The nonpsychotropic cannabinoid cannabidiol modulates and directly activates alpha-1 and alpha-1-beta glycine receptor function

Pharmacology

Volumn 83, Issue 4, 2009, Pages 217-222

  Ahrens, Jörg ^a,d   Demir, Reyhan ^a   Leuwer, Martin ^c   De La Roche, Jeanne ^a   Krampfl, Klaus ^b   Foadi, Nilufar ^a   Karst, Matthias ^a   Haeseler, Gertrud ^a  

^a OE 8050   (Germany)

^b HANNOVER MEDICAL SCHOOL   (Germany)

^c UNIVERSITY OF LIVERPOOL   (United Kingdom)

^d Clinic for Anaesthesia and Critical Care Medicine   (Germany)

Author keywords

Cannabidiol; Cannabinoids; Glycine receptor

Indexed keywords

ALPHA 1 BETA GLYCINE RECEPTOR; ALPHA 1 GLYCINE RECEPTOR; CANNABIDIOL; GLYCINE; GLYCINE RECEPTOR; STRYCHNINE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CONCENTRATION RESPONSE; DRUG MECHANISM; DRUG TARGETING; HUMAN; HUMAN CELL; IN VITRO STUDY; INHIBITORY POSTSYNAPTIC POTENTIAL; NEUROPROTECTION; PATCH CLAMP; PRIORITY JOURNAL; RECEPTOR UPREGULATION; SPINAL CORD DORSAL HORN; SYNAPTIC TRANSMISSION;

CANNABIDIOL; CANNABINOIDS; CELL LINE, TRANSFORMED; CELLS, CULTURED; EMBRYONIC STEM CELLS; GLYCINE; HUMANS; MEMBRANE POTENTIALS; RECEPTORS, GLYCINE; TRANSFECTION;

EID: 59549106886     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000201556     Document Type: Article

References (21)

1. Betz H, Laube B: Glycine receptors: recent insights into their structural organization and functional diversity. J Neurochem 2006; 97:1600-1610.
2. Knabl J, Witschi R, Hosl K, et al: Reversal of pathological pain through specific spinal GABAA receptor subtypes. Nature 2008; 451: 330-334.
3. Laube B, Maksay G, Schemm R, Betz H: Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses? Trends Pharmacol Sci 2002; 23: 519-527.
4. Zeilhofer HU: The glycinergic control of spinal pain processing. Cell Mol Life Sci 2005; 62:2027-2035.
5. Hejazi N, Zhou C, Oz M, et al: Delta9-tetra-hydrocannabinol and endogenous cannabinoid anandamide directly potentiate the function of glycine receptors. Mol Pharmacol 2006; 69:991-997.
6. Mihic SJ, Ye Q, Wick MJ, et al: Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors. Nature 1997; 389:385-389.
7. Costa B: On the pharmacological properties of Delta9-tetrahydrocannabinol (THC). Chem Biodivers 2007; 4:1664-1677.
8. McCarberg BH, Barkin RL: The future of cannabinoids as analgesic agents: a pharma-cologic, pharmacokinetic, and pharmacody-namic overview. Am J Ther 2007; 14: 475-483.
9. Mechoulam R, Peters M, Murillo-Rodriguez E, Hanus LO: Cannabidiol: recent advances. Chem Biodivers 2007; 4:1678-1692.
10. Pribilla I, Takagi T, Langosch D, et al: The atypical M2 segment of the beta subunit confers picrotoxinin resistance to inhibitory glycine receptor channels. EMBO J 1992; 11: 4305-4311.
11. Haeseler G, Ahrens J, Kr a mpf l K, et a l : St r uctural 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.
12. 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: 85-10 0.
13. Franke C, Hatt H, Dudel J: Liquid filament switch for ultra-fast exchanges of solutions at excised patches of synaptic membrane of crayf ish muscle. Neurosci Lett 1987; 77: 199-204.
14. 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.
15. Jentsch TJ, Stein V, Weinreich F, Zdebik AA: Molecular structure and physiological function of chloride channels. Physiol Rev 2002; 82: 503-568.
16. Gr udzi nsk a J, Schem m R , Hae ger S , e t a l: T he beta subunit determines the ligand binding properties of synaptic glycine receptors. Neuron 2005; 45: 727-739.
17. Shan Q, Haddrill JL, Lynch JW: A single beta subunit M2 domain residue controls the picrotoxin sensitivity of alphabeta heteromeric glycine receptor chloride channels. J Neurochem 2001; 76: 1109-1120.
18. 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.
19. Agarwal N, Pacher P, Tegeder I, et al: Cannabinoids mediate analgesia largely via peripheral type 1 cannabinoid receptors in nociceptors. Nat Neurosci 2007; 10: 870-879.
20. Iatsenko NM, Tsintsadze T, Lozova NO: The synthetic cannabinoid analog WIN 55,212-2 potentiates the amplitudes of glycine-acti-vated currents. Fiziol Zh 2007; 53:31-37.
21. Tao Q, McAllister SD, Andreassi J, et al: Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity. Mol Pharmacol 1999; 55:605-613.