Search results for "Target engagement"

showing 2 items of 2 documents

Positron emission tomography in CNS drug discovery and drug monitoring.

2014

Molecular imaging methods such as positron emission tomography (PET) are increasingly involved in the development of new drugs. Using radioactive tracers as imaging probes, PET allows the determination of the pharmacokinetic and pharmacodynamic properties of a drug candidate, via recording target engagement, the pattern of distribution, and metabolism. Because of the noninvasive nature and quantitative end point obtainable by molecular imaging, it seems inherently suited for the examination of a pharmaceutical’s behavior in the brain. Molecular imaging, most especially PET, can therefore be a valuable tool in CNS drug research. In this Perspective, we present the basic principles of PET, th…

DrugCentral Nervous Systemmedia_common.quotation_subjectDopamineGlutamic AcidPharmacologyPermeabilityReceptors DopamineDrug DiscoverymedicineAnimalsHumansRadioactive Tracersmedia_commonEnd pointmedicine.diagnostic_testChemistryDrug discoveryDrug candidateTarget engagementBrainModels ChemicalPharmaceutical PreparationsPositron emission tomographyPositron-Emission TomographyReceptors SerotoninSchizophreniaMolecular MedicineMolecular imagingDrug MonitoringGlycolysisBiomedical engineeringCentral Nervous System AgentsJournal of medicinal chemistry
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Concurrent TMS-fMRI for causal network perturbation and proof of target engagement

2021

The experimental manipulation of neural activity by neurostimulation techniques overcomes the inherent limitations of correlative recordings, enabling the researcher to investigate causal brain-behavior relationships. But only when stimulation and recordings are combined, the direct impact of the stimulation on neural activity can be evaluated. In humans, this can be achieved non-invasively through the concurrent combination of transcranial magnetic stimulation (TMS) with functional magnetic resonance imaging (fMRI). Concurrent TMS-fMRI allows the assessment of the neurovascular responses evoked by TMS with excellent spatial resolution and full-brain coverage. This enables the functional ma…

Interleavedgenetic structuresComputer scienceCognitive Neurosciencemedicine.medical_treatmentNeurosciences. Biological psychiatry. NeuropsychiatryReviewbehavioral disciplines and activities050105 experimental psychologyTask (project management)03 medical and health sciencesNeural activity0302 clinical medicineTranscranial magnetic stimulation (TMS)medicineHumans0501 psychology and cognitive sciencesNeurostimulationTranscranial magnetic stimulation (TMS) ; Concurrent ; Simultaneous ; Functional magnetic resonance imaging (fMRI) ; Review ; InterleavedBrain MappingArtificial neural networkmedicine.diagnostic_test05 social sciencesTarget engagementMagnetic Resonance ImagingTranscranial Magnetic StimulationConcurrentTranscranial magnetic stimulationFunctional magnetic resonance imaging (fMRI)Functional mappingNeurologynervous systemNeurovascular CouplingNerve NetFunctional magnetic resonance imagingNeuroscienceSimultaneous030217 neurology & neurosurgerypsychological phenomena and processesRC321-571
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