References
- OlfsonMKingMSchoenbaumMBenzodiazepine use in the United StatesJAMA Psychiatry201572213614225517224
- DantzerRBehavioral effects of benzodiazepines: a reviewNeurosci Biobehav Rev1977127186
- ShaderRGreenblattDBalterMAppropriate use and regulatory control of benzodiazepinesJ Clin Pharmacol19913197817841687147
- SternbachLThe benzodiazepine storyJ Med Chem19792211734039
- OlsenRWamsleyJLeeRLomaxPBenzodiazepine/barbiturate/GABA receptor-chloride ionophore complex in a genetic model for generalized epilepsyAdv Neurol1986443653783010677
- HarrisIAddiction to barbiturates and the barbiturate abstinence syndromeAnn Intern Med195033110812115426096
- WolfBGrohmannRBiberDBrennePRütherEBenzodiazepine abuse and dependence in psychiatric inpatientsPharmacopsychiatry19892225460
- BustoUSellersENaranjoCCappellHSanchez-CraigMSimpkinsJPatterns of benzodiazepine abuse and dependenceAddiction19868118794
- PerraultGMorelESangerDZivkovicBLack of tolerance and physical dependence upon repeated treatment with the novel hypnotic zolpidemJ Pharmacol Exp Ther199226312983031403792
- Victorri-VigneauCDaillyEVeyracGJollietPEvidence of zolpidem abuse and dependence: results of the French Centre for Evaluation and Information on Pharmacodependence (CEIP) network surveyBr J Clin Pharmacol200764219820917324242
- KlepnerCLippaABensonDSanoMBeerBResolution of two biochemically and pharmacologically distinct benzodiazepine receptorsPharmacol Biochem Behav1979114457462523502
- AtackJRegional differences in the inhibition of mouse in vivo [3H] Ro 15-1788 binding reflect selectivity for α1 versus α2 and α3 subunit-containing GABAA receptorsNeuropsychopharmacology199920325526210063485
- SieghartWGABAA receptors: ligand-gated Cl− ion channels modulated by multiple drug-binding sitesTrends Pharmacol Sci199213124464501338138
- StudyRBarkerJDiazepam and (–)-pentobarbital: fluctuation analysis reveals different mechanisms for potentiation of gamma-aminobutyric acid responses in cultured central neuronsProc Natl Acad Sci U S A19817811718071846273918
- SieghartWSperkGSubunit composition, distribution and function of GABA-A receptor subtypesCurr Top Med Chem20022879581612171572
- RudolphUCrestaniFBenkeDBenzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypesNature1999401675579680010548105
- FritschyJMohlerHGABAA-receptor heterogeneity in the adult rat brain: differential regional and cellular distribution of seven major subunitsJ Comp Neurol199535911541948557845
- VinkersCOlivierBMechanisms underlying tolerance after long-term benzodiazepine use: a future for subtype-selective receptor modulators?Adv Pharmacol Sci20122012119
- WaffordKGABAA receptor subtypes: any clues to the mechanism of benzodiazepine dependence?Curr Opin Pharmacol200551475215661625
- HindmarchITrickLRidoutFA double-blind, placebo- and positive-internal-controlled (alprazolam) investigation of the cognitive and psychomotor profile of pregabalin in healthy volunteersPsychopharmacology2005183213314316205916
- McKernanRRosahlTReynoldsDSedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtypeNat Neurosci20003658759210816315
- KnablJWitschiRHöslKReversal of pathological pain through specific spinal GABAA receptor subtypesNature2008451717633033418202657
- AutaJKadriuBGiustiPCostaEGuidottiAAnticonvulsant, anxiolytic, and non-sedating actions of imidazenil and other imidazo-benzodiazepine carboxamide derivativesPharmacol Biochem Behav201095438338920227434
- AtackJTPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for α2- and α3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primatesJ Pharmacol Exp Ther2005316141042216183706
- HuangMRadadiaKMaconeBAuerbachSDattaSEffects of eszopi-clone and zolpidem on sleep–wake behavior, anxiety-like behavior and contextual memory in ratsBehav Brain Res20102101546620153782
- AtackJGABAA receptor subtype-selective efficacy: TPA023, an α2/α3 selective non-sedating anxiolytic and α5IA, an α5 selective cognition enhancerCNS Drug Rev20081412535
- ChengVMartinJErinMα5GABAA receptors mediate the amnestic but not sedative-hypnotic effects of the general anesthetic etomidateJ Neurosci200626143713372016597725
- RoehrsTMerlottiLZorickFRothTSedative, memory, and performance effects of hypnoticsPsychopharmacology199411621301347862941
- LöwKCrestaniFKeistRMolecular and neuronal substrate for the selective attenuation of anxietyScience2000290548913113411021797
- DiasREvidence for a significant role of α3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepinesJ Neurosci20052546106821068816291941
- AtackJHutsonPCollinsonNAnxiogenic properties of an inverse agonist selective for α3 subunit-containing GABAA receptorsBr J Clin Pharmacol20051443357366
- NavarroJBurónEMartín-LópezMAnxiolytic-like activity of SB-205384 in the elevated plus-maze test in micePsicothema200618110010417296016
- CrestaniFMöhlerHRudolphUAnxiolytic-like action of diazepam: mediated by GABAA receptors containing the α2-subunitTrends Pharmacol Sci2001228403
- ReynoldsDMcKernanRDawsonGAnxiolytic-like action of diazepam: which GABAA receptor subtype is involved?Trends Pharmacol Sci2001228402
- RudolphUCrestaniFMöhlerHGABAA receptor subtypes: dissecting their pharmacological functionsTrends Pharmacol Sci200122418819411282419
- TanKRudolphULüscherCHooked on benzodiazepines: GABAA receptor subtypes and addictionTrends Neurosci201134418819721353710
- RudolphUKnoflachFBeyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypesNat Rev Drug Discov201110968569721799515
- SamardzicJSvob StracDBenzodiazepines and anxiety disorders: from laboratory to clinicNew Developments in Anxiety DisordersCroatia, RijekaInTech2016
- MirzaNMunroGThe role of GABA(A) receptor subtypes as analgesic targetsDrug News Perspect201023635136020697602
- McEownKTreitDα2 GABAA receptor sub-units in the ventral hippocampus and α5 GABAA receptor sub-units in the dorsal hippocampus mediate anxiety and fear memoryNeuroscience201325216917723962649
- MorrisHDawsonGReynoldsDAtackJStephensDBoth α2 and α3 GABAA receptor subtypes mediate the anxiolytic properties of benzodiazepine site ligands in the conditioned emotional response paradigmEur J Neurosci20062392495250416706856
- BaileyDTetzlaffJCookJHeXHelmstetterFEffects of hippocampal injections of a novel ligand selective for the α5β2γ2 subunits of the GABA/benzodiazepine receptor on Pavlovian conditioningNeurobiol Learn Mem200278111012071663
- CrestaniFKeistRFritschyJTrace fear conditioning involves hippocampal α5 GABAA receptorsProc Natl Acad Sci U S A200299138980898512084936
- DawsonGMaubachKACollinsonNAn inverse agonist selective for α5 subunit-containing GABAA receptors enhances cognitionJ Pharmacol Exp Ther200531631335134516326923
- RudolphUCrestaniFBenkeDBenzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypesNature1999401675579680010548105
- KadriuBGuidottiACostaEAutaJImidazenil, a non-sedating anticonvulsant benzodiazepine, is more potent than diazepam in protecting against DFP-induced seizures and neuronal damageToxicology2009256316417419111886
- CrestaniFLöwKKeistRMandelliMMöhlerHRudolphUMolecular targets for the myorelaxant action of diazepamMol Pharmacol200159344244511179437
- MilićMDivljakovićJRallapalliSvan LinnMTimićTCookJSavićMThe role of α1 and α5 subunit-containing GABAA receptors in motor impairment induced by benzodiazepines in ratsBehav Pharmacol201223219119722327019
- LicataSPlattDCookJVan LinnMRowlettJContribution of α1 subunit-containing γ-aminobutyric acid A (GABAA) receptors to motor-impairing effects of benzodiazepines in squirrel monkeysPsychopharmacology2008203353954619031072
- AtackJWaffordKStreetLMRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humansJ Psychopharmacol201025331432820147571
- AtorNAtackJHargreavesRBurnsHDawsonGReducing abuse liability of GABAA/benzodiazepine ligands via selective partial agonist efficacy at α1 and α2/3 subtypesJ Pharmacol Exp Ther2009332141619789360
- RowlettJPlattDLelasSAtackJDawsonGDifferent GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primatesProc Natl Acad Sci U S A2005102391592015644443
- FischerBAtackJPlattDReynoldsDDawsonGRowlettJContribution of GABAA receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeysPsychopharmacology2010215231131921190016
- AtackJHalletDJTyeSPreclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonistJ Psychopharmacol201025332934420156926
- PiantadosiSFrenchBPoeMSex-dependent anti-stress effect of an α5 subunit containing GABAA receptor positive allosteric modulatorFront Pharmacol2016744627920723
- Boeuf-CazouOBongueBAnsiauDMarquiéJLapeyre-MestreMImpact of long-term benzodiazepine use on cognitive functioning in young adults: the VISAT cohortEur J Clin Pharmacol201167101045105221494764
- MoldofskyHLueFMouslyCRoth-SchechterBReynoldsWThe effect of zolpidem in patients with fibromyalgia: a dose ranging, double blind, placebo controlled, modified crossover studyJ Rheumatol19962335295338832997
- NickollsSMaceHFishRA comparison of the α2/3/5 selective positive allosteric modulators L-838,417 and TPA023 in preclinical models of inflammatory and neuropathic painAdv Pharmacol Sci20112011112
- HeikkinenAMöykkynenTKorpiELong-lasting modulation of glutamatergic transmission in VTA dopamine neurons after a single dose of benzodiazepine agonistsNeuropsychopharmacology200934229029818563060
- CrestaniFMartinJMöhlerHRudolphUMechanism of action of the hypnotic zolpidem in vivoBr J Clin Pharmacol2000131712511254
- StephensDPistovcakovaJWorthingLAtackJDawsonGRole of GABAA α5-containing receptors in ethanol reward: the effects of targeted gene deletion, and a selective inverse agonistEur J Pharmacol20055261–324025016253225
- TanKBrownMLabouèbeGNeural bases for addictive properties of benzodiazepinesNature2010463728276977420148031
- EnginEBakhurinKSmithKNeural Basis of Benzodiazepine Reward: Requirement for α2 Containing GABAA Receptors in the Nucleus AccumbensNeuropsychopharmacology201239818051815
- ShindayNSawyerEFischerBReinforcing effects of compounds lacking intrinsic efficacy at α1 subunit-containing GABAA receptor subtypes in midazolam- but not cocaine-experienced rhesus monkeysNeuropsychopharmacology20123861006101423303046
- LaliveARudolphULüscherCTanKIs there a way to curb benzodiazepine addiction?Swiss Med Wkly2011141w1327722012428
- BustoUKaplanHZawertailoLSellersEPharmacologic effects and abuse liability of bretazenil, diazepam, and alprazolam in humansClin Pharmacol Ther19945544514638162672
- VashchinkinaEPanhelainenAVekovischevaOGABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboonsJ Neurosci201232155310532022496576
- HarveySFosterKMcKayPThe GABAA receptor α1 subtype in the ventral pallidum regulates alcohol-seeking behaviorsJ Neurosci20022293765377511978852
- KaminskiBVan LinnMCookJYinWWeertsEEffects of the benzodiazepine GABAA α1-preferring ligand, 3-propoxy-β-carboline hydrochloride (3-PBC), on alcohol seeking and self-administration in baboonsPsychopharmacology2012227112713623271191
- EilerWJuneHBlockade of GABAA receptors within the extended amygdala attenuates D2 regulation of alcohol-motivated behaviors in the ventral tegmental area of alcohol-preferring (P) ratsNeuropharmacology20075281570157917451754
- CooperSJBenzodiazepine–opiate antagonist interactions and reward processes: implications for drug dependencyNeuropharmacology19832245355386134251
- SolhiHMostafazadehBRezaKVHRezaGAShooshtarizadehABenefit effect of naloxone in benzodiazepines intoxication: findings of a preliminary studyHum Exp Toxicol201030753554020573655
- KangWStevenWMarleneWOverexpression of proenkephalin in the amygdala potentiates the anxiolytic effects of benzodiazepinesNeuropsychopharmacology2000221778810633493
- ConnollyJBoulterJHeinemannSα4-β2 and other nicotinic acetylcholine receptor subtypes as targets of psychoactive and addictive drugsBr J Clin Pharmacol19921053657666
- SherTChenYSharplesTJPhysiological roles of neuronal nicotinic receptors subtypes: new insights on the nicotinic modulation of neurotransmitter release, synaptic transmission and plasticityCurr Top Med Chem200343283297
- BuissonBBertrandDNicotine addiction: the possible role of functional upregulationTrends Pharmacol Sci200223313013611879680
- WilliamsMAdinoffBThe role of acetylcholine in cocaine addictionNeuropsychopharmacology20073381779179717928814
- RadaPHoebelBAcetylcholine in the accumbens is decreased by diazepam and increased by benzodiazepine withdrawal: a possible mechanism for dependencyEur J Pharmacol20055081–313113815680263
- DazziLMotzoCMairaGSannaASerraMBiggioGEnhancement of acetylcholine release by flumazenil in the hippocampus of rats chronically treated with diazepam but not with imidazenil or abecarnilPsychopharmacology199512121801858545523
- PeturssonHLaderMBenzodiazepine dependenceAddiction1981762133145
- TietzERosenbergHChiuTAutoradiographic localization of benzodiazepine receptor downregulationJ Pharmacol Exp Ther198623612842923001290
- GallagerDLakoskiJGonsalvesSRauchSChronic benzodiazepine treatment decreases postsynaptic GABA sensitivityNature1984308595474776322004
- ZhaoTChiuTRosenbergHReduced expression of gamma-aminobutyric acid type A/benzodiazepine receptor gamma 2 and alpha 5 subunit mRNAs in brain regions of flurazepam-treated ratsMol Pharmacol19944546576638183244
- PoisbeauPWilliamsSModyISilent GABAA synapses during flurazepam withdrawal are region-specific in the hippocampal formationJ Neurosci19971710346734759133372
- PesoldCCarunchoHImpagnatielloFTolerance to diazepam and changes in GABAA receptor subunit expression in rat neocortical areasNeuroscience19977924774879200730
- ArnotMDaviesMMartinIBatesonAGABAA receptor gene expression in rat cortex: differential effects of two chronic diazepam treatment regimesJ Neurosci Res200164661762511398186
- KalesAScharfMKalesJRebound insomnia: a new clinical syndromeScience1978201436010391041684426
- BrowneTPenryJBenzodiazepines in the treatment of epilepsy: a reviewEpilepsia19731432773104204764
- BatesonABasic pharmacologic mechanisms involved in benzodiazepine tolerance and withdrawalCurr Pharm Des20028152111812247
- SchweizerEMaintenance drug treatment of panic disorderArch Gen Psychiatry199350151608422222
- CowleyDBenzodiazepine sensitivity in panic disorder: effects of chronic alprazolam treatmentNeuropsychopharmacology19951221471577779243
- RijnsoeverVCRequirement of α5-GABAA receptors for the development of tolerance to the sedative action of diazepam in miceJ Neurosci200424306785679015282283
- HawkinsMPravicaMRadulovackiMChronic administration of diazepam downregulates adenosine receptors in the rat brainPharmacol Biochem Behav19883023033082845443
- HawkinsMPanWStefanovichPRadulovackiMDesensitization of adenosine A2 receptors in the striatum of the rat following chronic treatment with diazepamNeuropharmacology19882711113111402849727
- KaplanGCotreauMGreenblattDEffects of benzodiazepine administration on A1 adenosine receptor binding in-vivo and ex-vivoJ Pharm Pharmacol19924487007031359103
- NarimatsuEAokiMInvolvement of the adenosine neuromodulatory system in the benzodiazepine-induced depression of excitatory synaptic transmissions in rat hippocampal neurons in vitroNeurosci Res1999331576410096472
- NarimatsuENiiyaTKawamataMNamikiAThe mechanisms of depression by benzodiazepines, barbiturates and propofol of excitatory synaptic transmissions mediated by adenosine neuromodulationMasui2006556684691 Japanese16780077
- TsudaMChibaYSuzukiTMisawaMUpregulation of NMDA receptor subunit proteins in the cerebral cortex during diazepam withdrawalEur J Pharmacol19983412–3R1R29543260
- TsudaMShimizuNYajimaYSuzukiTMisawaMHypersusceptibility to DMCM-induced seizures during diazepam withdrawal in mice: evidence for upregulation of NMDA receptorsNaunyn Schmiedebergs Arch Pharmacol199835733093159550303
- BonavitaCFerreroACeresetoMVelardezMRubioMWikinskiSAdaptive changes in the rat hippocampal glutamatergic neurotrans-mission are observed during long-term treatment with lorazepamPsychopharmacology2003166216316712545333
- SongJShenGGreenfieldLTietzEBenzodiazepine withdrawal-induced glutamatergic plasticity involves up-regulation of GluR1-containing α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors in hippocampal CA1 neuronsJ Pharmacol Exp Ther2007322256958117510319
- FileSFernandesCDizocilpine prevents the development of tolerance to the sedative effects of diazepam in ratsPharmacol Biochem Behav19944748238268029250
- KoffJPritchardGGreenblattDMillerLThe NMDA receptor competitive antagonist CPP modulates benzodiazepine tolerance and discontinuationPharmacology19975552172279399331
- FernandesCFileSDizocilpine does not prevent the development of tolerance to the anxiolytic effects of diazepam in ratsBrain Res199981524314349878864
- SteppuhnKTurskiLDiazepam dependence prevented by glutamate antagonistsProc Natl Acad Sci U S A19939014688968938341715
- JacobTMichelsGSilayevaLHaydonJSuccolFMossSBenzodiazepine treatment induces subtype-specific changes in GABAA receptor trafficking and decreases synaptic inhibitionProc Natl Acad Sci U S A201210945185951860023091016
- HernandezTHeningerCWilsonMGallagerDRelationship of agonist efficacy to changes in GABA sensitivity and anticonvulsant tolerance following chronic benzodiazepine ligand exposureEur J Pharmacol198917031451552515976
- GonsalvesSGallagerDPersistent reversal of tolerance to anticonvulsant effects and GABAergic subsensitivity by a single exposure to benzodiazepine antagonist during chronic benzodiazepine administrationJ Pharmacol Exp Ther1988244179833121850
- KleinRMasciaMHarknessPHadinghamKWhitingPHarrisRRegulation of allosteric coupling and function of stably expressed gamma-aminobutyric acid (GABA)A receptors by chronic treatment with GABAA and benzodiazepine agonistsJ Pharmacol Exp Ther19952743148414927562525
- MillerLHellerJLumpkinMWeillCGreenblattDShaderRAugmentation of GABAA receptor function by chronic exposure to GABA-neutral and GABA-negative benzodiazepine ligands in cultured cortical neuronsBiochem Pharmacol1990406133713442169744
- LugoboniFLeoneRWhat is stopping us from using flumazenil?Addiction20121077135922509854
- SavicIFeasibility of reversing benzodiazepine tolerance with flumazenilLancet199133787341331371670787
- TietzEChiuTRosenbergHRegional GABA/benzodiazepine receptor/chloride channel coupling after acute and chronic benzodiazepine treatmentEur J Pharmacol1989167157652476326
- GutiérrezMFerreriMGravielleMGABA-induced uncoupling of GABA/benzodiazepine site interactions is mediated by increased GABAA receptor internalization and associated with a change in subunit compositionNeuroscience201425711912924215979
- TehraniMBarnesEAgonist-dependent internalization of gamma-aminobutyric acid A/benzodiazepine receptors in chick cortical neuronsJ Neurochem1991574130713121654391
- TehraniMBarnesEIdentification of GABAA/benzodiazepine receptors on clathrin-coated vesicles from rat brainJ Neurochem1993605175517618386222
- TehraniMBarnesESequestration of γ-aminobutyric acid A receptors on clathrin-coated vesicles during chronic benzodiazepine administration in vivoJ Pharmacol Exp Ther199728313843909336347
- TehraniMBaumgartnerBBarnesEClathrin-coated vesicles from bovine brain contain uncoupled GABAA receptorsBrain Res1997761–2195203
- GravielleMActivation-induced regulation of GABAA receptors: is there a link with the molecular basis of benzodiazepine tolerance?Pharmacol Res20161099210026733466
- LillySZengXTietzERole of protein kinase A in GABAA receptor dysfunction in CA1 pyramidal cells following chronic benzodiazepine treatmentJ Neurochem200385498899812716430
- AliNOlsenRChronic benzodiazepine treatment of cells expressing recombinant GABAA receptors uncouples allosteric binding: studies on possible mechanismsJ Neurochem200879511001108
- HuopaniemiLKeistRRandolphACertaURudolphUDiazepam-induced adaptive plasticity revealed by α1 GABAA receptor-specific expression profilingJ Neurochem20048851059106715009662
- AutaJImpagnatielloFKadriuBGuidottiACostaEImidazenil: a low efficacy agonist at α1- but high efficacy at α5-GABAA receptors fail to show anticonvulsant cross tolerance to diazepam or zolpidemNeuropharmacology200855214815318555494
- ZanottiAMariotRContarinoALipartitiMGiustiPLack of anticonvulsant tolerance and benzodiazepine receptor down regulation with imidazenil in ratsBr J Clin Pharmacol19961174647652
- GhianiCSerraMMotzoCChronic administration of an anti-convulsant dose of imidazenil fails to induce tolerance of GABAA receptor function in miceEur J Pharmacol199425432993028013567
- KadriuBGocelJLarsonJAbsence of tolerance to the anticonvulsant and neuroprotective effects of imidazenil against DFP-induced seizure and neuronal damageNeuropharmacology20116181463146921903116
- AutaJGuidottiACostaEImidazenil prevention of alprazolam-induced acquisition deficit in patas monkeys is devoid of toleranceProc Natl Acad Sci U S A20009752314231910696114
- VinkersCvan OorschotRNielsenEGABAA receptor α subunits differentially contribute to diazepam tolerance after chronic treatmentPLoS One201278e4305422912786
- RundfeldtCWlaźPHönackDLöscherWAnticonvulsant tolerance and withdrawal characteristics of benzodiazepine receptor ligands in different seizure models in mice. Comparison of diazepam, bretazenil and abecarnilJ Pharmacol Exp Ther199527526937027473156
- SannaEBusoneroFTalaniGLow tolerance and dependence liabilities of etizolam: molecular, functional, and pharmacological correlatesEur J Pharmacol20055191–2314216107249
- O’ConnellCSadlerCToliaVLyBSaitmanAFitzgeraldROverdose of etizolam: the abuse and rise of a benzodiazepine analogAnn Emerg Med201565446546625805032