Valerenic acid potentiates and inhibits GABAA receptors: Molecular mechanism and subunit specificity

Neuropharmacology

Volumn 53, Issue 1, 2007, Pages 178-187

  Khom, S ^a   Baburin, I ^a   Timin, E ^a   Hohaus, A ^a   Trauner, G ^a   Kopp, B ^a   Hering, S ^a  

^a UNIVERSITY OF VIENNA   (Austria)

Author keywords

2 Microelectrode voltage clamp technique; GABAA receptors; Subunit specific modulation; Valerenic acid; Xenopus oocyte

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; ACETOXYVALERENIC ACID; DIAZEPAM; FLUMAZENIL; HYDROXYVALERENIC ACID; LORECLEZOLE; UNCLASSIFIED DRUG; VALERENIC ACID; VALERIAN;

ANIMAL CELL; ARTICLE; CHLORIDE CURRENT; CONTROLLED STUDY; DRUG MECHANISM; NEUROPHARMACOLOGY; NONHUMAN; OOCYTE; POINT MUTATION; PRIORITY JOURNAL; VOLTAGE CLAMP; XENOPUS LAEVIS;

ANIMALS; CHLORIDE CHANNELS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOSE-RESPONSE RELATIONSHIP, RADIATION; DRUG INTERACTIONS; ELECTRIC STIMULATION; FLUMAZENIL; GABA AGONISTS; GABA ANTAGONISTS; GABA MODULATORS; GAMMA-AMINOBUTYRIC ACID; INDENES; MEMBRANE POTENTIALS; MUTATION; OOCYTES; PATCH-CLAMP TECHNIQUES; PROTEIN SUBUNITS; RECEPTORS, GABA-A; SESQUITERPENES; XENOPUS LAEVIS;

EID: 34547229341     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2007.04.018     Document Type: Article

References (40)

1. Akk G., and Steinbach J.H. Activation and block of recombinant GABA(A) receptors by pentobarbitone: a single-channel study. Br. J. Pharmacol. 130 (2000) 249-258
2. Anderson G.D., Elmer G.W., Kantor E.D., Templeton I.E., and Vitiello M.V. Pharmacokinetics of valerenic acid after administration of valerian in healthy subjects. Phytother. Res. 19 (2005) 801-803
3. Baburin I., Beyl S., and Hering S. Automated fast perfusion of Xenopus oocytes for drug screening. Pflugers Arch. 453 (2006) 117-123
4. Barnard E.A., Skolnick P., Olsen R.W., Mohler H., Sieghart W., Biggio G., Braestrup C., Bateson A.N., and Langer S.Z. International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function. Pharmacol. Rev. 50 (1998) 291-313
5. Baur R., Simmen U., Senn M., Sequin U., and Sigel E. Novel plant substances acting as beta subunit isoform-selective positive allosteric modulators of GABAA receptors. Mol. Pharmacol. 68 (2005) 787-792
6. Boileau A.J., Baur R., Sharkey L.M., Sigel E., and Czajkowski C. The relative amount of cRNA coding for gamma2 subunits affects stimulation by benzodiazepines in GABA(A) receptors expressed in Xenopus oocytes. Neuropharmacology 43 (2002) 695-700
7. Dalziel J.E., Cox G.B., Gage P.W., and Birnir B. Mutant human alpha(1)beta(1) (T262Q) GABA(A) receptors are directly activated but not modulated by pentobarbital. Eur. J. Pharmacol. 385 (1999) 283-286
8. De Smet P.A. Herbal remedies. N. Engl. J. Med. 347 (2002) 2046-2056
9. Ernst M., Brauchart D., Boresch S., and Sieghart W. Comparative modeling of GABA(A) receptors: limits, insights, future developments. Neuroscience 119 (2003) 933-943
10. Ernst M., Bruckner S., Boresch S., and Sieghart W. Comparative models of GABAA receptor extracellular and transmembrane domains: important insights in pharmacology and function. Mol. Pharmacol. 68 (2005) 1291-1300
11. Feng H.J., Bianchi M.T., and Macdonald R.L. Pentobarbital differentially modulates alpha1beta3delta and alpha1beta3gamma2L GABAA receptor currents. Mol. Pharmacol. 66 (2004) 988-1003
12. Galzi J.L., and Changeux J.P. Neuronal nicotinic receptors: molecular organization and regulations. Neuropharmacology 34 (1995) 563-582
13. Garcia D.A., Bujons J., Vale C., and Sunol C. Allosteric positive interaction of thymol with the GABAA receptor in primary cultures of mouse cortical neurons. Neuropharmacology 50 (2006) 25-35
14. Granger R.E., Campbell E.L., and Johnston G.A. (+)- And (-)-borneol: efficacious positive modulators of GABA action at human recombinant alpha1beta2gamma2L GABA(A) receptors. Biochem. Pharmacol. 69 (2005) 1101-1111
15. Haas K.F., and Macdonald R.L. GABAA receptor subunit gamma2 and delta subtypes confer unique kinetic properties on recombinant GABAA receptor currents in mouse fibroblasts. J. Physiol. 514 Pt 1 (1999) 27-45
16. Hevers W., and Lüddens H. The diversity of GABAA receptors. Pharmacological and electrophysiological properties of GABAA channel subtypes. Mol. Neurobiol. 18 (1998) 35-86
17. Hong Z., and Wang D.S. Potentiation, activation and blockade of GABAA receptors by etomidate in the rat sacral dorsal commissural neurons. Neuroscience 132 (2005) 1045-1053
18. Horton R.M., Hunt H.D., Ho S.N., Pullen J.K., and Pease L.R. Engineering hybrid genes without the use of restriction enzymes: gene splicing by overlap extension. Gene 77 (1989) 61-68
19. Huen M.S., Hui K.M., Leung J.W., Sigel E., Baur R., Wong J.T., and Xue H. Naturally occurring 2′-hydroxyl-substituted flavonoids as high-affinity benzodiazepine site ligands. Biochem. Pharmacol. 66 (2003) 2397-2407
20. Hui K.M., Huen M.S., Wang H.Y., Zheng H., Sigel E., Baur R., Ren H., Li Z.W., Wong J.T., and Xue H. Anxiolytic effect of wogonin, a benzodiazepine receptor ligand isolated from Scutellaria baicalensis Georgi. Biochem. Pharmacol. 64 (2002) 1415-1424
21. Jones M.V., and Westbrook G.L. Desensitized states prolong GABAA channel responses to brief agonist pulses. Neuron 15 (1995) 181-191
22. Khom S., Baburin I., Timin E.N., Hohaus A., Sieghart W., and Hering S. Pharmacological properties of GABAA receptors containing gamma1 subunits. Mol. Pharmacol. 69 (2006) 640-649
23. Krampfl K., Wolfes H., Dengler R., and Bufler J. Kinetic analysis of the agonistic and blocking properties of pentobarbital on recombinant rat alpha(1)beta(2)gamma(2S) GABA(A) receptor channels. Eur. J. Pharmacol. 435 (2002) 1-8
24. Krishek B.J., Moss S.J., and Smart T.G. Homomeric beta 1 gamma-aminobutyric acid A receptor-ion channels: evaluation of pharmacological and physiological properties. Mol. Pharmacol. 49 (1996) 494-504
25. Lam D.W., and Reynolds J.N. Modulatory and direct effects of propofol on recombinant GABAA receptors expressed in Xenopus oocytes: influence of alpha- and gamma2-subunits. Brain Res. 784 (1998) 179-187
26. Marder M., Viola H., Wasowski C., Fernandez S., Medina J.H., and Paladini A.C. 6-Methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS. Pharmacol. Biochem. Behav. 75 (2003) 537-545
27. Methfessel C., Witzemann V., Takahashi T., Mishina M., Numa S., and Sakmann B. Patch clamp measurements on Xenopus laevis oocytes: currents through endogenous channels and implanted acetylcholine receptor and sodium channels. Pflugers Arch. 407 (1986) 577-588
28. Rho J.M., Donevan S.D., and Rogawski M.A. Direct activation of GABAA receptors by barbiturates in cultured rat hippocampal neurons. J. Physiol. 497 Pt 2 (1996) 509-522
29. Sampson W. Studying herbal remedies. N. Engl. J. Med. 353 (2005) 337-339
30. Sanna E., Murgia A., Casula A., Usala M., Maciocco E., Tuligi G., and Biggio G. Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology 35 (1996) 1753-1760
31. Schulz D.W., and Macdonald R.L. Barbiturate enhancement of GABA-mediated inhibition and activation of chloride ion conductance: correlation with anticonvulsant and anesthetic actions. Brain Res. 209 (1981) 177-188
32. Sieghart W. Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes. Pharmacol. Rev. 47 (1995) 181-234
33. Sigel E. Mapping of the benzodiazepine recognition site on GABA(A) receptors. Curr. Top. Med. Chem. 2 (2002) 833-839
34. Sigel E., and Buhr A. The benzodiazepine binding site of GABAA receptors. Trends Pharmacol. Sci. 18 (1997) 425-429
35. Simon J., Wakimoto H., Fujita N., Lalande M., and Barnard E.A. Analysis of the set of GABA(A) receptor genes in the human genome. J. Biol. Chem. 279 (2004) 41422-41435
36. Thompson S.A., Whiting P.J., and Wafford K.A. Barbiturate interactions at the human GABAA receptor: dependence on receptor subunit combination. Br. J. Pharmacol. 117 (1996) 521-527
37. Ueno S., Bracamontes J., Zorumski C., Weiss D.S., and Steinbach J.H. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J. Neurosci. 17 (1997) 625-634
38. Wafford K.A., Bain C.J., Quirk K., McKernan R.M., Wingrove P.B., Whiting P.J., and Kemp J.A. A novel allosteric modulatory site on the GABAA receptor beta subunit. Neuron 12 (1994) 775-782
39. Wingrove P.B., Wafford K.A., Bain C., and Whiting P.J. The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit. Proc. Natl. Acad. Sci. U.S.A. 91 (1994) 4569-4573
40. Yuan C.S., Mehendale S., Xiao Y., Aung H.H., Xie J.T., and Ang-Lee M.K. The gamma-aminobutyric acidergic effects of valerian and valerenic acid on rat brainstem neuronal activity. Anesth. Analg. 98 (2004) 353-358