gaba modulators

Summary

Summary: Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.

Top Publications

  1. Paterson N, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A. Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. J Pharmacol Exp Ther. 2008;326:306-14 pubmed publisher
    ..Thus, GABA(B) receptor-positive modulators may be useful antismoking medications. ..
  2. Ho K, Ismail H. Use of intrathecal midazolam to improve perioperative analgesia: a meta-analysis. Anaesth Intensive Care. 2008;36:365-73 pubmed
    ..A multicentre registry or large randomised controlled study with a prolonged follow-up period would be useful to confirm the clinical safety of intrathecal midazolam. ..
  3. Zaugg J, Baburin I, Strommer B, Kim H, Hering S, Hamburger M. HPLC-based activity profiling: discovery of piperine as a positive GABA(A) receptor modulator targeting a benzodiazepine-independent binding site. J Nat Prod. 2010;73:185-91 pubmed publisher
    ..These data show that piperine (5) represents a new scaffold of positive allosteric GABA(A) receptor modulators targeting a benzodiazepine-independent binding site...
  4. Rudolph U, Knoflach F. Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes. Nat Rev Drug Discov. 2011;10:685-97 pubmed publisher
  5. Di Lio A, Benke D, Besson M, Desmeules J, Daali Y, Wang Z, et al. HZ166, a novel GABAA receptor subtype-selective benzodiazepine site ligand, is antihyperalgesic in mouse models of inflammatory and neuropathic pain. Neuropharmacology. 2011;60:626-32 pubmed publisher
    ..e. no tolerance development). These findings provide further evidence that compounds selective for ?2- and ?3-GABA(A) receptors might constitute a novel class of analgesics suitable for the treatment of chronic pain. ..
  6. Zaugg J, Eickmeier E, Ebrahimi S, Baburin I, Hering S, Hamburger M. Positive GABA(A) receptor modulators from Acorus calamus and structural analysis of (+)-dioxosarcoguaiacol by 1D and 2D NMR and molecular modeling. J Nat Prod. 2011;74:1437-43 pubmed publisher
    ..9%; EC??: 109.4 ± 46.6 ?M and 6: 241% ± 23.1%; EC??: 34.0 ± 6.7 ?M). The relative configuration of 2 was established as 4R*8S*10R* by NOESY experiments and conformational analysis. ..
  7. Maccioni P, Thomas A, Carai M, Gessa G, Malherbe P, Colombo G. The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration. Drug Alcohol Depend. 2010;109:96-103 pubmed publisher
    ..The present data constitute a further piece of evidence on the capacity of positive allosteric modulators of the GABA(B) receptor to reduce alcohol's reinforcing properties in rats. ..
  8. Zaugg J, Khom S, Eigenmann D, Baburin I, Hamburger M, Hering S. Identification and characterization of GABA(A) receptor modulatory diterpenes from Biota orientalis that decrease locomotor activity in mice. J Nat Prod. 2011;74:1764-72 pubmed publisher
    ..No significant anxiolytic-like activity was observed in doses between 1 and 30 mg/kg body weight in mice. ..
  9. Maccioni P, Carai M, Kaupmann K, Guery S, Froestl W, Leite Morris K, et al. Reduction of alcohol's reinforcing and motivational properties by the positive allosteric modulator of the GABA(B) receptor, BHF177, in alcohol-preferring rats. Alcohol Clin Exp Res. 2009;33:1749-56 pubmed publisher

More Information

Publications92

  1. Costa C, Kohn D, de Lima V, Gargano A, Florio J, Costa M. The GABAergic system contributes to the anxiolytic-like effect of essential oil from Cymbopogon citratus (lemongrass). J Ethnopharmacol. 2011;137:828-36 pubmed publisher
    ..However, despite this widely use, there are few controlled studies confirming its biological activity in central nervous system...
  2. Ong J, Kerr D. Clinical potential of GABAB receptor modulators. CNS Drug Rev. 2005;11:317-34 pubmed
  3. Campo Soria C, Chang Y, Weiss D. Mechanism of action of benzodiazepines on GABAA receptors. Br J Pharmacol. 2006;148:984-90 pubmed
    ..8+/-3.7 nM). Our results support a mechanism in which DZP increases the apparent affinity of the receptor, not by altering the affinity of the closed state, but rather by shifting the equilibrium towards the high-affinity open state. ..
  4. Paronis C. Modulating GABA modulators. Br J Pharmacol. 2006;147:237-8 pubmed
    ..of ligands for each of these distinct binding sites, very little research has examined the effects of GABA modulators given in combination...
  5. García D, Bujons J, Vale C, Suñol C. Allosteric positive interaction of thymol with the GABAA receptor in primary cultures of mouse cortical neurons. Neuropharmacology. 2006;50:25-35 pubmed
    ..Thymol (0-1 mM) did not affect cellular viability. ..
  6. Downing S, Lee Y, Farb D, Gibbs T. Benzodiazepine modulation of partial agonist efficacy and spontaneously active GABA(A) receptors supports an allosteric model of modulation. Br J Pharmacol. 2005;145:894-906 pubmed
  7. Rüsch D, Forman S. Classic benzodiazepines modulate the open-close equilibrium in alpha1beta2gamma2L gamma-aminobutyric acid type A receptors. Anesthesiology. 2005;102:783-92 pubmed
    ..A Monod-Wyman-Changeux coagonist gating model quantitatively predicts these effects, suggesting that benzodiazepines minimally alter orthosteric ligand binding. ..
  8. Feng H, Bianchi M, Macdonald R. Pentobarbital differentially modulates alpha1beta3delta and alpha1beta3gamma2L GABAA receptor currents. Mol Pharmacol. 2004;66:988-1003 pubmed
    ..The remarkable increase in gating efficacy of alpha1beta3delta receptors suggests that alphabetadelta isoforms, and by inference tonic forms of inhibition, may be important targets for barbiturates. ..
  9. Akk G, Bracamontes J, Steinbach J. Activation of GABA(A) receptors containing the alpha4 subunit by GABA and pentobarbital. J Physiol. 2004;556:387-99 pubmed
    ..The results from single-channel experiments were confirmed by macroscopic recordings from HEK cells in the presence of GABA or pentobarbital. ..
  10. Baur R, Simmen U, Senn M, Séquin U, Sigel E. Novel plant substances acting as beta subunit isoform-selective positive allosteric modulators of GABAA receptors. Mol Pharmacol. 2005;68:787-92 pubmed
    ..In summary, these positive allosteric modulators of GABAA receptors of plant origin have a novel unusual chemical structure and act at a site independent of that of benzodiazepines and loreclezole. ..
  11. Ahveninen J, Lin F, Kivisaari R, Autti T, HAMALAINEN M, Stufflebeam S, et al. MRI-constrained spectral imaging of benzodiazepine modulation of spontaneous neuromagnetic activity in human cortex. Neuroimage. 2007;35:577-82 pubmed
    ..Anatomically constrained spectral imaging displays the cortical loci of drug effects on oscillatory brain activity, providing a novel tool for human pharmacological neuroimaging. ..
  12. Khom S, Baburin I, Timin E, Hohaus A, Sieghart W, Hering S. Pharmacological properties of GABAA receptors containing gamma1 subunits. Mol Pharmacol. 2006;69:640-9 pubmed
    ..05). These data provide new insight into the pharmacological properties of GABA(A) receptors containing gamma(1) subunits and may aid in the design of specific ligands for this receptor subtype. ..
  13. Orru A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, et al. Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur J Pharmacol. 2005;525:105-11 pubmed
    ..These data also suggest that positive allosteric modulation of the GABA(B) receptor may constitute a potential strategy for developing new drugs for treating alcohol dependence. ..
  14. Liang J, Chen F, Krstew E, Cowen M, Carroll F, Crawford D, et al. The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology. 2006;50:632-9 pubmed
    ..These data demonstrate the potential of positive allosteric modulators of metabotropic GABA(B) receptors to regulate alcohol responding...
  15. Bustos S, Maldonado H, Molina V. Midazolam disrupts fear memory reconsolidation. Neuroscience. 2006;139:831-42 pubmed
    ..All these data support the idea that stimulating GABA A receptor sites via MDZ selectively disrupts the reconsolidation process of a contextual fear memory. ..
  16. Li J, Fish R, Cook S, Tattersall F, Atack J. Comparison of in vivo and ex vivo [3H]flumazenil binding assays to determine occupancy at the benzodiazepine binding site of rat brain GABAA receptors. Neuropharmacology. 2006;51:168-72 pubmed
    ..0mg/kg). As expected, ex vivo binding can give an underestimation of receptor occupancy but this can be minimised by careful attention to the kinetics of unlabelled drug and radioligand. ..
  17. Fedi M, Berkovic S, Marini C, Mulligan R, Tochon Danguy H, Reutens D. A GABAA receptor mutation causing generalized epilepsy reduces benzodiazepine receptor binding. Neuroimage. 2006;32:995-1000 pubmed
    ..As synaptic inhibition in the human brain is largely mediated by the GABA(A) receptor, these findings are likely to represent an important clue to the mechanisms linking this gene defect and the epilepsy phenotype. ..
  18. Khom S, Baburin I, Timin E, Hohaus A, Trauner G, Kopp B, et al. Valerenic acid potentiates and inhibits GABA(A) receptors: molecular mechanism and subunit specificity. Neuropharmacology. 2007;53:178-87 pubmed
    ..A possible open channel block mechanism is discussed. In summary, VA was identified as a subunit specific allosteric modulator of GABA(A) receptors that is likely to interact with the loreclezole binding pocket. ..
  19. Yamawaki N, Stanford I, Hall S, Woodhall G. Pharmacologically induced and stimulus evoked rhythmic neuronal oscillatory activity in the primary motor cortex in vitro. Neuroscience. 2008;151:386-95 pubmed
    ..Stimulation at 20 Hz evoked mixed theta and gamma responses. These data suggest that within M1, evoked theta, gamma and fast oscillations may coexist with and in some cases modulate pharmacologically induced beta oscillations. ..
  20. Riker R, Shehabi Y, Bokesch P, Ceraso D, Wisemandle W, Koura F, et al. Dexmedetomidine vs midazolam for sedation of critically ill patients: a randomized trial. JAMA. 2009;301:489-99 pubmed publisher
    ..The most notable adverse effect of dexmedetomidine was bradycardia. clinicaltrials.gov Identifier: NCT00216190 Published online February 2, 2009 (doi:10.1001/jama.2009.56). ..
  21. Ayissi Mbomo R, Gartside S, Ngo Bum E, Njikam N, Okello E, McQuade R. Effect of Mimosa pudica (Linn.) extract on anxiety behaviour and GABAergic regulation of 5-HT neuronal activity in the mouse. J Psychopharmacol. 2012;26:575-83 pubmed publisher
    ..This study suggests that the aqueous extract of M. pudica L. contains a positive modulator of GABA(A) receptor function and provides impetus for further investigation of the neuropharmacologically active constituents of the extract...
  22. Hall S, Barnes G, Furlong P, Seri S, Hillebrand A. Neuronal network pharmacodynamics of GABAergic modulation in the human cortex determined using pharmaco-magnetoencephalography. Hum Brain Mapp. 2010;31:581-94 pubmed publisher
  23. Alonso J, Mananas M, Romero S, Hoyer D, Riba J, Barbanoj M. Drug effect on EEG connectivity assessed by linear and nonlinear couplings. Hum Brain Mapp. 2010;31:487-97 pubmed publisher
    ..The use of both linear and nonlinear approaches revealed the importance of assessing changes in EEG connectivity as this can provide interesting information about psychopharmacological effects. ..
  24. Askgaard G, Hallas J, Fink Jensen A, Molander A, Madsen K, Pottegård A. Phenobarbital compared to benzodiazepines in alcohol withdrawal treatment: A register-based cohort study of subsequent benzodiazepine use, alcohol recidivism and mortality. Drug Alcohol Depend. 2016;161:258-64 pubmed publisher
    ..Phenobarbital treatment was associated with decreased mortality, which might be confounded by somatic comorbidity among patients receiving chlordiazepoxide. ..
  25. Spence A, Guerin G, Goeders N. Differential modulation of the discriminative stimulus effects of methamphetamine and cocaine by alprazolam and oxazepam in male and female rats. Neuropharmacology. 2016;102:146-57 pubmed publisher
    ..These results also demonstrate that alprazolam can differentially affect the discriminative stimulus effects of methamphetamine and cocaine. ..
  26. Qian M, Krishnan K, Kudova E, Li P, Manion B, Taylor A, et al. Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of ?-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone. J Med Chem. 2014;57:171-90 pubmed publisher
    ..The results indicate that ent-steroids have considerable potential to be developed as anesthetic agents and as drugs to treat brain disorders that are ameliorated by positive allosteric modulators of GABAA receptor function. ..
  27. Grasshoff C, Netzhammer N, Schweizer J, Antkowiak B, Hentschke H. Depression of spinal network activity by thiopental: shift from phasic to tonic GABA(A) receptor-mediated inhibition. Neuropharmacology. 2008;55:793-802 pubmed publisher
    ..With increasing concentrations of the drug, inhibition via sIPSCs is limited by negative feedback on interneuronal firing whereas action potential-independent GABAergic inhibition due to tonic currents gains progressively in impact. ..
  28. Søgaard R, Ebert B, Klaerke D, Werge T. Triton X-100 inhibits agonist-induced currents and suppresses benzodiazepine modulation of GABA(A) receptors in Xenopus oocytes. Biochim Biophys Acta. 2009;1788:1073-80 pubmed publisher
    ..The present study suggests that Triton X-100 may stabilize open and desensitized states of the GABA(A) receptor through changes in lipid bilayer elasticity. ..
  29. Petrus D, Fabel K, Kronenberg G, Winter C, Steiner B, Kempermann G. NMDA and benzodiazepine receptors have synergistic and antagonistic effects on precursor cells in adult hippocampal neurogenesis. Eur J Neurosci. 2009;29:244-52 pubmed publisher
    ..We propose that NMDA receptor-dependent signalling maintains the precursor cells in the dentate gyrus while blocking initial stages of development and promoting more advanced stages. ..
  30. Zier J, Rivard P, Krach L, Wendorf H. Effectiveness of sedation using nitrous oxide compared with enteral midazolam for botulinum toxin A injections in children. Dev Med Child Neurol. 2008;50:854-8 pubmed publisher
    ..One child in the midazolam group and eight in the N(2)O group had adverse effects, all of which resolved promptly. N(2)O appears to be an effective means of sedation for children undergoing outpatient BoNT-A injections. ..
  31. Bell C, Hood S, Potokar J, Nash J, Adrover M, Frampton C, et al. Rapid tryptophan depletion following cognitive behavioural therapy for panic disorder. Psychopharmacology (Berl). 2011;213:593-602 pubmed publisher
    ..We suggest that the partial return of symptoms in response to flumazenil reflects a vulnerability to RTD in this group of panic disorder patients who had responded to treatment with CBT. ..
  32. Walsh J, Thacker S, Knowles L, Tasker T, Hunneyball I. The partial positive allosteric GABA(A) receptor modulator EVT 201 is efficacious and safe in the treatment of adult primary insomnia patients. Sleep Med. 2009;10:859-64 pubmed publisher
    ..Adverse events were infrequent and all were mild to moderate in severity. ..
  33. Grundmann O, Wang J, McGregor G, Butterweck V. Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic system. Planta Med. 2008;74:1769-73 pubmed publisher
    ..The active dose was effectively antagonized by flumazenil, but not by WAY-100 635. This study is the first demonstration of the IN VIVO, GABA-mediated anxiolytic activity of an HPLC- characterized extract of Passiflora incarnata. ..
  34. Gannon R, Millan M. Positive allosteric modulators at GABAB receptors exert intrinsic actions and enhance the influence of baclofen on light-induced phase shifts of hamster circadian activity rhythms. Pharmacol Biochem Behav. 2011;99:712-7 pubmed publisher
    ..GABA(B) receptors clearly warrant further investigation as agents for modulation of circadian dysfunction associated with CNS disorders such as depression. ..
  35. Garlet Q, Pires L, Milanesi L, Marafiga J, Baldisserotto B, Mello C, et al. (+)-Dehydrofukinone modulates membrane potential and delays seizure onset by GABAa receptor-mediated mechanism in mice. Toxicol Appl Pharmacol. 2017;332:52-63 pubmed publisher
    ..The present study highlights the therapeutic potential of the natural compound DHF as a suppressor of neuronal excitability. ..
  36. Vuilleumier P, Besson M, Desmeules J, Arendt Nielsen L, Curatolo M. Evaluation of anti-hyperalgesic and analgesic effects of two benzodiazepines in human experimental pain: a randomized placebo-controlled study. PLoS ONE. 2013;8:e43896 pubmed publisher
    ..Our data also provide information on the most suitable experimental models for future investigation of GABAergic compounds. ClinicalTrials.gov NCT01011036. ..
  37. Curley M, Ferrigno M, Lovrincevic M, Wylegala J, Lundgren C. Extending submarine crew survival by reducing CO2 production with quickly reversible sedation. Aviat Space Environ Med. 2010;81:537-44 pubmed
    ..Reversible sedation to lower crew metabolism in a disabled submarine may be effective, safe, and practical. ..
  38. de Moraes M, do Amaral Bezerra B, da Rocha Neto P, de Oliveira Soares A, Pinto L, de Lisboa Lopes Costa A. Randomized trials for the treatment of burning mouth syndrome: an evidence-based review of the literature. J Oral Pathol Med. 2012;41:281-7 pubmed publisher
    ..Thus, future studies are required to establish the treatment for patients suffering from this chronic and painful syndrome. ..
  39. Kukanich B, Hubin M. The pharmacokinetics of ketoconazole and its effects on the pharmacokinetics of midazolam and fentanyl in dogs. J Vet Pharmacol Ther. 2010;33:42-9 pubmed publisher
    ..81 to 1.49 h. The elimination of fentanyl was not significantly altered by co-administration of ketoconazole with the MRT being 3.90 and 6.35 h. The MRT was the most robust estimate of decreased drug elimination. ..
  40. Klumpers U, Boellaard R, Veltman D, Kloet R, Hoogendijk W, Lammertsma A. Parametric [11C]flumazenil images. Nucl Med Commun. 2012;33:422-30 pubmed publisher
    ..Parametric Logan VT, MRTM2 and RPM1-2 BP ND methods allow the best quantitative comparison of FMZ binding between groups and show good discriminating performance in SPM analysis. ..
  41. Namjoshi D, McErlane S, Taepavarapruk N, Soja P. Network actions of pentobarbital in the rat mesopontine tegmentum on sensory inflow through the spinothalamic tract. J Neurophysiol. 2009;102:700-13 pubmed publisher
    ..This study provides a provenance for investigating electrophysiologically the actions on STT neurons of other current agents used clinically to maintain the state of general anesthesia. ..
  42. Wang L, Chen Y, Chen C, Chou W, Chou M. Trends in anxiolytic-hypnotic use and polypharmacy in Taiwan, 2002-2009: a nationwide, population-based survey. Psychiatr Serv. 2014;65:208-14 pubmed publisher
    ..The adverse effects of the long-term use of anxiolytics-hypnotics have been established, and unnecessary use of these drugs, particularly in polypharmacy regimens, should be avoided. ..
  43. Carter L. Potential impact of drug effects, availability, pharmacokinetics, and screening on estimates of drugs implicated in cases of assault. Drug Test Anal. 2011;3:586-93 pubmed publisher
  44. Minc D, Machado S, Bastos V, Machado D, Cunha M, Cagy M, et al. Gamma band oscillations under influence of bromazepam during a sensorimotor integration task: an EEG coherence study. Neurosci Lett. 2010;469:145-9 pubmed publisher
    ..We propose that the gamma band plays an important role in the binding among several brain areas in complex motor tasks and that each hemisphere is influenced in a different manner by the neuromodulator. ..
  45. West R, Pesce A, West C, Crews B, Mikel C, Almazan P, et al. Comparison of clonazepam compliance by measurement of urinary concentration by immunoassay and LC-MS/MS in pain management population. Pain Physician. 2010;13:71-8 pubmed
    ..These data illustrate the limitations of using a 200 ng/mL cutoff to monitor clonazepam compliance and suggest that a cutoff of 40 ng/mL or less is needed to reliably monitor use of this drug. ..
  46. Tandra S, Chalasani N, Jones D, Mattar S, Hall S, Vuppalanchi R. Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients. Ann Surg. 2013;258:262-9 pubmed publisher
    ..RYGB recipients have significantly shorter tmax for the studied orally administered medications, but otherwise no other significant changes in PK were reported. ..
  47. Facciolo R, Crudo M, Zizza M, Giusi G, Canonaco M. ? GABA(A) subunit-orexin receptor interactions activate learning/motivational pathways in the goldfish. Behav Brain Res. 2012;234:349-56 pubmed publisher
  48. Seymour V, Everitt A, Tierney M. Differential drug responses on native GABA(A) receptors revealing heterogeneity in extrasynaptic populations in cultured hippocampal neurons. J Membr Biol. 2009;227:111-22 pubmed publisher
  49. Tanabe K, Kozawa O, Iida H. Midazolam suppresses interleukin-1?-induced interleukin-6 release from rat glial cells. J Neuroinflammation. 2011;8:68 pubmed publisher
    ..These results strongly suggest that midazolam inhibits IL-1?-induced IL-6 release in rat C6 glioma cells via suppression of STAT3 activation. Midazolam may affect immune system function in the CNS. ..
  50. Markoula S, Konitsiotis S, Chatzistefanidis D, Lagos G, Kyritsis A. Akathisia induced by mirtazapine after 20 years of continuous treatment. Clin Neuropharmacol. 2010;33:50-1 pubmed publisher
    ..It illustrates the importance of being alert to any movement disorder emerging in patients treated with mirtazapine, even after many years of treatment. ..
  51. Leiter E, Hitchcock G, Godwin S, Johnson M, Sedgwick W, Jones W, et al. Evaluation of the anxiolytic properties of myristicin, a component of nutmeg, in the male Sprague-Dawley rat. AANA J. 2011;79:109-14 pubmed
    ..Myristicin may antagonize the anxiolytic effects of midazolam, increase anxiety, and affect motor movements. ..
  52. Su C, Miao J, Liu Y, Liu R, Lei G, Zhang W, et al. Multiple forms of rhythmic movements in an adolescent boy with rhythmic movement disorder. Clin Neurol Neurosurg. 2009;111:896-9 pubmed publisher
  53. Zwierzyńska E, Pietrzak B. [Retigabine - a new antiepileptic drug with a different mechanism of action]. Postepy Hig Med Dosw (Online). 2013;67:973-81 pubmed publisher
    ..The efficacy of retigabine is being tested in other types of seizures and disorders characterized by neuronal hyperexcitability. Neuroprotective activity of retigabine is also being researched. ..
  54. Hall S, Stanford I, Yamawaki N, McAllister C, Rönnqvist K, Woodhall G, et al. The role of GABAergic modulation in motor function related neuronal network activity. Neuroimage. 2011;56:1506-10 pubmed publisher
    ..However, in contrast, the transient increase in synchronous power observed in PMBR and MRGS appears to be generated by a non-GABA-A receptor mediated process; the elucidation of which may offer important insights into motor processes. ..
  55. Frankle W, Cho R, Mason N, Chen C, Himes M, Walker C, et al. [11C]flumazenil binding is increased in a dose-dependent manner with tiagabine-induced elevations in GABA levels. PLoS ONE. 2012;7:e32443 pubmed publisher
    ..67, p = 0.05) measured via EEG during a cognitive control task. These data provide a replication of our previous study demonstrating the ability to measure in vivo, with PET, acute shifts in extracellular GABA. ..
  56. Foster K, Lin S, Turck C. Current and emerging strategies for treating hepatic encephalopathy. Crit Care Nurs Clin North Am. 2010;22:341-50 pubmed publisher
    ..Probiotics, acarbose, and drugs such as L-carnitine and flumazenil, may also be helpful in treating HE. ..
  57. Mikulecká A, Mares P, Kubova H. Rebound increase in seizure susceptibility but not isolation-induced calls after single administration of clonazepam and Ro 19-8022 in infant rats. Epilepsy Behav. 2011;20:12-9 pubmed publisher
    ..Anxiolytic-like effects of these drugs were still present at the time when animals exhibited rebound proconvulsant effects. ..
  58. Eppolito A, Bai X, Gerak L. Discriminative stimulus effects of pregnanolone in rats: role of training dose in determining mechanism of action. Psychopharmacology (Berl). 2012;223:139-47 pubmed publisher
    ..There was little difference in discriminative stimulus effects of pregnanolone across different training conditions, confirming a predominant, if not exclusive, role of GABA(A) receptors in these effects of pregnanolone. ..
  59. Deeb T, Nakamura Y, Frost G, Davies P, Moss S. Disrupted Cl(-) homeostasis contributes to reductions in the inhibitory efficacy of diazepam during hyperexcited states. Eur J Neurosci. 2013;38:2453-67 pubmed publisher
  60. Kim H, Hwang K, Park W. Cardioprotection via modulation of calcium homeostasis by thiopental in hypoxia-reoxygenated neonatal rat cardiomyocytes. Yonsei Med J. 2010;51:187-96 pubmed publisher
    ..Thiopental is likely to modulate expression of genes that regulate Ca(2+) homeostasis, which reduces apoptotic cell death and results in cardioprotection. ..
  61. Di Domenico S, Santori G, Balbis E, Traverso N, Gentile R, Bocca B, et al. Biochemical and morphologic effects after extended liver resection in rats: preliminary results. Transplant Proc. 2010;42:1061-5 pubmed publisher
    ..Mitochondrial dysfunction and oxidative injury seem to have a crucial role in early onset of liver damage. ..
  62. Fajemiroye J, Galdino P, Alves S, de Paula J, de Paula J, Ghedini P, et al. Involvement of 5-HT1A in the anxiolytic-like effect of dichloromethane fraction of Pimenta pseudocaryophyllus. J Ethnopharmacol. 2012;141:872-7 pubmed publisher
    ..Despite its popular therapeutic acceptance and claims, there are scanty scientific reports to corroborate its central biological activities...
  63. Dashti Khavidaki S, Chamani N, Khalili H, Hajhossein Talasaz A, Ahmadi F, Lessan Pezeshki M, et al. Comparing effects of clonazepam and zolpidem on sleep quality of patients on maintenance hemodialysis. Iran J Kidney Dis. 2011;5:404-9 pubmed
    ..03). Zolpidem was better tolerated in the hemodialysis patients. Clonazepam was more effective than zolpidem in the improvement of sleep quality of hemodialysis patients, while zolpidem was better tolerated in these patients. ..
  64. Contó M, Hipolide D, de Carvalho J, Venditti M. Rats with different thresholds for DMCM-induced clonic convulsions differ in the sleep-time of diazepam and [(3)H]-Ro 15-4513 binding. Epilepsy Res. 2012;98:216-22 pubmed publisher
    ..These results suggest that differences in the benzodiazepine site on the GABA(A) receptor may underlie the susceptibility to DMCM-induced convulsions and sensitivity to the hypnotic effect of diazepam. ..
  65. Hoestgaard Jensen K, Dalby N, Wolinsky T, Murphey C, Jones K, Rottländer M, et al. Pharmacological characterization of a novel positive modulator at alpha 4 beta 3 delta-containing extrasynaptic GABA(A) receptors. Neuropharmacology. 2010;58:702-11 pubmed publisher
    ..We conclude that AA29504 exerts a major action via alpha(4)beta(3)delta-containing GABA(A) receptors, which will be important for interpreting its effect in vivo. ..
  66. Myers T, Hamilton L. Delayed match-to-sample performance in African green monkeys (Chlorocebus aethiops sabaeus): effects of benzodiazepine, cholinergic, and anticholinergic drugs. Behav Pharmacol. 2011;22:814-23 pubmed publisher
    ..Thus, the African green monkey may function as a suitable alternative to macaque species in behavioral pharmacology research. ..
  67. Bossard J, Ponté C, Dupouy J, Lapeyre Mestre M, Jouanjus E. Disproportionality Analysis for the Assessment of Abuse and Dependence Potential of Pregabalin in the French Pharmacovigilance Database. Clin Drug Investig. 2016;36:735-742 pubmed publisher
    ..Considering evidence of pregabalin abuse worldwide, this analysis underlines the limitations of spontaneous reporting system in the field of addictovigilance. ..
  68. Watson T, Petrakis I, Edgecombe J, Perrino A, Krystal J, Mathalon D. Modulation of the cortical processing of novel and target stimuli by drugs affecting glutamate and GABA neurotransmission. Int J Neuropsychopharmacol. 2009;12:357-70 pubmed publisher
    ..Overall, the data suggest that both the GABA-A and NMDA receptor systems modulate P3b and P3a. NMDA antagonism appears to lead to more varied effects on the neural correlates of novelty processing. ..
  69. Yilmaz K, Sahin D. Midazolam or diazepam administration during electroencephalography helps to diagnose subacute sclerosing panencephalitis (SSPE). J Child Neurol. 2010;25:994-9 pubmed publisher
    ..The findings suggest that midazolam or diazepam administration increases the contribution of EEG recording in atypical cases with subacute sclerosing panencephalitis. ..
  70. Araújo F, Machado S, Paes F, Cunha M, Budde H, Cagy M, et al. The effects of bromazepam over the temporo-parietal areas during the performance of a visuomotor task: a qEEG study. Neurosci Lett. 2011;496:116-20 pubmed publisher
    ..We then hypothesize about the specific role of this drug during the execution of a visuomotor task and within the sensorimotor integration process. ..
  71. Kamino H, Yamazaki Y, Saito K, Takizawa D, Kakizaki S, Moore R, et al. Nuclear receptor CAR-regulated expression of the FAM84A gene during the development of mouse liver tumors. Int J Oncol. 2011;38:1511-20 pubmed publisher
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    ..Diazepam inhibits the proliferation of human GBM T98G cells by inducing G0/G1 phase arrest. Diazepam has potential to be a lead for new drugs in GBM therapy because of its antitumor activity. ..
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    ..Exploratory post hoc analyses revealed that midazolam exposure was 1.9-fold higher in men compared to women. i.v. flumazenil can be used in conjunction with oral midazolam for CYP3A phenotyping. ..
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    ..0 mg/kg zolpidem. These data raise the possibility that ?1 subunit-containing GABAA receptors play a major role in physical dependence-related behaviors following a single injection of a benzodiazepine. ..
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    ..Midazolam is an efficient treatment for RSE in children. Morbidity and mortality appear to be lower with midazolam compared with other antiepileptic drugs used for the treatment of RSE. ..
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    ..The CASE PR paradigm shows promise as a laboratory method for use in drug development and phenotyping studies. ..
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    ..These changes may be due to neonatal alterations in BDNF levels. ..
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    ..Our results suggest that ACZP was a weak partial BZR agonist and that ACZP may competitively modify the effect of CZP, leading to clinical consequences for patients with high levels of ACZP. ..