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Volumn 3, Issue 4, 2012, Pages 293-301

Structurally diverse GABA antagonists interact differently with open and closed conformational states of the ρ1 receptor

Author keywords

Conformational change; Cys loop receptor; GABA binding site; GABAC receptors; Gating

Indexed keywords

4 AMINOBUTYRIC ACID C RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR BLOCKING AGENT; 4 AMINOCYCLOPENT 1 ENECARBOXAMIDE; ALANINE; AMIDE; CYSTEINE; SERINE; TYROSINE; UNCLASSIFIED DRUG;

EID: 84859891117     PISSN: None     EISSN: 19487193     Source Type: Journal    
DOI: 10.1021/cn200121r     Document Type: Article
Times cited : (12)

References (39)
  • 4
    • 78651504961 scopus 로고    scopus 로고
    • GABAC Receptors in the Lateral Amygdala: A Possible Novel Target for the Treatment of Fear and Anxiety Disorders?
    • Cunha, C., Monfils, M. H., and Ledoux, J. E. (2010) GABAC Receptors in the Lateral Amygdala: A Possible Novel Target for the Treatment of Fear and Anxiety Disorders? Front. Behav. Neurosci. 4, 6.
    • (2010) Front. Behav. Neurosci. , vol.4 , pp. 6
    • Cunha, C.1    Monfils, M.H.2    Ledoux, J.E.3
  • 6
    • 0034745280 scopus 로고    scopus 로고
    • Study of a GABAC receptor antagonist on sleep-waking behavior in rats
    • Arnaud, C., Gauthier, P., and Gottesmann, C. (2001) Study of a GABAC receptor antagonist on sleep-waking behavior in rats. Psychopharmacology (Berlin, Ger.) 154, 415-419.
    • (2001) Psychopharmacology (Berlin, Ger.) , vol.154 , pp. 415-419
    • Arnaud, C.1    Gauthier, P.2    Gottesmann, C.3
  • 7
    • 0036676724 scopus 로고    scopus 로고
    • Medicinal chemistry and molecular pharmacology of GABA(C) receptors
    • Johnston, G. A. (2002) Medicinal chemistry and molecular pharmacology of GABA(C) receptors. Curr. Top. Med. Chem. 2, 903-913.
    • (2002) Curr. Top. Med. Chem. , vol.2 , pp. 903-913
    • Johnston, G.A.1
  • 10
    • 0028796049 scopus 로고
    • Evolutionary history of the ligand-gated ion-channel superfamily of receptors
    • Ortells, M. O., and Lunt, G. G. (1995) Evolutionary history of the ligand-gated ion-channel superfamily of receptors. Trends Neurosci. 18, 121-127.
    • (1995) Trends Neurosci. , vol.18 , pp. 121-127
    • Ortells, M.O.1    Lunt, G.G.2
  • 11
    • 0032056332 scopus 로고    scopus 로고
    • Molecular composition of GABAC receptors
    • Enz, R., and Cutting, G. R. (1998) Molecular composition of GABAC receptors. Vision Res. 38, 1431-1441.
    • (1998) Vision Res. , vol.38 , pp. 1431-1441
    • Enz, R.1    Cutting, G.R.2
  • 12
    • 0033385856 scopus 로고    scopus 로고
    • Localization of GABA receptor rho2 and rho3 subunits in rat brain and functional expression of homooligomeric rho3 receptors and heterooligomeric rho2rho3 receptors
    • Ogurusu, T., Yanagi, K., Watanabe, M., Fukaya, M., and Shingai, R. (1999) Localization of GABA receptor rho 2 and rho 3 subunits in rat brain and functional expression of homooligomeric rho 3 receptors and heterooligomeric rho 2 rho 3 receptors. Recept. Channels 6, 463-475. (Pubitemid 30025674)
    • (1999) Receptors and Channels , vol.6 , Issue.6 , pp. 463-475
    • Ogurusu, T.1    Yanagi, K.2    Watanabe, M.3    Fukaya, M.4    Shingai, R.5
  • 13
    • 0034692175 scopus 로고    scopus 로고
    • GABA-activated ligand gated ion channels: Medicinal chemistry and molecular biology
    • DOI 10.1021/jm9904349
    • Chebib, M., and Johnston, G. A. (2000) GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology. J. Med. Chem. 43, 1427-1447. (Pubitemid 30238425)
    • (2000) Journal of Medicinal Chemistry , vol.43 , Issue.8 , pp. 1427-1447
    • Chebib, M.1    Johnston, G.A.R.2
  • 16
    • 41149168686 scopus 로고    scopus 로고
    • X-ray structure of a prokaryotic pentameric ligand-gated ion channel
    • DOI 10.1038/nature06717, PII NATURE06717
    • Hilf, R. J., and Dutzler, R. (2008) X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature 452, 375-379. (Pubitemid 351430790)
    • (2008) Nature , vol.452 , Issue.7185 , pp. 375-379
    • Hilf, R.J.C.1    Dutzler, R.2
  • 17
    • 58149242730 scopus 로고    scopus 로고
    • Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel
    • Hilf, R. J., and Dutzler, R. (2009) Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel. Nature 457, 115-118.
    • (2009) Nature , vol.457 , pp. 115-118
    • Hilf, R.J.1    Dutzler, R.2
  • 18
    • 3042515233 scopus 로고    scopus 로고
    • A) receptor
    • DOI 10.1042/BST0320540
    • Kash, T. L., Trudell, J. R., and Harrison, N. L. (2004) Structural elements involved in activation of the gamma-aminobutyric acid type A (GABAA) receptor. Biochem. Soc. Trans. 32, 540-546. (Pubitemid 38813557)
    • (2004) Biochemical Society Transactions , vol.32 , Issue.3 , pp. 540-546
    • Kash, T.L.1    Trudell, J.R.2    Harrison, N.L.3
  • 19
    • 0035141668 scopus 로고    scopus 로고
    • Structure and dynamics of the GABA binding pocket: A narrowing cleft that constricts during activation
    • Wagner, D. A., and Czajkowski, C. (2001) Structure and dynamics of the GABA binding pocket: A narrowing cleft that constricts during activation. J. Neurosci. 21, 67-74. (Pubitemid 32098727)
    • (2001) Journal of Neuroscience , vol.21 , Issue.1 , pp. 67-74
    • Wagner, D.A.1    Czajkowski, C.2
  • 20
    • 0037113888 scopus 로고    scopus 로고
    • Identification of a tyrosine in the agonist binding site of the homomeric rho1 gamma-aminobutyric acid (GABA) receptor that, when mutated, produces spontaneous opening
    • DOI 10.1074/jbc.M202007200
    • Torres, V. I., and Weiss, D. S. (2002) Identification of a tyrosine in the agonist binding site of the homomeric rho1 gammaaminobutyric acid (GABA) receptor that, when mutated, produces spontaneous opening. J. Biol. Chem. 277, 43741-43748. (Pubitemid 36157792)
    • (2002) Journal of Biological Chemistry , vol.277 , Issue.46 , pp. 43741-43748
    • Torres, V.I.1    Weiss, D.S.2
  • 24
    • 0032771146 scopus 로고    scopus 로고
    • 3H]tetracaine
    • Gallagher, M. J., and Cohen, J. B. (1999) Identification of amino acids of the torpedo nicotinic acetylcholine receptor contributing to the binding site for the noncompetitive antagonist [3H]tetracaine. Mol. Pharmacol. 56, 300-307. (Pubitemid 29347605)
    • (1999) Molecular Pharmacology , vol.56 , Issue.2 , pp. 300-307
    • Gallagher, M.J.1    Cohen, J.B.2
  • 26
    • 0037166316 scopus 로고    scopus 로고
    • 1K70 region mediate GABA and SR-95531 actions
    • 1K70 region mediate GABA and SR-95531 actions. J. Biol. Chem. 277, 18785-18792.
    • (2002) J. Biol. Chem. , vol.277 , pp. 18785-18792
    • Holden, J.H.1    Czajkowski, C.2
  • 27
    • 0034740846 scopus 로고    scopus 로고
    • An improved, versatile synthesis of the GABAC antagonists (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and (piperidin-4-yl)methylphosphinic acid (P4MPA)
    • Hanrahan, J. R., Mewett, K. N., Chebib, M., Burden, P. M., and Johnston, G. A. R. (2001) An improved, versatile synthesis of the GABAC antagonists (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and (piperidin-4-yl)methylphosphinic acid (P4MPA). J. Chem. Soc., Perkin Trans. 1, 2389-2392.
    • (2001) J. Chem. Soc., Perkin Trans. , vol.1 , pp. 2389-2392
    • Hanrahan, J.R.1    Mewett, K.N.2    Chebib, M.3    Burden, P.M.4    Johnston, G.A.R.5
  • 29
    • 46849096458 scopus 로고    scopus 로고
    • 1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships
    • DOI 10.1021/jm7015842
    • Kumar, R. J., Chebib, M., Hibbs, D. E., Kim, H. L., Johnston, G. A., Salam, N. K., and Hanrahan, J. R. (2008) Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships. J. Med. Chem. 51, 3825-3840. (Pubitemid 351956513)
    • (2008) Journal of Medicinal Chemistry , vol.51 , Issue.13 , pp. 3825-3840
    • Kumar, R.J.1    Chebib, M.2    Hibbs, D.E.3    Kim, H.-L.4    Johnston, G.A.R.5    Salam, N.K.6    Hanrahan, J.R.7
  • 30
    • 0022966452 scopus 로고
    • Synthesis of analogues of GABA. XV. Preparation and resolution of some potent cyclopentene and cyclopentane derivatives
    • Allan, R. D., and Fong, J. (1986) γ-Aminobutyric acid. Synthesis of analogs of GABA. XV. Preparation and resolution of some potent cyclopentene and cyclopentane derivatives. Aust. J. Chem. 39, 855-864. (Pubitemid 17169789)
    • (1986) Australian Journal of Chemistry , vol.39 , Issue.6 , pp. 855-864
    • Allan, R.D.1    Fong, J.2
  • 33
    • 77955950892 scopus 로고    scopus 로고
    • Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: Application to four-step synthesis of gabazine (SR-95531)
    • Gavande, N., Johnston, G. A., Hanrahan, J. R., and Chebib, M. (2010) Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: application to four-step synthesis of gabazine (SR-95531). Org. Biomol. Chem. 8, 4131-4136.
    • (2010) Org. Biomol. Chem. , vol.8 , pp. 4131-4136
    • Gavande, N.1    Johnston, G.A.2    Hanrahan, J.R.3    Chebib, M.4
  • 34
    • 69049101035 scopus 로고    scopus 로고
    • GABA analogues derived from 4-aminocyclopent-1-enecarboxylic acid
    • Locock, K. E., Johnston, G. A., and Allan, R. D. (2009) GABA analogues derived from 4-aminocyclopent-1-enecarboxylic acid. Neurochem. Res. 34, 1698-1703.
    • (2009) Neurochem. Res. , vol.34 , pp. 1698-1703
    • Locock, K.E.1    Johnston, G.A.2    Allan, R.D.3
  • 35
    • 0032544773 scopus 로고    scopus 로고
    • GABA(C) receptor antagonists differentiate between human rho1 and rho2 receptors expressed in Xenopus oocytes
    • DOI 10.1016/S0014-2999(98)00552-4, PII S0014299998005524
    • Chebib, M., Mewett, K. N., and Johnston, G. A. (1998) GABAC receptor antagonists differentiate between human rho1 and rho2 receptors expressed in Xenopus oocytes. Eur. J. Pharmacol. 357, 227-234. (Pubitemid 28439199)
    • (1998) European Journal of Pharmacology , vol.357 , Issue.2-3 , pp. 227-234
    • Chebib, M.1    Mewett, K.N.2    Johnston, G.A.R.3
  • 36
    • 0030998429 scopus 로고    scopus 로고
    • Unsaturated phosphinic analogues of gamma-aminobutyric acid as GABAC receptor antagonists
    • Chebib, M., Vandenberg, R. J., Froestl, W., and Johnston, G. A. (1997) Unsaturated phosphinic analogues of gamma-aminobutyric acid as GABAC receptor antagonists. Eur. J. Pharmacol. 329, 223-229.
    • (1997) Eur. J. Pharmacol. , vol.329 , pp. 223-229
    • Chebib, M.1    Vandenberg, R.J.2    Froestl, W.3    Johnston, G.A.4
  • 38
    • 0035798363 scopus 로고    scopus 로고
    • C receptors
    • DOI 10.1016/S0014-2999(01)01390-5, PII S0014299901013905
    • Chebib, M., Duke, R. K., Allan, R. D., and Johnston, G. A. (2001) The effects of cyclopentane and cyclopentene analogues of GABA at recombinant GABAC receptors. Eur. J. Pharmacol. 430, 185-192. (Pubitemid 33050037)
    • (2001) European Journal of Pharmacology , vol.430 , Issue.2-3 , pp. 185-192
    • Chebib, M.1    Duke, R.K.2    Allan, R.D.3    Johnston, G.A.R.4
  • 39
    • 0027466612 scopus 로고
    • Characterization of bicuculline/baclofen-insensitive (rho-like) gamma- aminobutyric acid receptors expressed in Xenopus oocytes. II. Pharmacology of gamma-aminobutyric acid(A) and gamma-aminobutyric acid(B) receptor agonists and antagonists
    • Woodward, R. M., Polenzani, L., and Miledi, R. (1993) Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes. II. Pharmacology of gamma-aminobutyric acidA and gamma-aminobutyric acidB receptor agonists and antagonists. Mol. Pharmacol. 43, 609-625. (Pubitemid 23112739)
    • (1993) Molecular Pharmacology , vol.43 , Issue.4 , pp. 609-625
    • Woodward, R.M.1    Polenzani, L.2    Miledi, R.3


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