Effects of the Fyn kinase inhibitor saracatinib on ventral striatal activity during performance of an fMRI monetary incentive delay task in individuals family history positive or negative for alcohol use disorder. A pilot randomised trial
Patel KT, Stevens MC, Dunlap A, Gallagher A, O’Malley S, DeMartini K, Potenza MN, Krystal JH, Pearlson GD. Effects of the Fyn kinase inhibitor saracatinib on ventral striatal activity during performance of an fMRI monetary incentive delay task in individuals family history positive or negative for alcohol use disorder. A pilot randomised trial. Neuropsychopharmacology 2021, 47: 840-846. PMID: 34475522, PMCID: PMC8882177, DOI: 10.1038/s41386-021-01157-5.Peer-Reviewed Original ResearchConceptsProtein tyrosine kinasesSrc regulationSrc familyProtein kinaseTyrosine kinaseFyn kinaseSrc inhibitorSrc/FynDependent pathwayKinaseNMDAR upregulationNMDAR functionNMDA receptorsRegulationSaracatinibGluN2B subunitGlutamate receptorsFynInhibitorsReceptorsSubunitsN-methyl-D-aspartate (NMDA) glutamate receptorsPrevious evidenceSaracatinib Fails to Reduce Alcohol-Seeking and Consumption in Mice and Human Participants
Thompson SL, Gianessi CA, O'Malley SS, Cavallo DA, Shi JM, Tetrault JM, DeMartini KS, Gueorguieva R, Pittman B, Krystal JH, Taylor JR, Krishnan-Sarin S. Saracatinib Fails to Reduce Alcohol-Seeking and Consumption in Mice and Human Participants. Frontiers In Psychiatry 2021, 12: 709559. PMID: 34531767, PMCID: PMC8438169, DOI: 10.3389/fpsyt.2021.709559.Peer-Reviewed Original ResearchNMDA receptorsSrc/FynAlcohol consumptionEffect of saracatinibVehicle 2 hChronic alcohol useDays of treatmentDSM-IV criteriaMore effective treatmentsNumber of drinksGlutamatergic systemAdditional drinkAlcohol drinkingAdditional dosesEthanol exposureEffective treatmentNR2B subunitAlcohol abuseHuman studiesPriming drinkAlcohol cravingSaracatinibDrinking paradigmNovel pharmacotherapeuticsHuman participants