Gaboxadol: In vitro interaction studies with benzodiazepines and ethanol suggest functional selectivity

European Journal of Pharmacology

Volumn 467, Issue 1-3, 2003, Pages 49-56

  Stórustovu, Signe í ^a   Ebert, Bjarke ^a  

^a H LUNDBECK A S   (Denmark)

Author keywords

Benzodiazepine; Ethanol; Gaboxadol; THIP

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; ALCOHOL; BENZODIAZEPINE RECEPTOR STIMULATING AGENT; DIAZEPAM; FLUMAZENIL; FLUNITRAZEPAM; GABOXADOL; INDIPLON; LORAZEPAM; UNCLASSIFIED DRUG; ZALEPLON; ZOLPIDEM;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BRAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ALCOHOL INTERACTION; DRUG EFFECT; DRUG MECHANISM; DRUG POTENTIATION; MALE; MOTOR ACTIVITY; NONHUMAN; OOCYTE; PRIORITY JOURNAL; RAT; XENOPUS;

EID: 0037466427     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(03)01603-0     Document Type: Article

References (20)

1. Adkins C.E., Pillai G.V., Kerby J., Bonnert T.P., Haldon C., McKernan R.M., Gonzalez J.E., Oades K., Whiting P.J., Simpson P.B. alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J. Biol. Chem. 276:2001;38934-38939.
2. Brown N., Kerby J., Bonnert T.P., Whiting P.J., Wafford K.A. Pharmacological characterization of a novel cell line expressing human alpha(4)beta(3)delta GABA(A) receptors. Br. J. Pharmacol. 136:2002;965-974.
3. Dämgen K., Lüddens H. Zaleplon displays a selectivity to recombinant GABAA receptors different from zolpidem, zopiclone, and benzodiazepines. Neurosci. Res. Comm. 25:1999;1686-1696.
4. Ebert B., Wafford K.A., Whiting P.J., Krogsgaard-Larsen P., Kemp J.A. Molecular pharmacology of gamma-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different alpha, beta, and gamma receptor subunit combinations. Mol. Pharmacol. 46:1994;957-963.
5. Ebert B., Thompson S.A., Saounatsou K., McKernan R., Krogsgaard-Larsen P., Wafford K.A. Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human gamma-aminobutyric acid type A receptors. Mol. Pharmacol. 52:1997;1150-1156.
6. Ebert B., Storustovu S., Mortensen M., Frølund B. Characterization of GABA(A) receptor ligands in the rat cortical wedge preparation: evidence for action at extrasynaptic receptors? Br. J. Pharmacol. 137:2002;1-8.
7. Faulhaber J., Steiger A., Lancel M. The GABAA agonist THIP produces slow wave sleep and reduces spindling activity in NREM sleep in humans. Psychopharmacology (Berl.). 130:1997;285-291.
8. Fritschy J.M., Möhler H. GABAA-receptor heterogeneity in the adult rat brain: differential regional and cellular distribution of seven major subunits. J. Comp. Neurol. 359:1995;154-194.
9. Hadingham K.L., Wingrove P., le Bourdelles B., Palmer K.J., Ragan C.I., Whiting P.J. Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma- aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol. Pharmacol. 43:1993;970-975.
10. 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. Role of the beta subunit in determining the pharmacology of human gamma- aminobutyric acid type A receptors. Mol. Pharmacol. 44:1993;1211-1218.
11. Harrison N.L., Simmonds M.A. Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex. Br. J. Pharmacol. 84:1985;381-391.
12. Lancel M. The GABA(A) agonist THIP increases non-REM sleep and enhances non-REM sleep-specific delta activity in the rat during the dark period. Sleep. 20:1997;1099-1104.
13. Lancel M. Role of GABAA receptors in the regulation of sleep: initial sleep responses to peripherally administered modulators and agonists. Sleep. 22:1999;33-42.
14. Lancel M., Faulhaber J. The GABAA agonist THIP (gaboxadol) increases non-REM sleep and enhances delta activity in the rat. NeuroReport. 7:1996;2241-2245.
15. Lancel M., Wetter T.C., Steiger A., Mathias S. Effect of the GABAA agonist gaboxadol on nocturnal sleep and hormone secretion in healthy elderly subjects. Am. J. Physiol., Endocrinol. Metabol. 281:2001;E130-E137.
16. Mathias S., Steiger A., Lancel M. The GABA(A) agonist gaboxadol improves the quality of post-nap sleep. Psychopharmacology (Berl.). 157:2001;299-304.
17. Sieghart W., Sperk G. Subunit composition, distribution and function of GABA(A) receptor subtypes. Curr. Top. Med. Chem. 2:2002;795-816.
18. Smith A.J., Alder L., Silk J., Adkins C., Fletcher A.E., Scales T., Kerby J., Marshall G., Wafford K.A., McKernan R.M., Atack J.R. Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux. Mol. Pharmacol. 59:2001;1108-1118.
19. Sperk G., Schwarzer C., Tsunashima K., Fuchs K., Sieghart W. GABA(A) receptor subunits in the rat hippocampus: I. Immunocytochemical distribution of 13 subunits. Neuroscience. 80:1997;987-1000.
20. Wisden W., Laurie D.J., Monyer H., Seeburg P.H. The distribution of 13 GABAA receptor subunit mRNAs in the rat brain: I. Telencephalon, diencephalon, mesencephalon. J. Neurosci. 12:1992;1040-1062.