A functional comparison of the antagonist bicuculline and picrotoxin at recombinant GABA(A) receptors

Neuropharmacology

Volumn 35, Issue 9-10, 1996, Pages 1289-1298

  Krishek, B J ^a   Moss, S J ^b   Smart, T G ^a  

^a UNIVERSITY OF LONDON   (United Kingdom)

^b UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

Bicuculline; Picrotoxin; Recombinant GABA(A) receptors; Xenopus oocyte

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; BICUCULLINE; PICROTOXIN; RECEPTOR SUBUNIT; RECOMBINANT RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; RECOMBINANT PROTEIN;

ALLOSTERISM; ANIMAL CELL; ARTICLE; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ANTAGONISM; FEMALE; GENE EXPRESSION; MEMBRANE CONDUCTANCE; MOUSE; NONHUMAN; OOCYTE; PRIORITY JOURNAL; XENOPUS LAEVIS; ANIMAL; CELL MEMBRANE POTENTIAL; COMPARATIVE STUDY; DRUG EFFECT; ELECTROPHYSIOLOGY; HUMAN; METABOLISM; PATCH CLAMP;

ANIMALS; BICUCULLINE; ELECTROPHYSIOLOGY; GABA AGONISTS; GABA ANTAGONISTS; HUMANS; MEMBRANE POTENTIALS; MICE; OOCYTES; PATCH-CLAMP TECHNIQUES; PICROTOXIN; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; XENOPUS LAEVIS;

EID: 0030329985     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(96)00089-5     Document Type: Article

References (34)

1. Arunlakshana P., Schild H.O. Some quantitative uses of drug antagonists. Br. J. Pharmac. Chemother. 14:1959;48-58.
2. A receptor form ion channels with properties of the native receptor. Science. 242:1988;577-579.
3. 1 (GABRR1) to human chromosome 6q14-q21 and mouse chromosome 4. Genomics. 12:1992;801-806.
4. Doble A., Martin I.L. Multiple benzodiazepine receptors: no reason for anxiety. Trends Pharmac. Sci. 13:1992;76-81.
5. 2+. Neuron. 5:1990;781-788.
6. Enz R., Bormann J. A single point mutation decreases picrotoxinin sensitivity of the human GABA receptor ρ1 subunit. NeuroReport. 6:1995;1569-1572.
7. ffrench-Constant R.H., Rocheleau T.A., Steichen J.C., Chalmers A.E. A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature. 363:1993;449-451.
8. A channel that abolish block by picrotoxin. Receptors and Channels. 3:1995;13-20.
9. A receptors containing bovine α1, β1, γ2L sub-units stably transfected into mouse fibroblast L-cells. Br. J. Pharmac. 107:1992;732-737.
10. Jenkinson D. How we describe competitive antagonists: three questions of usage. Trends Pharmac. Sci. 12:1991;53-54.
11. Kemp J.A., Marshall G.R., Woodruff G.N. Quantitative evaluation of the potencies of GABA-receptor agonists and antagonists using the rat hippocampal slice preparation. Br. J. Pharmac. 87:1986;677-684.
12. A receptor function by protein kinase C phosphorylation. Neuron. 12:1994;1081-1095.
13. A receptor ion channels: evaluation of pharmacological and physiological properties. Molec. Pharmac. 49:1996;494-504.
14. Macdonald R.L., Olsen R.W. GABA receptor channels. Ann. Rev. Neurosci. 17:1994;569-602.
15. Pritchett D.B., Sontheimer H., Shivers B.D., Ymer S., Kettenmann H., Schofield P.R., Seeburg P.H. Importance of a novel GABAA receptor subunit for benzodiazepine pharmacology. Nature. 338:1989;582-585.
16. A receptor research. Synapse. 21:1995;189-274.
17. A-benzodiazepine receptors. Trends Pharmac. Sci. 10:1989;407-411.
18. A receptor subtypes. Pharmac. Rev. 47:1995;182-234.
19. 2+ and amino-butyrate type A channels. Proc. Natn. Acad. Sci. U.S.A. 85:1988;6192-6196.
20. A receptor forms a picrotoxin sensitive anion channel open in the absence of GABA. Fedn Eur. Biochem. Socs Lett. 257:1989;377-379.
21. A receptors on channel function. Neuron. 5:1990;703-711.
22. Simmonds M.A. Classification of some GABA antagonists with regard to site of action and potency in slices of rat cuneate nucleus. Eur. J. Pharmac. 80:1982;347-358.
23. Simmonds M.A. (1990) Use of slices for quantitative pharmacology. In: Preparations of Vertebrate Central Nervous System in vitro (Jahnsen H., Ed.), pp. 49-76. John Wiley, Chichester.
24. Smart, T.G. (1996). Electrophysiology of GABA receptors. In: Amino Acid Neurotransmission. Portland Press, London, in press.
25. Smart T.G., Constanti A. Studies on the mechanism of action of picrotoxinin and other convulsants at the crustacean muscle GABA receptor. Proc. Roy. Soc. Lond. B. 227:1986;191-216.
26. Smart T.G., Constanti A., Houamed K., Bilbe G., Brown D.A., Barnard E.A. and VanRenterghem C. (1986) Expression of vertebrate amino acid receptors in Xenopus oocytes. In: Advances in Experimental Medicine and Biology: Excitatory Amino Acids and Epilepsy (Schwarcz R. and Ben-Ari Y., Eds), Vol. 203, pp. 525-542. Plenum Press, New York.
27. A receptors are differentially sensitive to zinc: dependence on subunit composition. Br. J. Pharmac. 103:1991;1837-1839.
28. Smart T.G., Xie X., Krishek B.J. Modulation of inhibitory and excitatory amino acid receptor ion channels by zinc. Progr. Neurobiol. 42:1994;393-441.
29. A receptor: dependence on receptor subunit combination. Br. J. Pharmac. 117:1996;521-527.
30. A receptors depend upon subunit composition. Neuron. 4:1990;919-928.
31. Wang T.-L., Hackam A.S., Guggino W.A., Cutting G.R. A single amino acid in γ-aminobutyric acid ρ1 receptors affects competitive and noncompetitive components of picrotoxin inhibition. Proc. Natn. Acad. Sci. U.S.A. 92:1995;11751-11755.
32. A receptor channel-lining residues probed in cysteine mutants. Biophys. J. 69:1995;1858-1867.
33. Zhang D., Pan Z.H., Zhang X., Brideau A.D., Lipton S.A. Cloning of a γ-aminobutyric acid type C receptor subunit in rat retina with a methionine residue critical for picrotoxinin channel block. Proc. Natn. Acad. Sci. U.S.A. 92:1995;11756-11760.
34. Zhang H.-G., Lee H.-J., Rocheleau T., ffrench-Constant R.H., Jackson M.B. Subunit composition determines picrotoxin and bicuculline sensitivity of Drosophila γ-aminobutyric acid receptors. Molec. Pharmac. 48:1995;835-840.