2015
Role of GABA Deficit in Sensitivity to the Psychotomimetic Effects of Amphetamine
Ahn KH, Sewell A, Elander J, Pittman B, Ranganathan M, Gunduz-Bruce H, Krystal J, D'Souza DC. Role of GABA Deficit in Sensitivity to the Psychotomimetic Effects of Amphetamine. Neuropsychopharmacology 2015, 40: 2822-2831. PMID: 25953357, PMCID: PMC4864658, DOI: 10.1038/npp.2015.132.Peer-Reviewed Original ResearchConceptsGABA deficitHealthy subjectsPsychotomimetic effectsIntravenous infusionSchizophrenia patientsPANSS positive symptoms subscaleDouble-blind crossover designStriatal dopamine releasePositive symptom subscaleAdministration of drugsDose of AMPHPartial inverse agonistSubclinical responsePharmacokinetic interactionsSubthreshold doseDopamine releaseBenzodiazepine receptorsSymptom subscalesCrossover designCADSS scoresPositive symptomsAMPHInverse agonistSubjective effectsTest day
2012
Sex‐specific differences in GABAA‐benzodiazepine receptor availability: relationship with sensitivity to pain and tobacco smoking craving
Esterlis I, McKee SA, Kirk K, Lee D, Bois F, Stiklus SM, Seibyl JP, Krishnan‐Sarin S, O'Malley SS, Staley JK, Cosgrove KP. Sex‐specific differences in GABAA‐benzodiazepine receptor availability: relationship with sensitivity to pain and tobacco smoking craving. Addiction Biology 2012, 18: 370-378. PMID: 22353491, PMCID: PMC3378766, DOI: 10.1111/j.1369-1600.2011.00403.x.Peer-Reviewed Original ResearchMeSH KeywordsAdultAffective SymptomsAnalysis of VarianceAnimalsBrainFemaleFlumazenilGABA ModulatorsHumansMaleMiddle AgedNicotinePain PerceptionReceptors, GABA-ASex CharacteristicsSmoking CessationSubstance Withdrawal SyndromeTobacco Use DisorderTomography, Emission-Computed, Single-PhotonYoung AdultConceptsMale smokersFemale smokersPain sensitivitySmoking interactionSmoking cravingBrain GABA levelsTobacco smoking behaviorSingle photon emissionPain symptomsLast cigaretteSmoking cessationGABA levelsSex-specific differencesTobacco smokeCigarette cravingNicotine dependenceBenzodiazepine receptorsSmokersSmoking behaviorReceptor availabilityBrain regionsCravingSex-specific regulationSignificant differencesSex differences
2011
A phase II study of the Ras-MAPK signaling pathway inhibitor TLN-4601 in patients with glioblastoma at first progression
Mason WP, Belanger K, Nicholas G, Vallières I, Mathieu D, Kavan P, Desjardins A, Omuro A, Reymond D. A phase II study of the Ras-MAPK signaling pathway inhibitor TLN-4601 in patients with glioblastoma at first progression. Journal Of Neuro-Oncology 2011, 107: 343-349. PMID: 22048878, DOI: 10.1007/s11060-011-0747-6.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedAntineoplastic AgentsBrain NeoplasmsChromatography, LiquidDibenzazepinesErbB ReceptorsFemaleFollow-Up StudiesGene Expression Regulation, NeoplasticGlioblastomaHumansInfusions, IntraventricularKaplan-Meier EstimateMagnetic Resonance ImagingMaleMiddle AgedPTEN PhosphohydrolaseTandem Mass SpectrometryConceptsPharmacokinetic evaluationProgressive glioblastomaFirst progressionM2/dayPhase II studyMR scansPhase II trialContinuous intravenous administrationBlood-brain barrierLack of efficacyPeripheral benzodiazepine receptorEvaluable patientsStable diseaseII trialRadiographic progressionAdverse eventsII studyRecurrent glioblastomaDisease progressionDrug levelsIntravenous administrationBiomarker assessmentPatientsAnimal modelsBenzodiazepine receptorsErythrocyte peripheral type benzodiazepine receptor/voltage-dependent anion channels are upregulated by Plasmodium falciparum
Bouyer G, Cueff A, Egée S, Kmiecik J, Maksimova Y, Glogowska E, Gallagher PG, Thomas SL. Erythrocyte peripheral type benzodiazepine receptor/voltage-dependent anion channels are upregulated by Plasmodium falciparum. Blood 2011, 118: 2305-2312. PMID: 21795748, DOI: 10.1182/blood-2011-01-329300.Peer-Reviewed Original ResearchConceptsPeripheral-type benzodiazepine receptorBenzodiazepine receptorsNew permeability pathwaysP falciparumPlasmodium falciparumFalciparum-infected erythrocytesAnti-malarial therapyP falciparum-infected erythrocytesErythrocyte membranesInfected erythrocytesAnion channelIntraerythrocytic growthFalciparumReceptorsSelective inhibitionEndogenous channelsVoltage-dependent anion channelPharmacologic applicationsPermeability pathwaysErythrocytesMolecular identityObvious targetTherapyNeuroimaging insights into the role of cortical GABA systems and the influence of nicotine on the recovery from alcohol dependence
Cosgrove KP, Esterlis I, Mason GF, Bois F, O’Malley S, Krystal JH. Neuroimaging insights into the role of cortical GABA systems and the influence of nicotine on the recovery from alcohol dependence. Neuropharmacology 2011, 60: 1318-1325. PMID: 21276806, PMCID: PMC3078950, DOI: 10.1016/j.neuropharm.2011.01.020.Peer-Reviewed Original ResearchConceptsAlcohol withdrawalTobacco smokingGABA levelsNeuronal functionNeuronal nicotinic acetylcholine receptorsAlcohol-dependent smokersCortical GABA systemGABA neuronal functionProlonged alcohol withdrawalInfluence of nicotineNicotinic acetylcholine receptorsAlcohol-dependent individualsEffects of alcoholPreclinical evidenceRole of alcoholGABA systemPreclinical modelsTobacco smokeErminio CostaBenzodiazepine receptorsAcetylcholine receptorsAlcohol dependenceSmokingPrimary actionClinical experiments
2010
Probing GABA Receptor Function in Schizophrenia with Iomazenil
Ahn K, Gil R, Seibyl J, Sewell RA, D'Souza DC. Probing GABA Receptor Function in Schizophrenia with Iomazenil. Neuropsychopharmacology 2010, 36: 677-683. PMID: 21068719, PMCID: PMC3055690, DOI: 10.1038/npp.2010.198.Peer-Reviewed Original ResearchConceptsSchizophrenia patientsHealthy controlsGABA deficitHealthy subjectsBrief Psychiatric Rating ScaleGABA-deficit hypothesisPlacebo-controlled studyChronic schizophrenia patientsPathophysiology of schizophreniaPsychiatric Rating ScalePartial inverse agonistDissociative Symptoms ScaleGABA receptor functionPerceptual alterationsPsychotomimetic effectsPsychotic symptomsIomazenilBenzodiazepine receptorsPatientsSymptom ScalePharmacological inductionReceptor functionInverse agonistRating ScaleBrain imaging
2008
A ligand to the mitochondrial benzodiazepine receptor prevents ventricular arrhythmias and LV dysfunction after ischemia or glutathione depletion
Brown D, Aon M, Akar F, O’Rourke B. A ligand to the mitochondrial benzodiazepine receptor prevents ventricular arrhythmias and LV dysfunction after ischemia or glutathione depletion. The FASEB Journal 2008, 22: 747.7-747.7. DOI: 10.1096/fasebj.22.1_supplement.747.7.Peer-Reviewed Original ResearchContractile dysfunctionBenzodiazepine receptorsGlobal ischemia/reperfusionOxidative stressMitochondrial benzodiazepine receptorIschemia/reperfusionGuinea pig heartsSignificant clinical implicationsAnti-oxidant defensesReduced arrhythmiasLV dysfunctionVentricular dysfunctionR injuryVentricular arrhythmiasInduced arrhythmiasNormoxic perfusionIsolated myocytesDysfunctionClinical implicationsArrhythmiasIntact heartMetabolic challengesPig heartsGlutathione depletionMitochondrial membrane potential
2005
The mitochondrial origin of postischemic arrhythmias
Akar FG, Aon MA, Tomaselli GF, O'Rourke B. The mitochondrial origin of postischemic arrhythmias. Journal Of Clinical Investigation 2005, 115: 3527-3535. PMID: 16284648, PMCID: PMC1280968, DOI: 10.1172/jci25371.Peer-Reviewed Original ResearchMeSH KeywordsAction PotentialsAnimalsAnionsArrhythmias, CardiacDose-Response Relationship, DrugElectrophysiologyGuinea PigsHeartIntracellular MembranesIon ChannelsIschemiaMembrane PotentialsMicroscopy, ConfocalMitochondria, HeartMyocardial IschemiaMyocardial ReperfusionMyocardial Reperfusion InjuryMyocardiumMyocytes, CardiacOscillometryReactive Oxygen SpeciesReceptors, GABA-AReperfusion InjuryTemperatureTime FactorsConceptsAction potentialsVentricular fibrillationPostischemic functional recoveryIschemic heart diseaseGuinea pig heartsNew therapeutic targetsAbnormal electrical activationPostischemic arrhythmiasReperfusion arrhythmiasFunctional recoveryGlobal ischemiaHeart diseaseBolus infusionArrhythmia preventionElectrophysiological changesAP shorteningControl heartsPostischemic heartsBenzodiazepine receptorsElectrophysiological substrateTherapeutic targetArrhythmiasReperfusionPig heartsMitochondrial benzodiazepine receptorCortical γ-Aminobutyric Acid Type A–Benzodiazepine Receptors in Recovery From Alcohol Dependence: Relationship to Features of Alcohol Dependence and Cigarette Smoking
Staley JK, Gottschalk C, Petrakis IL, Gueorguieva R, O’Malley S, Baldwin R, Jatlow P, Verhoeff NP, Perry E, Weinzimmer D, Frohlich E, Ruff E, van Dyck CH, Seibyl JP, Innis RB, Krystal JH. Cortical γ-Aminobutyric Acid Type A–Benzodiazepine Receptors in Recovery From Alcohol Dependence: Relationship to Features of Alcohol Dependence and Cigarette Smoking. JAMA Psychiatry 2005, 62: 877-888. PMID: 16061765, DOI: 10.1001/archpsyc.62.8.877.Peer-Reviewed Original ResearchConceptsWeeks of abstinenceIomazenil single-photon emissionSingle photon emissionDays of sobrietyAlcohol dependenceIomazenil uptakeTomographic scanBenzodiazepine receptorsVoxel-based statistical parametric mappingReceptor adaptationDistribution volumeReceptor functionGamma-aminobutyric acid type ABenzodiazepine receptor levelsIodine I 123Reduced receptor functionHuman alcohol dependenceLast alcoholic drinkHealthy comparison groupStatistical parametric mappingAlcohol withdrawalClinical featuresSmoking statusCigarette smokingAcute withdrawal
2003
The proapoptotic benzodiazepine Bz-423 affects the growth and survival of malignant B cells.
Boitano A, Ellman JA, Glick GD, Opipari AW. The proapoptotic benzodiazepine Bz-423 affects the growth and survival of malignant B cells. Cancer Research 2003, 63: 6870-6. PMID: 14583485.Peer-Reviewed Original ResearchConceptsB cell linesSystemic lupus erythematosusMalignant B-cell linesMalignant B cellsPeripheral benzodiazepine receptorReactive oxygen species levelsEBV statusLupus erythematosusLymphoproliferative diseaseAntineoplastic therapyOxygen species levelsBurkitt's lymphomaAnimal modelsBenzodiazepine receptorsClinical developmentB cellsPotent antiproliferative agentBz-423Phase arrestBcl-2Expression levelsLymphomaAntiproliferative agentsCell deathDisease
2000
Decreased Benzodiazepine Receptor Binding in Prefrontal Cortex in Combat-Related Posttraumatic Stress Disorder
Bremner J, Innis R, Southwick S, Staib L, Zoghbi S, Charney D. Decreased Benzodiazepine Receptor Binding in Prefrontal Cortex in Combat-Related Posttraumatic Stress Disorder. American Journal Of Psychiatry 2000, 157: 1120-1126. PMID: 10873921, DOI: 10.1176/appi.ajp.157.7.1120.Peer-Reviewed Original ResearchConceptsBenzodiazepine receptor bindingPosttraumatic stress disorderBenzodiazepine receptorsReceptor bindingPrefrontal cortexComparison subjectsCase-matched healthy comparison subjectsDistribution volumeStress disorderSymptoms of PTSDBenzodiazepine receptor functionLow distribution volumeHealthy comparison subjectsCombat-related posttraumatic stress disorderMedial prefrontal cortexCentral benzodiazepine receptorsSingle photon emissionStatistical parametric mappingFrontal cortexPTSD patientsPatientsReceptor functionCortexTomography imagingParametric mappingSPECT [I-123]iomazenil measurement of the benzodiazepine receptor in panic disorder
Bremner J, Innis R, White T, Fujita M, Silbersweig D, Goddard A, Staib L, Stern E, Cappiello A, Woods S, Baldwin R, Charney D. SPECT [I-123]iomazenil measurement of the benzodiazepine receptor in panic disorder. Biological Psychiatry 2000, 47: 96-106. PMID: 10664825, DOI: 10.1016/s0006-3223(99)00188-2.Peer-Reviewed Original ResearchConceptsBenzodiazepine receptor bindingBenzodiazepine receptor functionPanic disorder patientsBenzodiazepine receptorsPanic disorderReceptor bindingDisorder patientsPanic attacksReceptor functionPrefrontal cortexSingle photon emissionStatistical parametric mappingGABAergic transmissionHealthy controlsFrontal cortexLeft hippocampusAnimal modelsComparison subjectsPatientsChronic stressPanic anxietyTomography imagingParametric mappingCortexSpecific decrease
1999
Kinetic modeling of benzodiazepine receptor binding with PET and high specific activity [11C]Iomazenil in healthy human subjects
Bremner J, Horti A, Staib L, Zea‐Ponce Y, Soufer R, Charney D, Baldwin R. Kinetic modeling of benzodiazepine receptor binding with PET and high specific activity [11C]Iomazenil in healthy human subjects. Synapse 1999, 35: 68-77. PMID: 10579810, DOI: 10.1002/(sici)1098-2396(200001)35:1<68::aid-syn9>3.0.co;2-h.Peer-Reviewed Original ResearchConceptsBenzodiazepine receptor bindingHealthy human subjectsReceptor bindingBenzodiazepine receptorsHuman subjectsBenzodiazepine receptor antagonistCompartment modelReceptor antagonistMultiple time pointsBolus injectionArterial samplesTime-activity curvesSPECT radioligandBrain tissueBrain tissue compartmentsPET imagingTime pointsPrior reportsRadioligandParent compoundTissue compartmentsRadioligand concentrationHigh specific activityWiley-LissReceptorsQuantitation of benzodiazepine receptor binding with PET [11C]iomazenil and SPECT [123I]iomazenil: preliminary results of a direct comparison in healthy human subjects
Bremner J, Baldwin R, Horti A, Staib L, Ng C, Tan P, Zea-Ponce Y, Zoghbi S, Seibyl J, Soufer R, Charney D, Innis R. Quantitation of benzodiazepine receptor binding with PET [11C]iomazenil and SPECT [123I]iomazenil: preliminary results of a direct comparison in healthy human subjects. Psychiatry Research 1999, 91: 79-91. PMID: 10515463, DOI: 10.1016/s0925-4927(99)00015-3.Peer-Reviewed Original ResearchConceptsPositron emission tomographyBenzodiazepine receptorsArterial blood samplesBenzodiazepine receptor bindingHealthy human subjectsHuman subjectsNeuroreceptor bindingSingle photon emissionSingle bolusOccipital cortexBlood samplesTemporal cortexEmission tomographyBrain compartmentsDynamic positron emission tomographyReceptor bindingSPECTSame human subjectsPhoton emissionCortexHuman brainRadioligandPreliminary findingsBrainReceptorsChanges of benzodiazepine receptors during chronic benzodiazepine administration in humans
Fujita M, Woods S, Verhoeff N, Abi-Dargham A, Baldwin R, Zoghbi S, Soares J, Jatlow P, Krystal J, Rajeevan N, Charney D, Seibyl J, Innis R. Changes of benzodiazepine receptors during chronic benzodiazepine administration in humans. European Journal Of Pharmacology 1999, 368: 161-172. PMID: 10193652, DOI: 10.1016/s0014-2999(99)00013-8.Peer-Reviewed Original ResearchConceptsClinical effectsReceptor levelsReceptor densityReceptor occupancyChronic benzodiazepine administrationBenzodiazepine receptor densityHealthy human subjectsComparison of baselineSingle photon emissionHopkins Verbal Learning TestInduced sedationVerbal Learning TestBenzodiazepine administrationOral administrationBaseline valuesBenzodiazepine receptorsTolerance developmentDay 3Day 17Day 4Day 10Central typeLearning TestReceptorsHuman subjects
1998
Alterations of Benzodiazepine Receptors in Type II Alcoholic Subjects Measured With SPECT and 123IIomazenil
Abi-Dargham A, Krystal JH, Anjilvel S, Scanley BE, Zoghbi S, Baldwin RM, Rajeevan N, Ellis S, Petrakis IL, Seibyl JP, Charney DS, Laruelle M, Innis RB. Alterations of Benzodiazepine Receptors in Type II Alcoholic Subjects Measured With SPECT and 123IIomazenil. American Journal Of Psychiatry 1998, 155: 1550-1555. PMID: 9812116, DOI: 10.1176/ajp.155.11.1550.Peer-Reviewed Original ResearchConceptsHealthy comparison subjectsBenzodiazepine receptorsComparison subjectsAlcoholic subjectsDistribution volumeAlcoholic patientsAnterior cingulateBenzodiazepine receptor densityRight middle frontal gyrusLeft occipital cortexType II alcoholismSingle photon emissionMiddle frontal gyrusStatistical parametric mappingContinuous infusionReceptor radiotracerReceptor densityOccipital cortexCerebellar cortexCortical regionsPatientsFrontal gyrusInterest analysisVivo studiesParametric mapping
1997
Benzodiazepine Receptor Antagonists
Abi-Dargham A, Charney D, Krystal J. Benzodiazepine Receptor Antagonists. CNS Drugs 1997, 8: 244-256. DOI: 10.2165/00023210-199708030-00007.Peer-Reviewed Original ResearchBenzodiazepine receptorsIdiopathic recurrent stuporBenzodiazepine receptor antagonistPotential therapeutic benefitBenzodiazepine toleranceCerebral ischaemiaGABAergic systemΓ-aminobutyric acidReceptor antagonistMovement disordersNeuronal markersSleep disordersTherapeutic benefitCognitive disordersPotential treatmentNeuropsychiatric illnessOnly agentInverse agonistFlumazenilPharmacological investigationsAdverse effectsReceptorsDisordersImaging agentEpilepsy
1995
Synthesis and PET imaging of the benzodiazepine receptor tracer [N-methyl-11C]iomazenil
Baldwin R, Horti A, Bremner J, Stratton M, Dannals R, Ravert H, Zea-Ponce Y, Ng C, Dey H, Soufer R, Charney D, Mazza S, Sparks R, Stubbs J, Innis R. Synthesis and PET imaging of the benzodiazepine receptor tracer [N-methyl-11C]iomazenil. Nuclear Medicine And Biology 1995, 22: 659-665. PMID: 7581177, DOI: 10.1016/0969-8051(94)00139-b.Peer-Reviewed Original ResearchConceptsHuman biodistribution dataUrinary bladder wallReceptor tracerHealthy human volunteersPositron emission tomographyBladder wallHigh doseBenzodiazepine receptorsTime-activity curvesUseful agentSPECT studiesEmission tomographyHuman volunteersBiodistribution dataAdult baboonsMCi/mumolPET imagingRadiation dosesN-methylEffective dose equivalentInjectionPurity 99MinCortexDose
1991
Anxiogenic β-carboline FG 7142 produces activation of noradrenergic neurons in specific brain regions of rats
Ida Y, Elsworth J, Roth R. Anxiogenic β-carboline FG 7142 produces activation of noradrenergic neurons in specific brain regions of rats. Pharmacology Biochemistry And Behavior 1991, 39: 791-793. PMID: 1784607, DOI: 10.1016/0091-3057(91)90166-y.Peer-Reviewed Original ResearchConceptsBrain noradrenergic activityFG 7142Specific brain regionsCerebral cortexNoradrenergic activityΒ-carboline FG 7142Brain regionsBeta-carboline FG 7142Rat brain noradrenalineBrain noradrenergic systemAntagonist Ro 15Brain noradrenalineAgonist clonidineNoradrenergic neuronsBZD receptorsMHPG levelsRo 15Sixty minNoradrenergic systemSame doseBenzodiazepine receptorsInverse agonistDihydroxyphenylglycolMajor metaboliteMetabolite levels
1990
Regionally specific alterations in the low-affinity GABAA receptor following perinatal exposure to diazepam
Gruen R, Elsworth J, Roth R. Regionally specific alterations in the low-affinity GABAA receptor following perinatal exposure to diazepam. Brain Research 1990, 514: 151-154. PMID: 2162709, DOI: 10.1016/0006-8993(90)90449-l.Peer-Reviewed Original ResearchConceptsLow-affinity GABAA receptorsPerinatal exposureGABAA receptorsAbility of GABAPerinatal periodAdult ratsBenzodiazepine receptorsCingulate cortexLow affinity formDiazepamSpecific alterationsSignificant decreaseReceptorsSignificant reductionExposureAffinity formAlterationsHypothalamusGABARatsCortex
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