메뉴 건너뛰기




Volumn 636, Issue 1-3, 2010, Pages 18-27

The point mutation γ2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes

Author keywords

2F77I mutation; Benzodiazepine site ligands; Efficacy; GABAA receptors; Potency; Recombinant receptors

Indexed keywords

3 METHYL 6 (3 TRIFLUOROMETHYLPHENYL) 1,2,4 TRIAZOLO[4,3 B]PYRIDAZINE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA2; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA3; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA4; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA5; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA6; 4 AMINOBUTYRIC ACID A RECEPTOR BETA3; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA2; 4 ETHYL 6,7 DIMETHOXY BETA CARBOLINE 3 CARBOXYLIC ACID METHYL ESTER; ABECARNIL; AMINO ACID; BENZODIAZEPINE DERIVATIVE; BRETAZENIL; CHLORIDE; DIAZEPAM; ETHYL 7 METHOXY 11,12,13,13A TETRAHYDRO 9 OXO 9H IMIDAZO[1,5 A]PYRROLO[2,1 C] [1,4]BENZODIAZEPINE 1 CARBOXYLIC ACID; FLUMAZENIL; L 655708; LIGAND; N METHYL BETA CARBOLINE 3 CARBOXAMIDE; UNCLASSIFIED DRUG; ZOLPIDEM; ZOPICLONE;

EID: 77952675421     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.03.015     Document Type: Article
Times cited : (45)

References (46)
  • 1
    • 0142122123 scopus 로고    scopus 로고
    • Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site
    • Atack J.R. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Curr. Drug Targets 2003, 2:213-232.
    • (2003) Curr. Drug Targets , vol.2 , pp. 213-232
    • Atack, J.R.1
  • 2
    • 33750608691 scopus 로고    scopus 로고
    • L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors
    • Atack J.R., Bayley P.J., Seabrook G.R., Wafford K.A., McKernan R.M., Dawson G.R. L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors. Neuropharmacology 2006, 51:1023-1029.
    • (2006) Neuropharmacology , vol.51 , pp. 1023-1029
    • Atack, J.R.1    Bayley, P.J.2    Seabrook, G.R.3    Wafford, K.A.4    McKernan, R.M.5    Dawson, G.R.6
  • 4
    • 52949100192 scopus 로고    scopus 로고
    • Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits
    • Baburin I., Khom S., Timin E., Hohaus A., Sieghart W., Hering S. Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits. Br. J. Pharmacol. 2008, 155:424-433.
    • (2008) Br. J. Pharmacol. , vol.155 , pp. 424-433
    • Baburin, I.1    Khom, S.2    Timin, E.3    Hohaus, A.4    Sieghart, W.5    Hering, S.6
  • 5
    • 0348010294 scopus 로고    scopus 로고
    • Individual properties of the two functional agonist sites in GABA(A) receptors
    • Baumann S.W., Baur R., Sigel E. Individual properties of the two functional agonist sites in GABA(A) receptors. J. Neurosci. 2003, 23:11158-11166.
    • (2003) J. Neurosci. , vol.23 , pp. 11158-11166
    • Baumann, S.W.1    Baur, R.2    Sigel, E.3
  • 6
    • 15744392087 scopus 로고    scopus 로고
    • Benzodiazepines affect channel opening of GABA A receptors induced by either agonist binding site
    • Baur R., Sigel E. Benzodiazepines affect channel opening of GABA A receptors induced by either agonist binding site. Mol. Pharmacol. 2005, 67:1005-1008.
    • (2005) Mol. Pharmacol. , vol.67 , pp. 1005-1008
    • Baur, R.1    Sigel, E.2
  • 7
    • 50849097106 scopus 로고    scopus 로고
    • Replacement of histidine in position 105 in the alpha(5) subunit by cysteine stimulates zolpidem sensitivity of alpha(5)beta(2)gamma(2) GABA(A) receptors
    • Baur R., Sigel E. Replacement of histidine in position 105 in the alpha(5) subunit by cysteine stimulates zolpidem sensitivity of alpha(5)beta(2)gamma(2) GABA(A) receptors. J. Neurochem. 2007, 103:2556-2564.
    • (2007) J. Neurochem. , vol.103 , pp. 2556-2564
    • Baur, R.1    Sigel, E.2
  • 8
    • 0030959309 scopus 로고    scopus 로고
    • A receptors drastically alter the affinity for ligands of the benzodiazepine binding site
    • A receptors drastically alter the affinity for ligands of the benzodiazepine binding site. J. Biol. Chem. 1997, 272:11799-11804.
    • (1997) J. Biol. Chem. , vol.272 , pp. 11799-11804
    • Buhr, A.1    Baur, R.2    Sigel, E.3
  • 12
    • 0030459356 scopus 로고    scopus 로고
    • Extensive heterogeneity of recombinant gamma-aminobutyric acidA receptors expressed in alpha 4 beta 3 gamma 2-transfected human embryonic kidney 293 cells
    • Ebert V., Scholze P., Sieghart W. Extensive heterogeneity of recombinant gamma-aminobutyric acidA receptors expressed in alpha 4 beta 3 gamma 2-transfected human embryonic kidney 293 cells. Neuropharmacology 1996, 35:1323-1330.
    • (1996) Neuropharmacology , vol.35 , pp. 1323-1330
    • Ebert, V.1    Scholze, P.2    Sieghart, W.3
  • 14
    • 14844323722 scopus 로고    scopus 로고
    • Variations on an inhibitory theme: phasic and tonic activation of GABA(A) receptors
    • Farrant M., Nusser Z. Variations on an inhibitory theme: phasic and tonic activation of GABA(A) receptors. Nat. Rev. Neurosci. 2005, 6:215-229.
    • (2005) Nat. Rev. Neurosci. , vol.6 , pp. 215-229
    • Farrant, M.1    Nusser, Z.2
  • 15
    • 0036070596 scopus 로고    scopus 로고
    • Molecular actions of (S)-desmethylzopiclone (SEP-174559), an anxiolytic metabolite of zopiclone
    • Fleck M.W. Molecular actions of (S)-desmethylzopiclone (SEP-174559), an anxiolytic metabolite of zopiclone. J. Pharmacol. Exp. Ther. 2002, 302:612-618.
    • (2002) J. Pharmacol. Exp. Ther. , vol.302 , pp. 612-618
    • Fleck, M.W.1
  • 16
    • 0030024882 scopus 로고    scopus 로고
    • Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors
    • Hadingham K.L., Garrett E.M., Wafford K.A., Bain C., Heavens R.P., Sirinathsinghji D.J., Whiting P.J. Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol. Pharmacol. 1996, 49:253-259.
    • (1996) Mol. Pharmacol. , vol.49 , pp. 253-259
    • Hadingham, K.L.1    Garrett, E.M.2    Wafford, K.A.3    Bain, C.4    Heavens, R.P.5    Sirinathsinghji, D.J.6    Whiting, P.J.7
  • 17
    • 34250018794 scopus 로고    scopus 로고
    • Rat alpha6beta2delta GABAA receptors exhibit two distinct and separable agonist affinities
    • Hadley S.H., Amin J. Rat alpha6beta2delta GABAA receptors exhibit two distinct and separable agonist affinities. J. Physiol. 2007, 581:1001-1018.
    • (2007) J. Physiol. , vol.581 , pp. 1001-1018
    • Hadley, S.H.1    Amin, J.2
  • 20
    • 0029827577 scopus 로고    scopus 로고
    • Pharmacological modulation of the diazepam-insensitive recombinant gamma-aminobutyric acidA receptors alpha 4 beta 2 gamma 2 and alpha 6 beta 2 gamma 2
    • Knoflach F., Benke D., Wang Y., Scheurer L., Luddens H., Hamilton B.J., Carter D.B., Mohler H., Benson J.A. Pharmacological modulation of the diazepam-insensitive recombinant gamma-aminobutyric acidA receptors alpha 4 beta 2 gamma 2 and alpha 6 beta 2 gamma 2. Mol. Pharmacol. 1996, 50:1253-1261.
    • (1996) Mol. Pharmacol. , vol.50 , pp. 1253-1261
    • Knoflach, F.1    Benke, D.2    Wang, Y.3    Scheurer, L.4    Luddens, H.5    Hamilton, B.J.6    Carter, D.B.7    Mohler, H.8    Benson, J.A.9
  • 21
    • 14744299830 scopus 로고    scopus 로고
    • Agonistic effects of the beta-carboline DMCM revealed in GABA(A) receptor gamma 2 subunit F77I point-mutated mice
    • Leppa E., Vekovischeva O.Y., Linden A.M., Wulff P., Oberto A., Wisden W., Korpi E.R. Agonistic effects of the beta-carboline DMCM revealed in GABA(A) receptor gamma 2 subunit F77I point-mutated mice. Neuropharmacology 2005, 48:469-478.
    • (2005) Neuropharmacology , vol.48 , pp. 469-478
    • Leppa, E.1    Vekovischeva, O.Y.2    Linden, A.M.3    Wulff, P.4    Oberto, A.5    Wisden, W.6    Korpi, E.R.7
  • 22
    • 0347627160 scopus 로고    scopus 로고
    • Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1, 5a]-[1, 4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist
    • Li X., Cao H., Zhang C., Furtmueller R., Fuchs K., Huck S., Sieghart W., Deschamps J., Cook J.M. Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1, 5a]-[1, 4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist. J. Med. Chem. 2003, 46:5567-5570.
    • (2003) J. Med. Chem. , vol.46 , pp. 5567-5570
    • Li, X.1    Cao, H.2    Zhang, C.3    Furtmueller, R.4    Fuchs, K.5    Huck, S.6    Sieghart, W.7    Deschamps, J.8    Cook, J.M.9
  • 23
    • 0021006468 scopus 로고
    • Pharmacological and behavioural studies of benzodiazepine antagonists and contragonists
    • Nutt D. Pharmacological and behavioural studies of benzodiazepine antagonists and contragonists. Adv. Biochem. Psychopharmacol. 1983, 38:153-173.
    • (1983) Adv. Biochem. Psychopharmacol. , vol.38 , pp. 153-173
    • Nutt, D.1
  • 24
    • 4644319039 scopus 로고    scopus 로고
    • Affinity of various benzodiazepine site ligands in mice with a point mutation in the GABA(A) receptor gamma2 subunit
    • Ogris W., Poltl A., Hauer B., Ernst M., Oberto A., Wulff P., Hoger H., Wisden W., Sieghart W. Affinity of various benzodiazepine site ligands in mice with a point mutation in the GABA(A) receptor gamma2 subunit. Biochem. Pharmacol. 2004, 68:1621-1629.
    • (2004) Biochem. Pharmacol. , vol.68 , pp. 1621-1629
    • Ogris, W.1    Poltl, A.2    Hauer, B.3    Ernst, M.4    Oberto, A.5    Wulff, P.6    Hoger, H.7    Wisden, W.8    Sieghart, W.9
  • 25
    • 54049137689 scopus 로고    scopus 로고
    • International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid(A) receptors: classification on the basis of subunit composition, pharmacology, and function. Update
    • Olsen R.W., 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.
    • (2008) Pharmacol. Rev. , vol.60 , pp. 243-260
    • Olsen, R.W.1    Sieghart, W.2
  • 26
    • 33645122408 scopus 로고    scopus 로고
    • Indiplon is a high-affinity positive allosteric modulator with selectivity for alpha1 subunit-containing GABAA receptors
    • Petroski R.E., Pomeroy J.E., Das R., Bowman H., Yang W., Chen A.P., Foster A.C. Indiplon is a high-affinity positive allosteric modulator with selectivity for alpha1 subunit-containing GABAA receptors. J. Pharmacol. Exp. Ther. 2006, 317:369-377.
    • (2006) J. Pharmacol. Exp. Ther. , vol.317 , pp. 369-377
    • Petroski, R.E.1    Pomeroy, J.E.2    Das, R.3    Bowman, H.4    Yang, W.5    Chen, A.P.6    Foster, A.C.7
  • 28
    • 0026550014 scopus 로고
    • Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at gamma-aminobutyric acid type A receptor
    • Puia G., Ducic I., Vicini S., Costa E. Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at gamma-aminobutyric acid type A receptor. Proc. Natl. Acad. Sci. U. S. A. 1992, 89:3620-3624.
    • (1992) Proc. Natl. Acad. Sci. U. S. A. , vol.89 , pp. 3620-3624
    • Puia, G.1    Ducic, I.2    Vicini, S.3    Costa, E.4
  • 33
    • 0028981088 scopus 로고
    • A receptor subtypes
    • A receptor subtypes. Pharmacol. Rev. 1995, 47:181-234.
    • (1995) Pharmacol. Rev. , vol.47 , pp. 181-234
    • Sieghart, W.1
  • 34
    • 0022415954 scopus 로고
    • Comparison of benzodiazepine receptor binding in membranes from human or rat brain
    • Sieghart W., Eichinger A., Riederer P., Jellinger K. Comparison of benzodiazepine receptor binding in membranes from human or rat brain. Neuropharmacology 1985, 24:751-759.
    • (1985) Neuropharmacology , vol.24 , pp. 751-759
    • Sieghart, W.1    Eichinger, A.2    Riederer, P.3    Jellinger, K.4
  • 36
    • 0025259031 scopus 로고
    • The effect of subunit composition of rat brain GABAA receptors on channel function
    • Sigel E., Baur R., Trube G., Mohler H., Malherbe P. The effect of subunit composition of rat brain GABAA receptors on channel function. Neuron 1990, 5:703-711.
    • (1990) Neuron , vol.5 , pp. 703-711
    • Sigel, E.1    Baur, R.2    Trube, G.3    Mohler, H.4    Malherbe, P.5
  • 37
    • 0021048041 scopus 로고
    • Benzodiazepine Ro 15-1788: electrophysiological evidence for partial agonist activity
    • Skerritt J.H., Macdonald R.L. Benzodiazepine Ro 15-1788: electrophysiological evidence for partial agonist activity. Neurosci. Lett. 1983, 43:321-326.
    • (1983) Neurosci. Lett. , vol.43 , pp. 321-326
    • Skerritt, J.H.1    Macdonald, R.L.2
  • 38
    • 0035039871 scopus 로고    scopus 로고
    • 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
    • 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. 2001, 59:1108-1118.
    • (2001) Mol. Pharmacol. , vol.59 , pp. 1108-1118
    • Smith, A.J.1    Alder, L.2    Silk, J.3    Adkins, C.4    Fletcher, A.E.5    Scales, T.6    Kerby, J.7    Marshall, G.8    Wafford, K.A.9    McKernan, R.M.10    Atack, J.R.11
  • 39
    • 0024270208 scopus 로고
    • Kindling with the beta-carboline FG7142 suggests separation between changes in seizure threshold and anxiety-related behaviour
    • Taylor S.C., Johnston A.L., Wilks L.J., Nicholass J.M., File S.E., Little H.J. Kindling with the beta-carboline FG7142 suggests separation between changes in seizure threshold and anxiety-related behaviour. Neuropsychobiology 1988, 19:195-201.
    • (1988) Neuropsychobiology , vol.19 , pp. 195-201
    • Taylor, S.C.1    Johnston, A.L.2    Wilks, L.J.3    Nicholass, J.M.4    File, S.E.5    Little, H.J.6
  • 40
    • 0020536527 scopus 로고
    • Is Ro15-1788 a partial agonist at benzodiazepine receptors?
    • Vellucci S.V., Webster R.A. Is Ro15-1788 a partial agonist at benzodiazepine receptors?. Eur. J. Pharmacol. 1983, 90:263-268.
    • (1983) Eur. J. Pharmacol. , vol.90 , pp. 263-268
    • Vellucci, S.V.1    Webster, R.A.2
  • 41
    • 0027328861 scopus 로고
    • Functional comparison of the role of gamma subunits in recombinant human gamma-aminobutyric acidA/benzodiazepine receptors
    • Wafford K.A., Bain C.J., Whiting P.J., Kemp J.A. Functional comparison of the role of gamma subunits in recombinant human gamma-aminobutyric acidA/benzodiazepine receptors. Mol. Pharmacol. 1993, 44:437-442.
    • (1993) Mol. Pharmacol. , vol.44 , pp. 437-442
    • Wafford, K.A.1    Bain, C.J.2    Whiting, P.J.3    Kemp, J.A.4
  • 42
    • 0027530534 scopus 로고
    • Differences in affinity and efficacy of benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes
    • Wafford K.A., Whiting P.J., Kemp J.A. Differences in affinity and efficacy of benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes. Mol. Pharmacol. 1993, 43:240-244.
    • (1993) Mol. Pharmacol. , vol.43 , pp. 240-244
    • Wafford, K.A.1    Whiting, P.J.2    Kemp, J.A.3
  • 43
    • 0033623608 scopus 로고    scopus 로고
    • Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms
    • Walters R.J., Hadley S.H., Morris K.D., Amin J. Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms. Nat. Neurosci. 2000, 3:1274-1281.
    • (2000) Nat. Neurosci. , vol.3 , pp. 1274-1281
    • Walters, R.J.1    Hadley, S.H.2    Morris, K.D.3    Amin, J.4
  • 44
    • 0029807606 scopus 로고    scopus 로고
    • Pharmacology of the human gamma-aminobutyric acidA receptor alpha 4 subunit expressed in Xenopus laevis oocytes
    • Whittemore E.R., Yang W., Drewe J.A., Woodward R.M. Pharmacology of the human gamma-aminobutyric acidA receptor alpha 4 subunit expressed in Xenopus laevis oocytes. Mol. Pharmacol. 1996, 50:1364-1375.
    • (1996) Mol. Pharmacol. , vol.50 , pp. 1364-1375
    • Whittemore, E.R.1    Yang, W.2    Drewe, J.A.3    Woodward, R.M.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.