A single amino acid confers barbiturate sensitivity upon the GABA ρ1 receptor

British Journal of Pharmacology

Volumn 127, Issue 3, 1999, Pages 601-604

  Belelli, Delia ^a   Pau, Davide ^a   Cabras, Giulia ^a   Peters, John A ^a   Lambert, Jeremy J ^a  

^a UNIVERSITY OF DUNDEE   (United Kingdom)

Author keywords

hexachlorocyclohexane; subunit; GABA(A) receptor; General anaesthetic; Pentobarbitone

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR; AMINO ACID; ANESTHETIC AGENT; BARBITURIC ACID DERIVATIVE; DELTA HEXACHLOROCYCLOHEXANE; ELTANOLONE; ISOLEUCINE; PENTOBARBITAL; PROPOFOL; RECEPTOR SUBUNIT; RECOMBINANT RECEPTOR; SERINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; DRUG SENSITIVITY; FEMALE; NEUROTRANSMISSION; NONHUMAN; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; XENOPUS LAEVIS;

ANESTHETICS, GENERAL; ANIMALS; BINDING SITES; CENTRAL NERVOUS SYSTEM DEPRESSANTS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GAMMA-AMINOBUTYRIC ACID; HUMANS; HYPNOTICS AND SEDATIVES; ISOLEUCINE; LINDANE; OOCYTES; PENTOBARBITAL; RECEPTORS, GABA-A; SERINE; STRUCTURE-ACTIVITY RELATIONSHIP; XENOPUS LAEVIS;

EID: 0033029755     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702611     Document Type: Article

References (19)

1. Amin, J. & Weiss, D.S. (1994). Homomeric ρ1 GABA channels: activation properties and domains. Receptors Channels, 2, 227-236.
2. Barnard, E.A., Skolnick, P., Olsen, R.W., Mohler, H., Sieghart, W., Biggio, G., Braestrup, C., Bateson, A.N. & Langer, S.Z. (1998). International Union of Pharmacology. XV. Subtypes of γ-aminobutyric acid A receptors: classification on the basis of subunit structure and receptor function. Pharmacol. Rev., 50, 291-313.
3. Belelli, D., Callachan, H., Hill Venning, C., Peters, J.A. & Lambert, J.J. (1996a). Interaction of positive allosteric modulators with human and Drosophila recombinant GABA receptors expressed in Xenopus laevis oocytes. Br. J. Pharmacol., 118, 563-576.
4. A receptors by pregnanediols. Neuropharmacology, 35, 1223-1231.
5. Belelli, D., Lambert, J.J., Peters, J.A., Wafford, K. & Whiting, P.J. (1997). The interaction of the general anesthetic etomidate with the γ-aminobutyric acid type A receptor is influenced by a single amino acid. Proc. Natl. Acad. Sci. U.S.A., 94, 11031-11036.
6. Colman, A. (1984). Expression of exogenous DNA in Xenopus oocytes. In Transcription and translation: A Practical approach. eds. Hames, B.D. & Higgins, S.J. pp. 49-68. IRL Press Ltd, Oxford.
7. Dempster, J. (1997). A new version of the Strathclyde Electrophysiology Software package running within the Windows environment. J. Physiol., 504, P57.
8. Franks, N.P. & Lieb, W.R. (1994). Molecular and cellular mechanisms of general anaesthesia. Nature, 367, 607-614.
9. Krasowski, M.D., Koltchine, V.V., Rick, C.E., Ye, Q., Finn, S.E. & Harrison, N.L. (1998). Propofol and other intravenous anesthetics have sites of action on the γ-aminobutyric acid type A receptor distinct from that for isoflurane. Mol. Pharmacol., 53, 530-538.
10. Kunkel, T.A., Roberts, J.D. & Zakour, R.A. (1987). Rapid and efficient site-specific mutagenesis without phenotypic selection. Methods Enzymol., 154, 367-382.
11. 3A(b)) expressed in Xenopus laevis oocytes. Br. J. Pharmacol., 124, 1667-1674.
12. McGurk, K.A., Pistis, M., Belelli, D., Hope, A.G. & Lambert, J.J. (1998). The effect of a transmembrane amino acid on etomidate sensitivity of an invertebrate GABA receptor. Br. J. Pharmacol., 124, 13-20.
13. 1 receptor GABA-ergic currents by alcohols and volatile anesthetics. J. Pharmacol. Exp. Ther., 277, 411-416.
14. A and glycine receptors. Nature, 389, 385-389.
15. 2L) and Drosophila (RDL) GABA receptors by a single amino acid residue. J. Physiol., 515, 3-18.
16. 1 receptor RNA induces bicuculline-, barbiturate-, and benzodiazepine-insensitive gamma-aminobutyric acid responses in Xenopus oocytes. Mol. Pharmacol., 41, 683-687.
17. Wick, M.J., Mihic, S.J., Ueno, S., Mascia, M.P., Trudell, J.R., Brozowski, S.J., Ye, Q., Harrison, N.L. & Harris, R.A. (1998). Mutations of γ-aminobutyric acid and glycine receptors change alcohol cutoff: evidence for an alcohol receptor? Proc. Natl. Acad. Sci. U.S.A., 95, 6504-6509.
18. A receptor. Eur. J. Neurosci., 9, 2225-2235.
19. Woodward, R.M., Polenzani, L. & Miuedi, R. (1992). Effects of hexachlorocyclohexanes on γ-aminobutyric acid receptors expressed in Xenopus oocytes by RNA from mammalian brain and retina. Mol. Pharmacol., 41, 1107-1115.