion channels with properties of the native receptor. Science (Washington D. C.) 242:577-579 (1988).
30. A receptor subunits. Science (Washington D. C.) 242:1306-1308 (1988).
31. Chou, P. Y., and G. D. Fasman. Prediction of the secondary structure of proteins from their amino acid sequence. Adv. Enzymol. 47:45-148 (1978).
32. A receptors. Mol. Pharmacol. 51:833-841 (1997).
33. Pritchett, D. B., and P. H. Seeburg. γ-Aminobutyric acid type A receptor point mutation increases the affinity of compounds for the benzodiazepine site. Proc. Natl. Acad. Sci. USA 88:1421-1425 (1991).
34. A receptors is essential for benzodiazepine agonist binding. J. Biol. Chem. 267:1426-1429 (1992).
35. A receptor. Nature (Lond.) 361:356-359 (1993).