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J. Bloomquist, P. Adams, D. Soderlund (1986)
Inhibition of gamma-aminobutyric acid-stimulated chloride flux in mouse brain vesicles by polychlorocycloalkane and pyrethroid insecticides.Neurotoxicology, 7 3
D. Turner, R. Ransom, J. Yang, R. Olsen (1989)
Steroid anesthetics and naturally occurring analogs modulate the gamma-aminobutyric acid receptor complex at a site distinct from barbiturates.The Journal of pharmacology and experimental therapeutics, 248 3
P. Suzdak (1993)
Lipophilic GABA uptake inhibitors: Biochemistry, pharmacology and therapeutic potentialDrugs of The Future, 18
(1998)
Eects of iso ̄urane and cis-9,10-octadecenoamide (cOA) on the rho(1) GABA receptor
D. Belelli, M. Pistis, J. Peters, J. Lambert (1999)
General anaesthetic action at transmitter-gated inhibitory amino acid receptors.Trends in pharmacological sciences, 20 12
B. Verdon, Jian Zheng, R. Nicholson, C Ganelli, G. Lees (2000)
Stereoselective modulatory actions of oleamide on GABAA receptors and voltage‐gated Na+ channels in vitro: a putative endogenous ligand for depressant drug sites in CNSBritish Journal of Pharmacology, 129
L. Hanus, H. Fales, T. Spande, A. Basile (1999)
A gas chromatographic-mass spectral assay for the quantitative determination of oleamide in biological fluids.Analytical biochemistry, 270 1
A. Mehta, M. Ticku (1999)
An update on GABAA receptorsBrain Research Reviews, 29
V. Koltchine, Ye Qing, S. Finn, N. Harrison (1996)
Chimeric GABAA/Glycine Receptors: Expression and Barbiturate PharmacologyNeuropharmacology, 35
B. Cravatt, O. Prospero-Garcia, G. Siuzdak, N. Gilula, S. Henriksen, D. Boger, R. Lerner (1995)
Chemical characterization of a family of brain lipids that induce sleep.Science, 268 5216
Yost Cs, Hampson Aj, D. Leonoudakis, Koblin Dd, Bornheim Lm, A. Gray (1998)
Oleamide potentiates benzodiazepine-sensitive gamma-aminobutyric acid receptor activity but does not alter minimum alveolar anesthetic concentration.Anesthesia & Analgesia, 86
B. Harris, E. Moody, E. Moody, Anthony Basile, Phil Skolnick (1994)
Volatile anesthetics bidirectionally and stereospecifically modulate ligand binding to GABA receptors.European journal of pharmacology, 267 3
L. Iversen, M. Neal (1968)
THE UPTAKE OF [3H]GABA BY SLICES OF RAT CEREBRAL CORTEXJournal of Neurochemistry, 15
D. Goodnough, J. Hawkinson (1995)
Neuroactive steroid modulation of [3H]muscimol binding to the GABAA receptor complex in rat cortex.European journal of pharmacology, 288 2
Joseph Cheer, A. Cadogan, C. Marsden, Kevin Fone, Dave Kendall (1999)
Modification of 5-HT2 receptor mediated behaviour in the rat by oleamide and the role of cannabinoid receptorsNeuropharmacology, 38
M. Negro, M. Chinchetru, Arsenio Fernández, P. Calvo (1995)
Effect of Ethanol Treatment on Rate and Equilibrium Constants for [3H]Muscimol Binding to Rat Brain Membranes: Alteration of Two Affinity States of the GABAA ReceptorJournal of Neurochemistry, 64
(1984)
The third international conference on molecular and cellular mechanisms of anaesthesiaPharmacology Biochemistry and Behavior, 20
S. Sakurai, A. Kume, D. Burdette, R. Albin (1994)
Quantitative autoradiography of [3H]t-butylbicycloorthobenzoate binding to the gamma-aminobutyric acid receptorA complex.The Journal of pharmacology and experimental therapeutics, 270 1
R. Nicholson, Jian Zheng, C. Ganellin, B. Verdon, G. Lees (2001)
Anesthetic-like Interaction of the Sleep-inducing Lipid Oleamide with Voltage-gated Sodium Channels in Mammalian BrainAnesthesiology, 94
D. Boger, J. Patterson, X. Guan, B. Cravatt, R. Lerner, N. Gilula (1998)
Chemical requirements for inhibition of gap junction communication by the biologically active lipid oleamide.Proceedings of the National Academy of Sciences of the United States of America, 95 9
S. Thompson, Paul Whiting, K. Wafford (1996)
Barbiturate interactions at the human GABAA receptor: dependence on receptor subunit combinationBritish Journal of Pharmacology, 117
N. Franks, W. Lieb (1994)
Molecular and cellular mechanisms of general anaesthesiaNature, 367
R. Halliwell, P. Thomas, D. Patten, C. James, A. Martínez-Torres, R. Miledi, T. Smart (1999)
Subunit‐selective modulation of GABAA receptors by the non‐steroidal anti‐inflammatory agent, mefenamic acidEuropean Journal of Neuroscience, 11
C. Thomsen, P. Sørensen, J. Egebjerg (1997)
1‐(3‐(9H‐Carbazol‐9‐yl)‐1‐propyl)‐4‐(2‐methoxyphenyl)‐4‐piperidinol, a novel subtype selective inhibitor of the mouse type II GABA‐transporterBritish Journal of Pharmacology, 120
G. Peterson (1977)
A simplification of the protein assay method of Lowry et al. which is more generally applicable.Analytical biochemistry, 83 2
Wallace Mendelson, Anthony Basile (1999)
The hypnotic actions of oleamide are blocked by a cannabinoid receptor antagonist.Neuroreport, 10 15
R. Ramanjaneyulu, M. Ticku (1984)
Binding Characteristics and Interactions of Depressant Drugs with [35S]t‐Butylbicyclophosphorothionate, a Ligand that Binds to the Picrotoxinin SiteJournal of Neurochemistry, 42
R. Squires, J. Casida, M. Richardson, E. Saederup (1983)
[35S]t-butylbicyclophosphorothionate binds with high affinity to brain-specific sites coupled to gamma-aminobutyric acid-A and ion recognition sites.Molecular pharmacology, 23 2
M. Edwards, G. Lees (1997)
Modulation of a recombinant invertebrate γ‐aminobutyric acid receptor‐chloride channel complex by isoflurane: effects of a point mutation in the M2 domainBritish Journal of Pharmacology, 122
P. Soja, F. López-Rodríguez, F. Morales, M. Chase (1991)
The postsynaptic inhibitory control of lumbar motoneurons during the atonia of active sleep: effect of strychnine on motoneuron properties, 11
Y. Ito, I. Ho (1994)
Studies on picrotoxin binding sites of GABAA receptors in rat cortical synaptoneurosomesBrain Research Bulletin, 33
R. Harris, A. Allan (1985)
Functional coupling of gamma-aminobutyric acid receptors to chloride channels in brain membranes.Science, 228 4703
T. Delorey, I. Kissin, P. Brown, G. Brown (1993)
Barbiturate‐Benzodiazepine Interactions at the γ‐Aminobutyric AcidA Receptor in Rat Cerebral Cortical SynaptoneurosomesAnesthesia & Analgesia, 77
R. Nicholson, G. Lees, Jian Zheng, B. Verdon (1999)
Inhibition of GABA‐gated chloride channels by 12,14‐dichlorodehydroabietic acid in mammalian brainBritish Journal of Pharmacology, 126
K. Wafford, C. Bain, K. Quirk, R. Mckernan, P. Wingrove, Paul Whiting, J. Kemp (1994)
A novel allosteric modulatory site on the GABAA receptor β subunitNeuron, 12
S. Mihic, S. Mihic, Q. Ye, M. Wick, V. Koltchine, Matthew Krasowski, S. Finn, M. Mascia, C. Valenzuela, Kirsten Hanson, Eric Greenblatt, R. Harris, R. Harris, Neil Harrison (1997)
Sites of alcohol and volatile anaesthetic action on GABAA and glycine receptorsNature, 389
(1977)
A simpli®cation of the protein assay
L. Tecott (2000)
Designer genes and anti-anxiety drugsNature Neuroscience, 3
K. Wafford, D. Burnett, N. Leidenheimer, D. Burt, Jia Wang, P. Kofuji, T. Dunwiddie, R. Harris, J. Sikela (1991)
Ethanol sensitivity of the GABAA receptor expressed in xenopus oocytes requires 8 amino acids contained in the γ2L subunitNeuron, 7
P. Pascoe (1994)
Drugs and the sleep-wakefulness continuum.Pharmacology & therapeutics, 61 1-2
LAWS (2001)
Oleamide: a putative endogenous ligand for anaesthetic receptor sitesBr. J. Anaesth., 87
D. Boring, B. Berglund, A. Howlett (1996)
Cerebrodiene, arachidonyl-ethanolamide, and hybrid structures: potential for interaction with brain cannabinoid receptors.Prostaglandins, leukotrienes, and essential fatty acids, 55 3
J. Huidobro‐Toro, R. Harris (1996)
Brain lipids that induce sleep are novel modulators of 5-hydroxytrypamine receptors.Proceedings of the National Academy of Sciences of the United States of America, 93 15
J. Koenig, I. Martin (1992)
Effect of free fatty acids on GABAA receptor ligand binding.Biochemical pharmacology, 44 1
D. Belelli, M. Pistis, J. Peters, J. Lambert (1999)
The interaction of general anaesthetics and neurosteroids with GABAA and glycine receptorsNeurochemistry International, 34
D. Martin, A. Smith (1972)
IONS AND THE TRANSPORT OF GAMMA‐AMINOBUTYRIC ACID BY SYNAPTOSOMESJournal of Neurochemistry, 19
D. Laws, B. Verdon, L. Coyne, G. Lees (2001)
Fatty acid amides are putative endogenous ligands for anaesthetic recognition sites in mammalian CNS.British journal of anaesthesia, 87 3
R. Lerner (1997)
A hypothesis about the endogenous analogue of general anesthesia.Proceedings of the National Academy of Sciences of the United States of America, 94 25
K. Beaumont, W. Chilton, H. Yamamura, S. Enna (1978)
Muscimol binding in rat brain: Association with synaptic GABA receptorsBrain Research, 148
Rachel Wilson, R. Nicoll (2001)
Endogenous cannabinoids mediate retrograde signalling at hippocampal synapsesNature, 410
J. Huang, J. Casida (1996)
Characterization of [3H]ethynylbicycloorthobenzoate ([3H]EBOB) binding and the action of insecticides on the gamma-aminobutyric acid-gated chloride channel in cultured cerebellar granule neurons.The Journal of pharmacology and experimental therapeutics, 279 3
D. Belelli, J. Lambert, J. Peters, K. Wafford, P. Whiting (1997)
The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid.Proceedings of the National Academy of Sciences of the United States of America, 94 20
George Lees, George Lees, Michelle Edwards, Abdul Hassoni, C. Ganellin, D. Galanakis (1998)
Modulation of GABAA receptors and inhibitory synaptic currents by the endogenous CNS sleep regulator cis‐9,10‐octadecenoamide (cOA)British Journal of Pharmacology, 124
L. Lawrence, C. Palmer, K. Gee, Xiaoyu Wang, H. Yamamura, J. Casida (1985)
t‐[3H]Butylbicycloorthobenzoate: New Radioligand Probe for the γ‐Aminobutyric Acid–Regulated Chloride IonophoreJournal of Neurochemistry, 45
M. Krasowski, N. Harrison (2000)
The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutationsBritish Journal of Pharmacology, 129
A. Basile, L. Hanus, W. Mendelson (1999)
Characterization of the hypnotic properties of oleamide.Neuroreport, 10 5
A. Itouji, N. Sakai, C. Tanaka, N. Saito (1996)
Neuronal and glial localization of two GABA transporters (GAT1 and GAT3) in the rat cerebellum.Brain research. Molecular brain research, 37 1-2
L. Cole, J. Casida (1992)
GABA-gated chloride channel: Binding site for 4′-ethynyl-4-n-[2,3-3H2]propylbicycloorthobenzoate ([3H]EBOB) in vertebrate brain and insect headPesticide Biochemistry and Physiology, 44
D. Boger, J. Patterson, Qing Jin (1998)
Structural requirements for 5-HT2A and 5-HT1A serotonin receptor potentiation by the biologically active lipid oleamide.Proceedings of the National Academy of Sciences of the United States of America, 95 8
M. Gobbi, T. Mennini, F. Valle, L. Cervo, M. Salmona, L. Diomede (1999)
Oleamide‐mediated sleep induction does not depend on perturbation of membrane homeoviscosityFEBS Letters, 463
We examine the sensitivity of GABAA and glycine receptors (same ionotropic superfamily) to oleamide. We address subunit‐dependence/modulatory mechanisms and analogies with depressant drugs. Oleamide modulated human GABAA currents (α1β2γ2L) in oocytes (EC50, 28.94±s.e.mean of 1.4 μM; Maximum 216%±35 of control, n=4). Modulation of human α1 glycine homo‐oligomers (significant), was less marked, with a lower EC50 (P<0.05) than GABA receptors (EC50, 22.12±1.4 μM; Maximum 171%±30, n=11). Only the hypnogenic cis geometric isomer enhanced glycine currents (without altering slope or maximal current, it reduced the glycine EC50 from 322 to 239 μM: P<0.001). Modulation was not voltage‐dependent or associated with a shift in Er. β1 containing GABAA receptors (insensitive to many depressant drugs) were positively modulated by oleamide. Oleamide efficacy was circa 2× greater at α1β1γ2L than α1β2γ2L (P=0.007). Splice variation in γ subunits did not alter oleamide sensitivity. cis‐9,10‐Octadecenoamide had no effect on the equilibrium binding of (3H)‐muscimol or (3H)‐EBOB to mouse brain membranes. It does not directly mimic GABA, or operate as a neurosteroid‐, benzodiazepine‐ or barbiturate‐like modulator of GABAA‐receptors. The transport of (3H)‐GABA into mouse brain synaptoneurosomes was unaffected by high micromolar concentrations of cis‐9,10‐octadecenoamide. Oleamide does not enhance GABA‐ergic currents or prolong IPSCs by inhibiting GABA transport. Oleamide is a non‐selective modulator of inhibitory ionotropic receptors. The sleep lipid exerts its effects indirectly, or at a novel recognition site on the GABAA complex. British Journal of Pharmacology (2002) 135, 1977–1987; doi:10.1038/sj.bjp.0704651
British Journal of Pharmacology – Wiley
Published: Apr 1, 2002
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