Agonist function of the recombinant α4β 3δ GABAA receptor is dependent on the human and rat variants of the α4-subunit

Clinical and Experimental Pharmacology and Physiology

Volumn 37, Issue 7, 2010, Pages 662-669

  Wang, Ming De ^a   Rahman, Mozibur ^a   Johansson, Inga Maj ^a   Bäckström, Torbjörn ^a  

^a UMEÅ UNIVERSITY   (Sweden)

Author keywords

GABA; GABAA receptor; pentobarbital; 4 subunit; 3 subunit; subunit

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA4; 4 AMINOBUTYRIC ACID A RECEPTOR BETA3; 4 AMINOBUTYRIC ACID A RECEPTOR DELTA; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; PENTOBARBITAL; RECOMBINANT RECEPTOR; UNCLASSIFIED DRUG; 4 AMINOBUTYRIC ACID A RECEPTOR; GABRA4 PROTEIN, HUMAN; GABRA4 PROTEIN, RAT; GABRB3 PROTEIN, HUMAN; GABRB3 PROTEIN, RAT; RECOMBINANT PROTEIN;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; FEMALE; GABAERGIC SYSTEM; GRANULE CELL; HIPPOCAMPUS; HUMAN; NONHUMAN; NUCLEOTIDE SEQUENCE; PROTEIN QUATERNARY STRUCTURE; RAT; RECEPTOR GENE; VOLTAGE CLAMP; WILD TYPE; XENOPUS; AGED; AGONISTS; ANIMAL; CELL CULTURE; DRUG EFFECTS; MALE; MIDDLE AGED; OOCYTE; PHYSIOLOGY; WISTAR RAT;

AGED; ANIMALS; CELLS, CULTURED; FEMALE; GABA-A RECEPTOR AGONISTS; GAMMA-AMINOBUTYRIC ACID; HIPPOCAMPUS; HUMANS; MALE; MIDDLE AGED; OOCYTES; PENTOBARBITAL; RATS; RATS, WISTAR; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; XENOPUS;

EID: 77953862217     PISSN: 03051870     EISSN: 14401681     Source Type: Journal    
DOI: 10.1111/j.1440-1681.2010.05374.x     Document Type: Article

References (41)

1. A receptor channels. Annu. Rev. Neurosci. 1994 17: 569 602.
2. A-benzodiazepine receptor subtypes. Adv. Biochem. Psychopharmacol. 1992 47: 155 162.
3. Nicoll RA, Eccles JC, Oshima T, Rubia F. Prolongation of hippocampal inhibitory postsynaptic potentials by barbiturates. Nature 1975 258: 625 627.
4. Belelli D, Lambert JJ, Peters JA, Wafford K, Whiting PJ. The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. Proc. Natl Acad. Sci. USA 1997 94: 11031 11036.
5. A responses in cells stably transfected with receptor subunits. Alcohol. Clin. Exp. Res. 1995 19: 226 232.
6. Majewska MD, Harrison NL, Schwartz RD, Barker JL, Paul SM. Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science 1986 232: 1004 1007.
7. Wang M, He Y, Eisenman LN et al. 3β-Hydroxypregnane steroids are pregnenolone sulfate-like GABA(A) receptor antagonists. J. Neurosci. 2002 22: 3366 3375.
8. Korpi ER, Grunder G, Luddens H. Drug interactions at GABA(A) receptors. Prog. Neurobiol. 2002 67: 113 159.
9. A receptor gene family: New opportunities for drug development. Curr. Opin. Drug Discov. Devel. 2003 6: 648 657.
10. A receptor: Recruitment by tracazolate and neurosteroids. Br. J. Pharmacol. 2008 153: 1062 1071.
11. Whiting PJ. GABA-A receptor subtypes in the brain: A paradigm for CNS drug discovery? Drug Discov. Today 2003 8: 445 450.
12. Korpi ER, Sinkkonen ST. GABA(A) receptor subtypes as targets for neuropsychiatric drug development. Pharmacol. Ther. 2006 109: 12 32.
13. Hosie AM, Wilkins ME, Smart TG. Neurosteroid binding sites on GABA(A) receptors. Pharmacol. Ther. 2007 116: 7 19.
14. Smith AJ, Alder L, Silk J et al. 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. 2001 59: 1108 1118.
15. McKernan RM, Wafford K, Quirk K et al. The pharmacology of the benzodiazepine site of the GABA-A receptor is dependent on the type of gamma-subunit present. J. Recept. Signal Transduct. Res. 1995 15: 173 183.
16. Wingrove PB, Thompson SA, Wafford KA, Whiting PJ. Key amino acids in the gamma subunit of the gamma-aminobutyric acid A receptor that determine ligand binding and modulation at the benzodiazepine site. Mol. Pharmacol. 1997 52: 874 881.
17. Buhr A, Baur R, Malherbe P, Sigel E. Point mutations of the alpha 1 beta 2 gamma 2 gamma-aminobutyric acid (A) receptor affecting modulation of the channel by ligands of the benzodiazepine binding site. Mol. Pharmacol. 1996 49: 1080 1084.
18. Stevenson A, Wingrove PB, Whiting PJ, Wafford KA. β-Carboline gamma-aminobutyric acid A receptor inverse agonists modulate gamma-aminobutyric acid via the loreclezole binding site as well as the benzodiazepine site. Mol. Pharmacol. 1995 48: 965 969.
19. Belelli D, Casula A, Ling A, Lambert JJ. The influence of subunit composition on the interaction of neurosteroids with GABA(A) receptors. Neuropharmacology 2002 43: 651 661.
20. Wohlfarth KM, Bianchi MT, Macdonald RL. Enhanced neurosteroid potentiation of ternary GABA(A) receptors containing the delta subunit. J. Neurosci. 2002 22: 1541 1549.
21. A receptors. Proc. Natl Acad. Sci. USA 2003 100: 14439 14444.
22. Wei W, Zhang N, Peng Z, Houser CR, Mody I. Perisynaptic localization of delta subunit-containing GABA(A) receptors and their activation by GABA spillover in the mouse dentate gyrus. J. Neurosci. 2003 23: 10650 10661.
23. Brown N, Kerby J, Bonnert TP, Whiting PJ, Wafford KA. Pharmacological characterization of a novel cell line expressing human alpha (4) beta (3) delta GABA(A) receptors. Br. J. Pharmacol. 2002 136: 965 974.
24. Adkins CE, Pillai GV, Kerby J et al. α4β3δ GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J. Biol. Chem. 2001 276: 38934 38939.
25. A receptors. Functional selectivity for extrasynaptic receptors is dependent on the absence of gamma 2. J. Pharmacol. Exp. Ther. 2006 316: 1351 1359.
26. Whittemore ER, Yang W, Drewe JA, Woodward RM. Pharmacology of the human gamma-aminobutyric acid A receptor alpha 4 subunit expressed in Xenopus laevis oocytes. Mol. Pharmacol. 1996 50: 1364 1375.
27. Wallner M, Hanchar HJ, Olsen RW. Ethanol enhances alpha 4 beta 3 delta and alpha 6 beta 3 delta gamma-aminobutyric acid type A receptors at low concentrations known to affect humans. Proc. Natl Acad. Sci. USA 2003 100: 15218 15223.
28. Borghese CM, Storustovu S, Ebert B et al. The delta subunit of gamma-aminobutyric acid type A receptors does not confer sensitivity to low concentrations of ethanol. J. Pharmacol. Exp. Ther. 2006 316: 1360 1368.
29. Wafford KA, Thompson SA, Thomas D, Sikela J, Wilcox AS, Whiting PJ. Functional characterization of human gamma-aminobutyric acid A receptors containing the alpha 4 subunit. Mol. Pharmacol. 1996 50: 670 678.
30. A receptor. Eur. J. Pharmacol. 2005 528: 1 6.
31. Rahman M, Zhu D, Lindblad C et al. GABA-site antagonism and pentobarbital actions do not depend on the alpha-subunit type in the recombinant rat GABA receptor. Acta Physiol. (Oxf) 2006 187: 479 488.
32. Sundstrom-Poromaa I, Smith DH, Gong QH et al. Hormonally regulated alpha (4) beta (2) delta GABA(A) receptors are a target for alcohol. Nat. Neurosci. 2002 5: 721 722.
33. Farrant M, Nusser Z. Variations on an inhibitory theme. Phasic and tonic activation of GABA(A) receptors. Nat. Rev. Neurosci. 2005 6: 215 229.
34. A receptors: Modulating gain and maintaining the tone. Trends Neurosci. 2004 27: 262 269.
35. Nusser Z, Mody I. Selective modulation of tonic and phasic inhibitions in dentate gyrus granule cells. J. Neurophysiol. 2002 87: 2624 2628.
36. Olsen RW, Sieghart W. International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid (A) receptors. Classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacol. Rev. 2008 60: 243 260.
37. A receptors: Subtypes provide diversity of function and pharmacology. Neuropharmacology 2009 56: 141 148.
38. Schwarzer C, Berresheim U, Pirker S et al. Distribution of the major gamma-aminobutyric acid (A) receptor subunits in the basal ganglia and associated limbic brain areas of the adult rat. J. Comp. Neurol. 2001 433: 526 549.
39. A receptors in hippocampal granule cells. Brain Res. 2004 1029: 207 216.
40. A beta-subunit homomeric receptors. Neuroreport 1996 7: 943 947.
41. Akk G, Bracamontes J, Steinbach JH. Activation of GABA(A) receptors containing the alpha4 subunit by GABA and pentobarbital. J. Physiol. 2004 556: 387 399.