Pharmacological characterization of agonists at δ-containing GABAA receptors: Functional selectivity for extrasynaptic receptors is dependent on the absence of γ2

Journal of Pharmacology and Experimental Therapeutics

Volumn 316, Issue 3, 2006, Pages 1351-1359

  Stórustovu, Signe Í ^a   Ebert, Bjarke ^a  

^a H LUNDBECK A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

3 AMINO 2 (3 CARBOXYPROPYL) 6 (4 METHOXYPHENYL)PYRIDAZINIUM BROMIDE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 4 IMIDAZOLEACETIC ACID; 4 PIPERIDINESULFONIC ACID; 5 (4 PIPERDIYL) 3 ISOTHIAZOLOL; 5 (4 PIPERDIYL) 3 ISOXAZOLOL; ARECAIDINE; BICUCULLINE METHOCHLORIDE; GABOXADOL; ISOXAZOLE DERIVATIVE; LANTHANUM; MUSCIMOL; PARTIAL AGONIST; RECEPTOR SUBUNIT; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; ZINC ION;

ANIMAL CELL; ARTICLE; COMPARATIVE STUDY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; FEMALE; IN VIVO STUDY; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GABA AGONISTS; GAMMA-AMINOBUTYRIC ACID; HUMANS; ISOXAZOLES; LANTHANUM; PROTEIN SUBUNITS; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; XENOPUS LAEVIS; ZINC;

EID: 33644772587     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.105.092403     Document Type: Article

References (40)

1. A receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J Biol Chem 276:38934-38939.
2. Ator NA and Griffiths RR (1986) Discriminative stimulus effects of atypical anxiolytics in baboons and rats. J Pharmacol Exp Ther 237:393-403.
3. A receptors in hippocampal neurons. Mol Pharmacol 59:814-824.
4. Brickley SG, Revilla V, Cull-Candy SG, Wisden W, and Farrant M (2001) Adaptive regulation of neuronal excitability by a voltage-independent potassium conductance. Nature (Lond) 409:88-92.
5. A receptors. Br J Pharmacol 136:965-974.
6. A receptors. Bioorg Med Chem Lett 11:1573-1577.
7. A receptor ligands in the rat cortical wedge preparation: evidence for action at extrasynaptic receptors? Br J Pharmacol 137:1-8.
8. Ebert B, Thompson SA, Saounatsou K, McKernan R, Krogsgaard-Larsen P, and Wafford KA (1997) Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human γ-aminobutyric acid type A receptors. Mol Pharmacol 52:1150-1156.
9. Ebert B, Wafford KA, Whiting PJ, Krogsgaard-Larsen P, and Kemp JA (1994) Molecular pharmacology of γ-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different γ, β and γ receptor subunit combinations. Mol Pharmacol 46:957-963.
10. A agonist THIP produces slow wave sleep and reduces spindling activity in NREM sleep in humans. Psychopharmacology 130:285-291.
11. 6-containing receptors. Mol Pharmacol 49:253-259.
12. Hadingham KL, Wingrove PB, Wafford KA, Bain C, Kemp JA, Palmer KJ, Wilson AW, Wilcox AS, Sikela JM, Ragan CI, et al. (1993) Role of the β subunit in determining the pharmacology of human γ-aminobutyric acid type A receptors. Mol Pharmacol 44:1211-1218.
13. 6 subunit of the γ-aminobutyric acid type A receptor: lack of effect on responses to ethanol, pentobarbital and general anesthetics. Mol Pharmacol 51:588-596.
14. 6 subunits. J Neurosci 18:2449-2457.
15. 6 subunit gene inactivation inhibits δ subunit expression. J Neurosci 17:1350-1362.
16. Jones HE and Balster RL (1998) Muscimol-like discriminative stimulus effects of GABA agonists in rats. Pharmacol Biochem Behav 59:319-326.
17. A receptors on CA1 hippocampal neurons is consistent with subunit changes in a model of alcohol withdrawal and dependence. J Pharmacol Exp Ther 310:1234-1245.
18. Madsen SM, Lindeburg T, Folsgard S, Jacobsen E, and Sillesen H (1983) Pharmacokinetics of the γ-aminobutyric acid agonist THIP (Gaboxadol) following intramuscular administration to man, with observations in dog. Acta Pharmacol Toxicol 53:353-357.
19. A receptors responsible for tonic and phasic conductances. Neurochem Res 26:907-913.
20. A receptors. J Physiol (Lond) 532:17-30.
21. 6 subunit gene. Eur J Neurosci 11:1685-1697.
22. A receptors to synaptic and extrasynaptic membranes of cerebellar granule cells. J Neurosci 18:1693-1703.
23. 2 subunits in the forebrain. J Comp Neurol 446:179-197.
24. Rowlett JK, Spealman RD, and Lelas S (1999) Discriminative stimulus effects of zolpidem in squirrel monkeys: comparison with conventional benzodiazepines and sedative-hypnotics. J Pharmacol Exp Ther 291:1233-1241.
25. A receptor subtypes with gephyrin at postsynaptic sites. J Comp Neurol 420:481-498.
26. A receptor subunits: role of the δ subunit. J Neurosci 14:7077-7086.
27. A receptor subunit expression in rat CA1 hippocampus: pharmacological and behavioural effects. Neuropharmacology 49:573-586.
28. A receptor subtypes. Curr Top Med Chem 2:795-816.
29. A receptors are differentially sensitive to zinc: dependence on subunit composition. Br J Pharmacol 103:1837-1839.
30. A receptors. Proc Natl Acad Sci USA 100:14439-14444.
31. Storustovu S and Ebert B (2003) Gaboxadol: in vitro interaction studies with benzodiazepines and ethanol suggest functional selectivity. Eur J Pharmacol 467:49-56.
32. A receptors in hippocampal granule cells. Brain Res 1029:207-216.
33. A receptors are a target for alcohol. Nat Neurosci 5:721-722.
34. A receptor in rat thalamus. Mol Pharmacol 56:110-115.
35. A receptor δ subunit. Br J Pharmacol 120:283P.
36. A receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-tolerance. Eur J Pharmacol 482:215-222.
37. 4 subunit. Mol Pharmacol 50:670-678.
38. 3δ γ-aminobutyric acid type A receptors at low concentrations known to affect humans. Proc Natl Acad Sci USA 100:15218-15223.
39. A receptors and their activation by GABA spillover in the mouse dentate gyrus. J Neurosci 23:10650-10661.
40. A receptor complex: dependence on the second transmembrane domain of β subunits. J Physiol (Lond) 505:633-640.