2022
Emraclidine, a novel positive allosteric modulator of cholinergic M4 receptors, for the treatment of schizophrenia: a two-part, randomised, double-blind, placebo-controlled, phase 1b trial
Krystal J, Kane J, Correll C, Walling D, Leoni M, Duvvuri S, Patel S, Chang I, Iredale P, Frohlich L, Versavel S, Perry P, Sanchez R, Renger J. Emraclidine, a novel positive allosteric modulator of cholinergic M4 receptors, for the treatment of schizophrenia: a two-part, randomised, double-blind, placebo-controlled, phase 1b trial. The Lancet 2022, 400: 2210-2220. PMID: 36528376, DOI: 10.1016/s0140-6736(22)01990-0.Peer-Reviewed Original ResearchConceptsTreatment of schizophreniaPositive allosteric modulatorsAdverse eventsUS sitesAllosteric modulatorsFavorable side effect profileMini International Neuropsychiatric InterviewNovel positive allosteric modulatorReceptor positive allosteric modulatorExtrapyramidal symptom assessmentMultiple ascending dosesCommon adverse eventsPhase 1b trialPlacebo-controlled studySide effect profileInternational Neuropsychiatric InterviewCohort of participantsAscending dosesSafety populationPrimary endpointBlood pressureM4 receptorsTreatment initiationDaily treatmentOral doses
2010
Potential Psychiatric Applications of Metabotropic Glutamate Receptor Agonists and Antagonists
Krystal JH, Mathew SJ, D’Souza D, Garakani A, Gunduz-Bruce H, Charney DS. Potential Psychiatric Applications of Metabotropic Glutamate Receptor Agonists and Antagonists. CNS Drugs 2010, 24: 669-693. PMID: 20658799, DOI: 10.2165/11533230-000000000-00000.Peer-Reviewed Reviews, Practice Guidelines, Standards, and Consensus StatementsConceptsPreliminary clinical trialsPositive allosteric modulatorsPsychiatric disordersClinical trialsAnimal modelsAllosteric modulatorsGroup II mGluR agonistGroup IMetabotropic glutamate receptor agonistAnxiety disordersPotential psychiatric applicationsGlutamate receptor agonistsMetabotropic glutamate receptorsTreatment of schizophreniaRole of glutamateForm of depressionMGluR agonistAntidepressant propertiesMGluR5 agonistReceptor agonistGlutamate receptorsMood disordersArea of schizophreniaPromising agentAgonists