Pharmacological properties of recombinant 'diazepam-insensitive' GABA(A) receptors

Neuropharmacology

Volumn 35, Issue 9-10, 1996, Pages 1307-1314

  Gunnersen, D ^a   Kaufman, C M ^a   Skolnick, P ^a  

^a NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES   (United States)

Author keywords

Benzodiazepine; Diazepam insensitive; GABA(A) receptor; Imidazobenzodiazepine; Recombinant receptors; Ro 15 4513

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 ETHYL 6,7 DIMETHOXY BETA CARBOLINE 3 CARBOXYLIC ACID METHYL ESTER; 5 BENZYLOXY 4 METHOXYMETHYL BETA CARBOLINE 3 CARBOXYLIC ACID ETHYL ESTER; 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A]THIENO[2,3 F][1,4]DIAZEPINE 3 CARBOXYLIC ACID TERT BUTYL ESTER; 6 BENZYLOXY 4 METHOXYMETHYL BETA CARBOLINE 3 CARBOXYLIC ACID ETHYL ESTER; 8 AZIDO 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPINE 3 CARBOXYLIC ACID ETHYL ESTER; 8 CHLORO 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPINE 3 CARBOXYLIC ACID TERT BUTYL ESTER; BENZODIAZEPINE DERIVATIVE; BETA CARBOLINE 3 CARBOXYLIC ACID METHYL ESTER; BETA CARBOLINE DERIVATIVE; DIAZEPAM; DM 236; DM 286; GABAERGIC RECEPTOR AFFECTING AGENT; IMIDAZO[1,5 A][1,4]BENZODIAZEPINE DERIVATIVE; PW 007A; PYRAZOLO[4,3 C]QUINOLINE DERIVATIVE; PZII 029; RADIOLIGAND; RECEPTOR SUBUNIT; RECOMBINANT RECEPTOR; SURICLONE; TRIAZOLAM; UNCLASSIFIED DRUG; ZG 234; ZOPICLONE;

ARTICLE; CELL LINE; CONTROLLED STUDY; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; KIDNEY CELL; LIGAND BINDING; PRIORITY JOURNAL; RECEPTOR AFFINITY; RECEPTOR BINDING;

ANIMALS; CELL LINE; CELL MEMBRANE; CEREBELLUM; DIAZEPAM; GABA MODULATORS; HUMANS; MALE; PLASMIDS; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; TRANSFECTION;

EID: 0030444049     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(96)00054-8     Document Type: Article

References (43)

1. Ausubel F.M., Brent R., Kingston R.E., Moore D.D., Seidman J.G., Smith J.A. and Struhl K. (Eds) (1989) Short Protocols in Molecular Biology, pp. 255-256. John Wiley, New York.
2. A Receptors and Anxiety: From Neurobiology to Treatment, Vol. 48 (Biggio G., Sanna E., Serra M. and Costa E., Eds), pp. 1-16. Raven Press, New York.
3. Cain M., Weber R., Guzman F., Cook J., Barker S., Rice K., Crawley J., Paul S., Skolnick P. β-Carbolines: synthesis, neurochemical, and pharmacologic actions on brain benzodiazepine receptors. J. Med. Chem. 25:1982;1081-1091.
4. A receptors. Eur. J. Pharmacol. Molec. Pharmacol. Sect. 244:1993;29-35.
5. Gu Z.Q., Wong G., Dominguez C., de Costa B.R., Rice K.C., Skolnick P. Synthesis and evaluation of imidazo[1,5-a]benzodiazepine esters with high affinities at "diazepam insensitive" benzodiazepine receptors. J. Med. Chem. 36:1993;1001-1006.
6. Hadingham K.L., Wingrove P.B., Wafford K.A., Bain C., Kemp J.A., Palmer K.J., Wilson A.W., Wilcox A.S., Sikela J.M., Ragan C.I., Whiting P.J. Role of the β subunit in determining the pharmacology of human γ-aminobutyric acid type A receptors. Molec. Pharmacol. 44:1993;1211-1218.
7. A receptors to the alcohol properties of Ro 15-4513 and related imidazobenzodiazepines. Pharmacol. Biochem. Behav. 52:1995;113-118.
8. 3H]Ro 15-4513 binding in the rodent brain and cultured cerebellar neuronal cells. Neurochem. Res. 19:1994;289-295.
9. A receptor α subunit is expressed only in cerebellar granule cells. J. Molec. Biol. 214:1990;619-624.
10. A/benzodiazepine receptor from rat cerebellum. J. Neurochem. 63:1994;371-374.
11. Kleingoor C., Wieland H.A., Korpi E.R., Seeburg P.H., Kettenmann H. Current potentiation by diazepam but not GABA sensitivity is determined by a single histidine residue. NeuroReport. 4:1993;187-190.
12. A receptor α6 subunit alters benzodiazepine affinity but not allosteric GABA effects. Eur. J. Pharmacol. 247:1993;23-27.
13. 3H]Ro 15-4513 binding sites. Eur. J. Pharmacol. 213:1992;323-329.
14. A receptor. Nature. 361:1993;356-359.
15. Lister R.G., Durcan M.J. Antagonism of the intoxicating effects of ethanol by the potent benzodiazepine receptor ligand Ro 19-4603. Brain Res. 482:1989;141-144.
16. A receptor selective for a behavioural alcohol antagonist. Nature. 346:1990;648-651.
17. 3H]Ro 15-4513 binding in intact cultured cerebellar granule cells. Eur. J. Pharmacol. 169:1989;53-60.
18. A/benzodiazepine receptor ligands. Med. Chem. Res. 5:1994;63-76.
19. A-gated chloride channels. J. Pharmacol. Exp. Ther. 246:1988;558-564.
20. A receptor populations with novel subunit combinations and drug binding profiles identified in brain by α5- and δ-subunit-specific immunopurification. J. Biol. Chem. 268:1993;5965-5973.
21. Petrack B., Czernik A., Cassidy J., Bernard P., Yokoyama N. Benzodiazepine receptor ligands with opposing pharmacologic actions. Adv. Biochem. Psychopharm. 38:1983;129-137.
22. A receptor subunit for benzodiazepine pharmacology. Nature. 338:1989;582-585.
23. Quirk K., Gillard N.G., Ragan C.I., Whiting P.J., McKernan R.M. Model of subunit composition of γ-aminobutyric acid A receptor subtypes expressed in rat cerebellum with respect to their α and γ/δ subunits. J. Biol. Chem. 269:1994;16020-16028.
24. 3H]Ro 15-4513: biochemical and autoradiographic study. J. Neurochem. 48:1987;46-52.
25. Suzdak P.D., Glowa J.R., Crawley J.N., Schwartz R.D., Skolnick P., Paul S.M. A selective imidazobenzodiazepine antagonist of ethanol in the rat. Science. 234:1986;1243-1247.
26. Suzdak P.D., Schwartz R.D., Skolnick P., Paul S.M. Ethanol stimulates γ-aminobutyric acid-mediated chloride transport in rat brain synaptoneurosomes. Proc. Natn. Acad. Sci. U.S.A. 83:1986;4071-4075.
27. Syapin P.J., Gee K.W., Alkana R.L. Ro 15-4513 differentially affects ethanol-induced hypnosis and hypothermia. Brain Res. Bull. 19:1987;603-605.
28. A receptor subtype that is insensitive to diazepam. J. Pharmacol. Exp. Ther. 257:1991;1236-1242.
29. 3H]Ro 15-4513, in cerebellar membranes from two rat lines developed for high and low alcohol sensitivity. J. Neurochem. 54:1990;1980-1987.
30. A receptors depend upon subunit composition. Neuron. 4:1990;919-928.
31. A receptor. J. Med. Chem. 37:1994;4576-4580.
32. A receptors is essential for benzodiazepine agonist binding. J. Biol. Chem. 267:1992;1426-1429.
33. A receptor α4 subunit. FEBS Lett. 289:1991;227-230.
34. Wisden W., Laurie D.J., Monyer H., Seeburg P.H. The distribution of 13 GABA-A receptor subunit mRNAs in the rat brain. I. Telencephalon, diencephalon, mesencephalon J. Neurosci. 12:1992;1040-1062.
35. Wong G., Skolnick P. High affinity ligands for "diazepam-insensitive" benzodiazepine receptors. Eur. J. Pharmacol. Molec. Pharmacol. Sect. 225:1992;63-68.
36. A receptors:subunit composition determines ligand efficacy. Pharmacol. Biochem. Behav. 42:1992;107-110.
37. A/benzodiazepine receptors. Med. Chem. Res. 32:1992;217-224.
38. A/benzodiazepine receptors in a transfected cell line. Mol. Pharmacol. 42:1992;996-1003.
39. 3H]tert-butyl-8-chloro-5,6-dihydro-5-methyl-oxo-4H-imidazo[1,5a] [1,4]benzodiazepine-3-carboxylate (ZG-63). Eur. J. Pharmacol. Molec. Pharmacol. Sect. 247:1993;57-64.
40. Wong G., Koehler K.F., Skolnick P., Gu Z.G., Ananthan S., Schonholzer P., Hunkeler W., Zhang W., Cook J.M. Synthetic and computer-assisted analysis of the structural requirements for selective, high-affinity ligand binding to diazepam-insensitive benzodiazepine receptors. J. Med. Chem. 36:1993;1820-1830.
41. A receptor α4 subunit: identification of a unique diazepam-insensitive binding site. Eur. J. Pharmacol. 291:1995;319-325.
42. A receptor α subunit. FEBS Lett. 258:1989;119-122.
43. A receptors. J. Med. Chem. 38:1995;1679-1688.