Gaboxadol, a selective extrasynaptic GABAA agonist, does not generalise to other sleep-enhancing drugs: A rat drug discrimination study

Neuropharmacology

Volumn 52, Issue 3, 2007, Pages 844-853

  McDonald, L M ^a   Sheppard, W F ^a   Staveley, S M ^a   Sohal, B ^a   Tattersall, F D ^a   Hutson, P H ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

Abuse liability; Benzodiazepines; Extrasynaptic receptor; GABAA receptor; Gaboxadol; Sleep

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1BETAGAMMA; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA4BETAGAMMA; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; GABOXADOL; INDIPLON; TIAGABINE; UNCLASSIFIED DRUG; ZOLPIDEM; ZOPICLONE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISCRIMINATION; DRUG EFFECT; MALE; NONHUMAN; PRIORITY JOURNAL; RACEMIC MIXTURE; RAT; RECEPTOR INTRINSIC ACTIVITY; SLEEP; SLOW WAVE SLEEP; SPRAGUE DAWLEY RAT; STIMULUS GENERALIZATION;

ANIMALS; CONDITIONING, OPERANT; DISCRIMINATION LEARNING; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION; DRUG INTERACTIONS; GABA AGONISTS; GENERALIZATION (PSYCHOLOGY); ISOXAZOLES; MALE; RATS; RATS, SPRAGUE-DAWLEY; SLEEP;

EID: 33846963868     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2006.10.009     Document Type: Article

References (57)

1. A receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. Journal of Biological Chemistry 276 42 (2001) 38934-38939
2. Agmo A., Pruneda R., Guzman M., and Gutierrez M. GABAergic drugs and conflict behavior in the rat: lack of similarities with the actions of benzodiazepines. Naunyn-Schmiedeberg's Archives of Pharmacology 344 (1991) 314-322
3. B agonist baclofen. Society for Neuroscience Abstracts 17 (1991) 1170
4. Ator N.A., and Griffiths R.R. Discriminative stimulus effects of atypical anxiolytics in baboons and rats. Journal of Pharmacology Experimental Therapeutics 237 2 (1986) 393-403
5. Ator N.A., and Griffiths R.R. Principles of drug abuse liability assessment in laboratory animals. Drug and Alcohol Dependence 70 (2003) S55-S72
6. A receptors of thalamocortical neurons: a molecular target for hypnotics. Journal of Neuroscience 25 50 (2005) 11513-11520
7. Bristow L.J., Cook G.P., Patel S., Curtis N., Mawer I., and Kulagowski J.J. Discriminative stimulus properties of the putative dopamine D3 receptor agonist, (+)-PD 128907: role of presynaptic dopamine D2 autoreceptors. Neuropharmacology 37 (1998) 793-802
8. A receptors. British Journal of Pharmacology 136 (2002) 965-974
9. Carlson J.N., Haskew R., Wacker J., Maisonneuve I.M., Glick S.D., and Jerussi T.P. Sedative and anxiolytic effects of zopiclone's enantiomers and metabolite. European Journal of Pharmacology 415 2-3 (2001) 181-189
10. Cognos. Cognos Plus Study #77. Insomnia (2004), Decision Resources Inc., Waltham, Massachusetts, USA
11. Corbett R., Fielding S., Cornfeldt M., and Dunn R.W. GABA mimetic agents display anxiolytic-like effects in the social interaction and elevated plus maze procedures. Psychopharmacology 104 3 (1991) 312-316
12. Crestani F., Martin J.R., Mohler H., and Rudolph U. Mechanism of action of the hypnotic zolpidem in vivo. British Journal of Pharmacology 131 (2000) 1251-1254
13. Davies M., Newell J.G., Derry J.M.C., Martin I.L., and Dunn S.M.J. Characterization of the interaction of zopiclone with γ-aminobutyric acid type A receptors. Molecular Pharmacology 58 4 (2000) 756-762
14. Ebert B., Thompson S.A., Saounatsou K., McKernan R.M., Krogsgaard-Larsen P., and Wafford K.A. Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human γ-aminobutyric acid type A receptors. Molecular Pharmacology 52 (1997) 1150-1156
15. Ebert B., Storostovu S., Mortensen M., and Frolund B. Characterization of GABA(A) receptor ligands in the rat cortical wedge preparation: evidence for extrasynaptic receptors?. British Journal of Pharmacology 137 (2002) 1-8
16. Engel S.R., Purdy R.H., and Grant K.A. Characterization of discriminative stimulus effects of the neuroactive steroid pregnanolone. Journal of Pharmacology Experimental Therapeutics 297 2 (2001) 489-495
17. A agonist THIP produces slow-wave sleep and reduces spindling activity in NREM sleep in humans. Psychopharmacology 130 (1997) 285-291
18. Foster A.C., Pelleymounter M.A., Cullen M.J., Lewis D., Joppa M., Chen T.K., Bozigian H.P., Gross R.S., and Gogas K.R. In vivo characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. Journal of Pharmacology Experimental Therapeutics 311 2 (2004) 547-559
19. Georgiev V. (S)-Zopiclone. Current Opinion Investigational Drugs 2 2 (2001) 271-273
20. Grech D.M., and Balster R.L. Pentobarbital-like discriminative stimulus effects of direct GABA agonists in rats. Psychopharmacology 110 (1993) 295-301
21. Grech D.M., and Balster R.L. Discriminative stimulus effects of presynaptic GABA agonists in pentobarbital-trained rats. Pharmacology Biochemistry Behaviour 47 (1994) 5-11
22. Grech D.M., and Balster R.L. The discriminative stimulus effects of muscimol in rats. Psychopharmacology 129 (1997) 339-347
23. Jones H.E., and Balster R.L. Muscimol-like discriminative stimulus effects of GABA agonists in rats. Pharmacology Biochemistry Behaviour 59 2 (1998) 319-326
24. Julou L., Bardone M.C., Blanchard J.C., Garret C., and Stutzmann J.M. Pharmacological studies on zopiclone. Pharmacology 27 suppl. 2 (1983) 46-58
25. Jursky F., Tamura S., Tamura A., Mandiyan S., Nelson H., and Nelson N.M. Structure, function and brain localisation of neurotransmitter transporters. Journal of Experimental Biology 196 (1994) 283-295
26. Kopp C., Rudolph U., and Tobler I. Sleep EEG changes after zolpidem in mice. Neuroreport 15 14 (2004) 2299-2302
27. A agonist THIP (gaboxadol) increases non-REM sleep and enhances delta activity in the rat. Neuroreport 7 (1996) 2241-2245
28. A receptors in sleep regulation: differential effects of muscimol and midazolam on sleep in rats. Neuropsychopharmacology 15 1 (1996) 63-74
29. Lancel M., Faulhaber J., and Deisz R.A. Effect of the GABA uptake inhibitor tiagabine on sleep and EEG power spectra in the rat. British Journal of Pharmacology 123 (1998) 1471-1477
30. A agonist gaboxadol on nocturnal sleep and hormone secretion in healthy elderly subjects. American Journal of Physiology Endocrinology Metabolism 281 (2001) E130-E137
31. Lelas S., Spealman R.D., and Rowlett J.K. Using behavior to elucidate receptor mechanisms: a review of the discriminative stimulus effects of benzodiazepines. Experimental Clinical Psychopharmacology 8 3 (2000) 294-311
32. A agonist gaboxadol improves the quality of post-nap sleep. Psychopharmacology 157 (2001) 299-304
33. Mathias S., Wetter T.C., Steiger A., and Lancel M. The GABA uptake inhibitor tiagabine promotes slow-wave sleep in normal elderly subjects. Neurobiology of Aging 22 (2001) 247-253
34. Maurer R. The GABA agonist THIP, a muscimol analogue, does not interfere with the benzodiazepine binding site on rats' cortical membranes. Neuroscience Letters 12 1 (1979) 65-68
35. McKernan R.M., Rosahl T.W., Reynolds D.S., Sur C., Wafford K.A., Atack J.R., Farrar S., Myers J., Cook G., Ferris P., Garrett L., Bristow L., Marshall G., Macaulay A., Brown N., Howell O., Moore K.W., Carling R.W., Street L.J., Castro J.L., Ragan C.I., Dawson G.R., and Whiting P.J. Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype. Nature Neuroscience 3 6 (2000) 587-592
36. Nakajima T., Sasaki T., Nakagome K., Takazawa S., Ikebuchi E., Ito Y., Miyazawa Y., Tanaka M., and Kanno O. Comparison of the effects of zolpidem and zopiclone on nocturnal sleep and sleep latency in the morning: a cross-over study in healthy young volunteers. Life Science 67 (2000) 81-90
37. Nielsen E.B., Valentine J.D., Holohean A.M., and Appel J.B. Benzodiazepine receptor mediated discriminative cues: effects of GABA-ergic drugs and inverse agonists. Life Science 33 (1983) 2213-2220
38. Nielsen E.B., Suzdak P.D., Andersen K.E., Knutsen L.J.S., Sonnewald U., and Braestrup C. Characterization of tiagabine (NO-328), a new, potent and selective GABA uptake inhibitor. European Journal of Pharmacology 196 (1991) 257-266
39. A receptors to synaptic and extrasynaptic membranes of cerebellar granule cells. Journal of Neuroscience 18 5 (1998) 1693-1703
40. Overton D.A. Historical context of state dependent learning and discriminative drug effects. Behavioural Pharmacology 2 4-5 (1991) 253-264
41. A receptor changes in δ subunit-deficient mice: altered expression of α4 and γ2 subunits in the forebrain. Journal Comparative Neurology 446 (2002) 179-197
42. Areceptors. Journal of Pharmacology Experimental Therapeutics 317 (2006) 369-377
43. A receptors: immunocytochemical distribution of 13 subunits in the adult rat brain. Neuroscience 101 4 (2000) 815-850
44. Rauch R.J., and Stolerman I.P. Midazolam cue in rats: effects of drugs acting on GABA and 5-hydroxytryptamine systems, anticonvulsants and sedatives. Journal of Psychopharmacology 2 (1987) 71-80
45. Sanger D.J., and Zivkovic. The discriminative stimulus properties of zolpidem, a novel imidazopyridine hypnotic. Psychopharmacology 89 (1986) 317-322
46. Schmitt U., and Hiemke C. Tiagabine, a γ-amino-butyric acid transporter inhibitor impairs spatial learning of rats in the Morris water maze. Behavioural Brain Research 133 (1999) 391-394
47. Storustovu S., and Ebert B. Pharmacological characterisation of agonists at δ-containing GABAA receptors: functional selectivity for extrasynaptic receptors is dependent on absence of γ2. Journal of Pharmacology Experimental Therapeutics 316 (2006) 1351-1359
48. Suzdak P.D. Lack of tolerance to the anticonvulsant effects of tiagabine following chronic (21 day) treatment. Epilepsy Research 19 (1994) 205-213
49. Suzdak P.D., and Jansen J.A. A review of the preclinical pharmacology of tiagabine: a potent and selective anticonvulsant GABA uptake inhibitor. Epilepsia 36 6 (1995) 612-626
50. Swainston Harrison T.S., and Keating G.M. Zolpidem: a review of its use in the management of insomnia. CNS Drugs 19 1 (2005) 65-89
51. Thomson Scientific, 2006. Drug report for: indiplon (immediate release), Pfizer/Neurocrine. Philadelphia, USA, http://scientific.thomson.com. (accessed 14 Feb 2006).
52. A receptor modulators: in vitro-in vivo correlations. Journal of Pharmacology Experimental Therapeutics 304 (2003) 88-101
53. A receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-tolerance. European Journal of Pharmacology 482 (2003) 215-222
54. Wafford K.A., and Ebert B. Gaboxadol-a new awakening in sleep. Current Opinion in Pharmacology 6 (2006) 30-36
55. A receptors containing the α4 subunit. Journal of Pharmacology Experimental Therapeutics 50 (1996) 670-678
56. Yoshimoto M., Higuchi H., Kamata M., Yoshida K., Shimizu T., and Hishikawa Y. The effects of benzodiazepine (triazolam), cyclopyrrolone (zopiclone) and imidazopyridine (zolpidem) hypnotics on the frequency of hippocampal theta activity and sleep structure in rats. European Neuropsychopharmacology 9 (1999) 29-35
57. Zammit G.K., McNabb L.J., Caron J., Amato D.A., and Roth T. Efficacy and safety of eszopiclone across 6 weeks of treatment for primary insomnia. Current Medical Research Opinion 20 12 (2004) 1979-1991