Structural features of phenol derivatives determining potency for activation of chloride currents via α 1 homomeric and α 1β heteromeric glycine receptors

British Journal of Pharmacology

Volumn 145, Issue 7, 2005, Pages 916-925

  Haeseler, Gertrud ^a   Ahrens, Jörg ^a   Krampfl, Klaus ^a   Bufler, Johannes ^a   Dengler, Reinhard ^a   Hecker, Hartmut ^a   Aronson, Jeffrey K ^b   Leuwer, Martin ^c  

^a HANNOVER MEDICAL SCHOOL   (Germany)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c UNIVERSITY OF LIVERPOOL   (United Kingdom)

Author keywords

Glycine receptors; Inhibitory synaptic transmission; Phenol derivatives

Indexed keywords

2,6 XYLENOL; 3,5 XYLENOL; ALPHA 1 GLYCINE RECEPTOR; ALPHA1BETA GLYCINE RECEPTOR; CHLOROCRESOL; CHLOROXYLENOL; GLYCINE; GLYCINE RECEPTOR; META CRESOL; ORTHO CRESOL; PHENOL DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CHLORIDE CURRENT; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; DRUG POTENTIATION; DRUG STRUCTURE; EVOKED RESPONSE; HALOGENATION; HUMAN; HUMAN CELL; IN VITRO STUDY; METHYLATION; PRIORITY JOURNAL; RECEPTOR UPREGULATION; STRUCTURE ACTIVITY RELATION;

CELLS, CULTURED; CHLORIDE CHANNELS; CHLOROPHENOLS; CRESOLS; DOSE-RESPONSE RELATIONSHIP, DRUG; GLYCINE; HUMANS; KIDNEY; MEMBRANE POTENTIALS; PATCH-CLAMP TECHNIQUES; PHENOLS; RECEPTORS, GLYCINE; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION; XYLENES;

EID: 23744468902     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706254     Document Type: Article

References (27)

1. AHRENS, J., HAESELER, G., LEUWER, M., MOHAMMADI, B., KRAMPFL, K., DENGLER, R. & BUFLER, J. (2004). 2,6 Di-tert-butylphenol, a non-anesthetic propofol analogue, modulates α1β glycine receptor function in a manner distinct from propofol. Anesth. Analg., 99, 91-96.
2. A IPSCs. Anesthesiology, 90, 120-134.
3. BELELLI, D., CALLACHAN, H., HILL-YENNING, C., PETERS, J.A. & LAMBERT, J.J. (1996). Interaction of positive allosteric modulators with human and Drosophila recombinant GABA receptors expressed in Xenopus laevis oocytes. Br. J. Pharmacol., 118, 563-576.
4. 2 subunit affects allosteric sensitivity to GABA and anesthetics. Mol. Pharmacol., 57, 474-484.
5. DONG, X.P. & XU, T.L. (2002). The actions of propofol on γ-aminobutyric acid-A and glycine receptors in acutely dissociated spinal dorsal horn neurons of the rat. Anesth. Analg., 95, 907-914.
6. FRANKE, C., HATT, H. & DUDEL, J. (1987). Liquid filament switch for ultra-fast exchanges of solutions at excised patches of synaptic membranes of crayfish muscle. Neurosci. Lett., 77, 199-204.
7. HAESELER, G., BUFLER, J., MERKEN, S., DENGLER, R., ARONSON, J. & LEUWER, M. (2002). Block of voltage-operated sodium channels by 2,6-dimethylphenol, a structural analogue of lidocaine's aromatic tail. Br. J. Pharmacol., 137, 285-293.
8. HAESELER, G., LEUWER, M., KAVAN, J., WÜRZ, A., DENGLER, R. & PIEPENBROCK, S. (1999). Voltage-dependent block of normal and mutant muscle sodium channels by 4-chloro-m-cresol. Br. J. Pharmacol., 128, 1259-1267.
9. HAESELER, G., PIEPENBRINK, A., BUFLER, J., DENGLER, R., ARONSON, J.K., PIEPENBROCK, S. & LEUWER, M. (2001). Structural requirements for voltage-dependent block of muscle sodium channels by phenol derivatives. Br. J. Pharmacol., 132, 1916-1924.
10. HALES, T.G. & LAMBERT, J.J. (1991). The actions of propofol on inhibitory amino acid receptors of bovine adrenomedullary chromaffine cells and rodent central neurones. Br. J. Pharmacol., 104, 619-628.
11. HAMILL, O.P., MARTY, A., NEHER, E., SAKMANN, B. & SIGWORTH, F.J. (1981). Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflügers Arch., 391, 85-100.
12. A receptors: implications for an enhanced GABAergic transmission. Eur. J. Anaesthesiol., 18, 377-383.
13. JAMES, R. & GLEN, J.B. (1980). Synthesis, biological evaluation, and preliminary structure-activity considerations of a series of alkylphenols as intravenous anesthetic agents. J. Med. Chem., 23, 1350-1357.
14. JENTSCH, T.J., STEIN, V., WEINREICH, F. & ZDEBIK, A.A. (2002). Molecular structure and physiological function of chloride channels. Physiol. Rev., 82, 503-568.
15. A receptor but not with lipid solubility. J. Pharmacol. Exp. Ther., 297, 338-351.
16. LANGOSCH, D., THOMAS, L. & BETZ, H. (1988). Conserved quaternary structure of ligand gated ion channels: the postsynaptic glycine receptor is a pentamer. Proc. Natl. Acad. Sci. U.S.A., 85, 7394-7398.
17. LAUBE, B., MAKSAY, G., SCHEMM, R. & BETZ, H. (2002). Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses? Trends Pharmacol. Sci., 23, 519-527.
18. A and glycine receptors. Nature, 389, 385-389.
19. A-receptors. Eur. J. Pharmacol., 421, 85-91.
20. A and glycine receptors expressed in Xenopus laevis oocytes: a comparative study. Br. J. Pharmacol., 122, 1707-1719.
21. PRIBILLA, I., TAKAGI, T., LANGOSCH, D., BORMANN, J. & BETZ, H. (1992). The atypical M2 segment of the β subunit confers picrotoxin resistance to inhibitory glycine receptor channels. EMBO J., 11, 4305-4311.
22. C receptors. Mol. Pharmacol., 67, 470-479.
23. A- and glycine receptor-mediated synaptic currents in brain stem motoneurons. J. Neurophysiol., 90, 870-875.
24. SHAN, Q., NEVIN, S.T., HADDRILL, J.L. & LYNCH, J.W. (2003). Assymetric contribution of α and β subunits to the activation of αβ heteromeric glycine receptors. J. Neurochem., 86, 498-507.
25. SHERMAN, S.E., LUO, L. & DOSTROVSKY, J.O. (1997a). Altered receptive fields and sensory modalities of rat VPL thalamic neurons during spinal strychnine-induced allodynia. J. Neurophysiol., 78, 2296-2308.
26. SHERMAN, S.E., LUO, L. & DOSTROVSKY, J.O. (1997b). Spinal strychnine alters response properties of nociceptive-specific neurons in rat medial thalamus. J. Neurophysiol., 78, 628-637.
27. A receptors. J. Med. Chem., 41, 1846-1854.