The anaesthetic steroid alphaxalone positively modulates α1-glycine receptor function

Pharmacology

Volumn 82, Issue 3, 2008, Pages 228-232

  Ahrens, Jörg ^a   Leuwer, Martin ^b   Demir, Reyhan ^a   Krampfl, Klaus ^a   Foadi, Nilufar ^a   Haeseler, Gertrud ^a  

^a HANNOVER MEDICAL SCHOOL   (Germany)

^b UNIVERSITY OF LIVERPOOL   (United Kingdom)

Author keywords

Glycine receptor; Inhibitory synaptic transmission; Neuroactive steroids

Indexed keywords

ALFAXALONE; ALPHA1 GLYCINE RECEPTOR; ANESTHETIC AGENT; GLYCINE; GLYCINE RECEPTOR; NEUROSTEROID; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

ARTICLE; CELL STRAIN HEK293; DRUG STRUCTURE; HUMAN; HUMAN CELL; NEUROMODULATION; NOCICEPTIVE STIMULATION; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; SPINAL CORD DORSAL HORN; SYNAPTIC TRANSMISSION;

ANESTHETICS; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; PATCH-CLAMP TECHNIQUES; PREGNANEDIONES; PROTEIN SUBUNITS; RECEPTORS, GLYCINE; SIGNAL TRANSDUCTION; SYNAPTIC TRANSMISSION;

EID: 52049099884     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000156489     Document Type: Article

References (23)

1. Belelli D, Lambert JJ: Neurosteroids: endogenous regulators of the GABA(A) receptor. Nat Rev Neurosci 2005;6:565-575.
2. Jentsch TJ, Stein V, Weinreich F, et al: Molecular structure and physiological function of chloride channels. Physiol Rev 2002;82:503-568.
3. Laube B, Maksay G, Schemm R, et al: Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses? Trends Pharmacol Sci 2002;23:519-527.
4. Betz H, Laube B: Glycine receptors: recent insights into their structural organization and functional diversity. J Neurochem 2006;97:1600-1610.
5. Langosch D, Thomas L, Betz H: Conserved quaternary structure of ligand-gated ion channels: the postsynaptic glycine receptor is a pentamer. Proc Natl Acad Sci USA 1988;85:7394-7398.
6. Lynch JW: Molecular structure and function of the glycine receptor chloride channel. Physiol Rev 2004;84:1051-1095.
7. Harvey RJ, Depner UB, Wassle H, et al: GlyR alpha3: an essential target for spinal PGE2-mediated inflammatory pain sensitization. Science 2004;304:884-887.
8. Belelli D, Herd MB, Mitchell EA, et al: Neuroactive steroids and inhibitory neurotransmission: mechanisms of action and physiological relevance. Neuroscience 2006;138:821-829.
9. Hamill OP, Marty A, Neher E, et al: Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 1981;391:85-100.
10. Franke C, Hatt H, Dudel J: Liquid filament switch for ultra-fast exchanges of solutions at excised patches of synaptic membrane of crayfish muscle. Neurosci Lett 1987;77:199-204.
11. Ahrens J, Haeseler G, Leuwer M, et al: 2,6 ditertbutylphenol, a nonanesthetic propofol analog, modulates alpha1beta glycine receptor function in a manner distinct from propofol. Anesth Analg 2004;99:91-96.
12. Sebe JY, Eggers ED, Berger AJ: Differential effects of ethanol on GABA(A) and glycine receptor-mediated synaptic currents in brain stem motoneurons. J Neurophysiol 2003;90:870-875.
13. Zeilhofer HU: The glycinergic control of spinal pain processing. Cell Mol Life Sci 2005;62:2027-2035.
14. Lynch JW, Callister RJ: Glycine receptors: a new therapeutic target in pain pathways. Curr Opin Investig Drugs 2006;7:48-53.
15. Weir CJ, Ling AT, Belelli D, et al: The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors. Br J Anaesth 2004;92:704-711.
16. Franks NP, Lieb WR: Molecular and cellular mechanisms of general anaesthesia. Nature 1994;367:607-614.
17. O'Shea SM, Becker L, Weiher H, et al: Propofol restores the function of 'hyperekplexic' mutant glycine receptors in Xenopus oocytes and mice. J Neurosci 2004;24:2322-2327.
18. Haeseler G, Ahrens J, Krampfl K, et al: Structural features of phenol derivatives determining potency for activation of chloride currents via alpha(1) homomeric and alpha(1)beta heteromeric glycine receptors. Br J Pharmacol 2005;145:916-925.
19. Pistis M, Belelli D, Peters JA, et al: The interaction of general anaesthetics with recombinant GABAA and glycine receptors expressed in Xenopus laevis oocytes: a comparative study. Br J Pharmacol 1997;122:1707-1719.
20. Belelli D, Pistis M, Peters JA, et al: General anaesthetic action at transmitter-gated inhibitory amino acid receptors. Trends Pharmacol Sci 1999;20:496-502.
21. Fodor L, Boros A, Dezso P, et al: Expression of heteromeric glycine receptor-channels in rat spinal cultures and inhibition by neuroactive steroids. Neurochem Int 2006;49:577-583.
22. Chen Y, Dai TJ, Zeng YM: Strychnine-sensitive glycine receptors mediate the analgesic but not hypnotic effects of emulsified volatile anesthetics. Pharmacology 2007;80:151-157.
23. Ahrens J, Leuwer M, Haeseler G: Strychnine-sensitive glycine receptors mediate the analgesic but not the hypnotic effects of emulsified volatile anaesthetics. Pharmacology 2008;81:195.