2025
Perioperative management of patients taking glucagon-like peptide 1 receptor agonists: Society for Perioperative Assessment and Quality Improvement (SPAQI) multidisciplinary consensus statement
Oprea A, Ostapenko L, Sweitzer B, Selzer A, Irizarry-Alvarado J, Hurtado Andrade M, Mendez C, Kelley K, Stewart E, Fernandez Robles C, Chadha R, Camilleri M, Mathur R, Umpierrez G, Hepner D. Perioperative management of patients taking glucagon-like peptide 1 receptor agonists: Society for Perioperative Assessment and Quality Improvement (SPAQI) multidisciplinary consensus statement. British Journal Of Anaesthesia 2025, 135: 48-78. PMID: 40379536, DOI: 10.1016/j.bja.2025.04.001.Peer-Reviewed Original ResearchConceptsGlucagon-like peptide 1 receptor agonistsPeptide 1 receptor agonistsPerioperative management of patientsMultidisciplinary consensus statementManagement of patientsSociety for Perioperative AssessmentPerioperative managementPerioperative assessmentConsensus statementPreoperative fasting timeMedical managementAgonistsModified Delphi processPatientsSystematic reviewImmune inhibitory receptor agonist therapeutics
Lovewell R, Langermann S, Flies D. Immune inhibitory receptor agonist therapeutics. Frontiers In Immunology 2025, 16: 1566869. PMID: 40207220, DOI: 10.3389/fimmu.2025.1566869.Peer-Reviewed Original ResearchConceptsAgonist suppressionSurface of immune cellsCheckpoint inhibitorsStimulatory cellsStimulatory receptorsSuppressive cellsDysregulated inflammationImmune cellsPre-clinicalTreat diseasesDisease settingsAgonistsImmune systemImmune pathwaysClinical therapeuticsTherapeutic interventionsDiseaseReceptorsCellular levelTherapeuticsCellsPathwayInduced signalsAutoimmunityInflammation
2024
The potential of non-psychedelic 5-HT2A agents in the treatment of substance use disorders: a narrative review of the clinical literature
Pulido-Saavedra A, Borelli A, Kitaneh R, Alrafayia M, Jalilian-Khave L, Funaro M, Potenza M, Angarita G. The potential of non-psychedelic 5-HT2A agents in the treatment of substance use disorders: a narrative review of the clinical literature. Expert Opinion On Pharmacotherapy 2024, 26: 133-146. PMID: 39708346, PMCID: PMC11786980, DOI: 10.1080/14656566.2024.2446623.Peer-Reviewed Original ResearchConceptsTreatment of substance use disordersSubstance use disordersTreating substance use disordersPsychedelic agentsNarrative reviewReceptor agonistsClinical literatureReceptor antagonistNovel interventionsClinical evidenceFDA approvalPublic health issueDisordersReceptorsAgonistsTreatmentCravingPositive resultsPsychedelicsAbstinenceReviewed literatureAgentsHealth issuesAntagonistPrimary affinity899-P: Combinations of the Mitochondrial Protonophore TLC-6740 and/or the ACC2 Inhibitor TLC-3595 Provide Additive Glycemic Benefits to Semaglutide (SEMA) in db/db Mice
VIJAYAKUMAR A, SRODA N, MURAKAMI E, WENG S, MYERS R, SUBRAMANIAN M, SHULMAN G. 899-P: Combinations of the Mitochondrial Protonophore TLC-6740 and/or the ACC2 Inhibitor TLC-3595 Provide Additive Glycemic Benefits to Semaglutide (SEMA) in db/db Mice. Diabetes 2024, 73 DOI: 10.2337/db24-899-p.Peer-Reviewed Original ResearchOral glucose tolerance testGLP-1R agonistsDb/db miceIncremental AUCGlucose tolerance testMale db/db miceImproved glucose toleranceSemaglutide groupGlycemic parametersSemaglutideTolerance testFood intakeGlucose toleranceGLP-1RLiver-targeted mitochondrial uncouplerDb/dbMiceGlucose bolusVEHAgonistsEvaluation of combinationsHbA1cDiabetesMitochondrial uncouplingAssess effectsDopamine D1 Receptor Agonists Rescue Age-related Decline in Temporal Order Memory
Bransom L, Bassett A, Zhou M, Cimino J, Mailman R, Yang Y. Dopamine D1 Receptor Agonists Rescue Age-related Decline in Temporal Order Memory. Neuroscience 2024, 551: 177-184. PMID: 38823551, PMCID: PMC11246218, DOI: 10.1016/j.neuroscience.2024.05.033.Peer-Reviewed Original ResearchTemporal order memoryOrder memoryAge-related declineDopamine D1 receptor agonistTreating age-related cognitive declineAge-related cognitive declineReceptor agonistsSpatial working memoryD1 receptor agonistPoorer memory performanceWorking memoryMemory performanceCognitive declineEffects of ageRecognition taskEffect sizeIndividual ratsMemoryOld ratsOptimal effective doseDopamineImproved therapeutic indexAgonistsTherapeutic indexFunctional selectivitySerotonergic Psychedelics: A Comparative Review of Efficacy, Safety, Pharmacokinetics, and Binding Profile
Holze F, Singh N, Liechti M, D'Souza D. Serotonergic Psychedelics: A Comparative Review of Efficacy, Safety, Pharmacokinetics, and Binding Profile. Biological Psychiatry Cognitive Neuroscience And Neuroimaging 2024, 9: 472-489. PMID: 38301886, DOI: 10.1016/j.bpsc.2024.01.007.Peer-Reviewed Original ResearchConceptsSerotonergic psychedelicsSerotonin 2A receptor agonistPsychedelic effectsPsychedelic compoundsReceptor agonistsReview of efficacyPsychedelicsReceptor profilePsilocybinTherapeutic indicationsTherapeutic potentialPotential treatmentBinding profilesTherapeutic useClinical researchSerotonergicSerotoninPharmacokineticsMescalineDepressionEfficacyEffective durationAgonistsLSDResearchA corneal neuralgia TRPV1 mutation increases response to acidic pH and alters agonist sensitization and desensitization
Gualdani R, Gailly P, Barbeau S, Jacobs D, Dib-Hajj S, Waxman S. A corneal neuralgia TRPV1 mutation increases response to acidic pH and alters agonist sensitization and desensitization. Biophysical Journal 2024, 123: 391a. DOI: 10.1016/j.bpj.2023.11.2378.Peer-Reviewed Original Research
2023
Highly multiplexed bioactivity screening reveals human and microbiota metabolome-GPCRome interactions
Chen H, Rosen C, González-Hernández J, Song D, Potempa J, Ring A, Palm N. Highly multiplexed bioactivity screening reveals human and microbiota metabolome-GPCRome interactions. Cell 2023, 186: 3095-3110.e19. PMID: 37321219, PMCID: PMC10330796, DOI: 10.1016/j.cell.2023.05.024.Peer-Reviewed Original ResearchGlucagon-like peptide 1 (GLP-1) receptor agonists as a protective factor for incident depression in patients with diabetes mellitus: A systematic review
Cooper D, Ramachandra R, Ceban F, Di Vincenzo J, Rhee T, Mansur R, Teopiz K, Gill H, Ho R, Cao B, Lui L, Jawad M, Arsenault J, Le G, Ramachandra D, Guo Z, McIntyre R. Glucagon-like peptide 1 (GLP-1) receptor agonists as a protective factor for incident depression in patients with diabetes mellitus: A systematic review. Journal Of Psychiatric Research 2023, 164: 80-89. PMID: 37331261, DOI: 10.1016/j.jpsychires.2023.05.041.Peer-Reviewed Original ResearchConceptsGLP-1 receptor agonistsGlucagon-like peptide-1 receptor agonistsPeptide-1 receptor agonistsIncident depressionDiabetes mellitusReceptor agonistType 2 diabetes mellitusRetrospective observational studyPubMed/MEDLINEEnglish-language articlesHigh interstudy heterogeneityGoogle Scholar databasesPaucity of literatureGlycemic controlNeuroprotective effectsAntidepressant propertiesNeuroprotective potentialInterstudy heterogeneityObservational studyPatientsSystematic reviewAgonistsMellitusScholar databasesProtective factorsNew Frontiers in Obesity Treatment: GLP-1 and Nascent Nutrient-Stimulated Hormone-Based Therapeutics
Jastreboff A, Kushner R. New Frontiers in Obesity Treatment: GLP-1 and Nascent Nutrient-Stimulated Hormone-Based Therapeutics. Annual Review Of Medicine 2023, 74: 125-139. PMID: 36706749, DOI: 10.1146/annurev-med-043021-014919.Peer-Reviewed Original ResearchConceptsGLP-1 RAsGlucagon-like peptide-1 receptor agonistsPeptide-1 receptor agonistsAnti-obesity therapeuticsTreatment of obesityMechanism-based treatmentsNeurobiology of obesityObesity treatmentReceptor agonistGLP-1Obesity therapeuticsEffective treatmentObesityHalf of AmericansFirst agentTreatmentTherapeuticsAgonistsAgents
2022
Insights into distinct signaling profiles of the µOR activated by diverse agonists
Qu Q, Huang W, Aydin D, Paggi J, Seven A, Wang H, Chakraborty S, Che T, DiBerto J, Robertson M, Inoue A, Suomivuori C, Roth B, Majumdar S, Dror R, Kobilka B, Skiniotis G. Insights into distinct signaling profiles of the µOR activated by diverse agonists. Nature Chemical Biology 2022, 19: 423-430. PMID: 36411392, PMCID: PMC11098091, DOI: 10.1038/s41589-022-01208-y.Peer-Reviewed Original ResearchConceptsRespiratory depressionCryo-EM structureMitragynine pseudoindoxylM-opioid receptorSignaling outcomesB-arrestinMolecular dynamics simulationsFatal respiratory depressionCryo-EMG-proteinBinding sitesMOR agonistsEffective analgesicSafety profileEfficacy profileSubtype activationAnimal studiesDynamics simulationsOrthosteric pocketLofentanilIntracellular sidePlant-derivedAgonistsDiverse agonistsActive-state conformationCellular Stress-Induced Metabolites in Escherichia coli
Gatsios A, Kim C, York A, Flavell R, Crawford J. Cellular Stress-Induced Metabolites in Escherichia coli. Journal Of Natural Products 2022, 85: 2626-2640. PMID: 36346625, PMCID: PMC9949963, DOI: 10.1021/acs.jnatprod.2c00706.Peer-Reviewed Original ResearchPharmacological characterization of 5-iodo-A-85380, a β2-selective nicotinic receptor agonist, in mice
Akinola LS, Bagdas D, Alkhlaif Y, Jackson A, Gurdap CO, Rahimpour E, Carroll FI, Papke RL, Damaj MI. Pharmacological characterization of 5-iodo-A-85380, a β2-selective nicotinic receptor agonist, in mice. Journal Of Psychopharmacology 2022, 36: 1280-1293. PMID: 36321267, PMCID: PMC9817006, DOI: 10.1177/02698811221132214.Peer-Reviewed Original ResearchConceptsNicotinic receptor agonistsReceptor agonistNicotinic acetylcholine receptorsLow sensitivityPharmacological characterizationΑ4β2 receptorsNicotine dependenceNicotinic subunitsPlace preferenceΑ4β2 nAChRsAcetylcholine receptorsPartial agonistFull agonistAgonistsDifferential efficacyBehavioral effectsNeurodegenerative diseasesSubtypesPathological conditionsNAChRsPotential targetPotential roleHypothermiaReceptorsΑ6The neural basis of psychedelic action
Kwan A, Olson D, Preller K, Roth B. The neural basis of psychedelic action. Nature Neuroscience 2022, 25: 1407-1419. PMID: 36280799, PMCID: PMC9641582, DOI: 10.1038/s41593-022-01177-4.Peer-Reviewed Original ResearchConceptsSerotonin 2A receptor agonistThalamocortical functional connectivityDownstream molecular signaling pathwaysDrug discoveryMolecular signaling pathwaysReceptor agonistSerotonin receptorsAssociation cortexPsychedelic actionSustained effectSubcortical regionsBasic neurobiologyFunctional connectivityTranscriptional changesPsychoactive moleculesSignaling pathwaysNeural mechanismsStructural plasticityNeural basisPsychedelic drugsChemistryPsychedelicsEnduring effectMoleculesAgonistsTop Ten Tips Palliative Care Clinicians Should Know About Buprenorphine
Neale KJ, Weimer MB, Davis MP, Jones KF, Kullgren JG, Kale SS, Childers J, Broglio K, Merlin JS, Peck S, Francis SY, Bango J, Jones CA, Sager Z, Ho JJ. Top Ten Tips Palliative Care Clinicians Should Know About Buprenorphine. Journal Of Palliative Medicine 2022, 26: 120-130. PMID: 36067137, DOI: 10.1089/jpm.2022.0399.Commentaries, Editorials and LettersConceptsPalliative carePain managementPartial mu-opioid receptor agonistSerious illnessMu-opioid receptor agonistTop Ten TipsOpioid use disorderLife-limiting illnessPC cliniciansCare cliniciansOpioid misuseBuprenorphine useReceptor agonistNurse practitionersUse disordersPopulation-wide trendsIllnessBuprenorphineCliniciansPatientsAgonistsPharmacistsPhysiciansCareSocial workersLeukoderma Induced by Rotigotine Patch, a Transdermal Dopamine Agonist
Talty R, Micevic G, Wang A, Ko CJ, Damsky W. Leukoderma Induced by Rotigotine Patch, a Transdermal Dopamine Agonist. Case Reports In Dermatology 2022, 14: 214-218. PMID: 36158852, PMCID: PMC9459519, DOI: 10.1159/000525894.Peer-Reviewed Original ResearchRestless legs syndromeRotigotine patchTransdermal patchRotigotine transdermal patchTransdermal dopamine agonistsPotential side effectsAbsence of melanocytesDopamine agonismSystemic medicationsTopical medicationsDopamine agonistsLegs syndromeCase reportHistopathologic examinationDermal-epidermal junctionAnterior shoulderPharmacologic substancesSide effectsPatch applicationPotential mechanismsLeukodermaMedicationsPatientsSyndromeAgonistsSynthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand: (S)-(+)- and (R)-(-)-[18F]FBFP
Wang T, Zhang Y, Zhang X, Chen L, Zheng M, Zhang J, Brust P, Deuther-Conrad W, Huang Y, Jia H. Synthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand: (S)-(+)- and (R)-(-)-[18F]FBFP. Chinese Chemical Letters 2022, 33: 3543-3548. DOI: 10.1016/j.cclet.2022.03.099.Peer-Reviewed Original ResearchIodonium ylide precursorsMicro-positron emission tomographyHigh brain uptakeBrain uptakeICR miceBrain kineticsBlood ratioReceptor radiotracerReceptor radioligandEmission tomographyFurther evaluationFast clearanceComparable high affinityReceptorsBrainUnlabeled compoundsVivo stabilitySuperior imaging propertiesMolar activityHigh affinityAgonistsAntagonistRatsMiceRadioligandSTING agonist delivery by tumour-penetrating PEG-lipid nanodiscs primes robust anticancer immunity
Dane E, Belessiotis-Richards A, Backlund C, Wang J, Hidaka K, Milling L, Bhagchandani S, Melo M, Wu S, Li N, Donahue N, Ni K, Ma L, Okaniwa M, Stevens M, Alexander-Katz A, Irvine D. STING agonist delivery by tumour-penetrating PEG-lipid nanodiscs primes robust anticancer immunity. Nature Materials 2022, 21: 710-720. PMID: 35606429, PMCID: PMC9156412, DOI: 10.1038/s41563-022-01251-z.Peer-Reviewed Original ResearchConceptsSTING agonistsRobust T cell activationInnate immune stimulatorsT cell activationTumor rechallengeAnticancer immunityDendritic cellsAgonist deliverySingle doseCyclic dinucleotidesTumor antigensImmune stimulatorImmune memorySolid tumorsEnhanced immunotherapySystemic deliveryTumorsTumor cellsCancer cellsAgonistsImmunityDeliveryCellsActivationCleavable linkerCommunity based buprenorphine micro-induction in the context of methadone maintenance treatment and fentanyl – Case report
Kaliamurthy S, Jegede O, Hermes G. Community based buprenorphine micro-induction in the context of methadone maintenance treatment and fentanyl – Case report. Journal Of Addictive Diseases 2022, 41: 175-180. PMID: 35377273, DOI: 10.1080/10550887.2022.2051985.Peer-Reviewed Case Reports and Technical NotesConceptsFull opioid agonistsOpioid use disorderFentanyl useOpioid agonistsUse disordersMethadone doseCommunity-based methadone maintenance programIllicit fentanyl useCharacteristics of patientsMethadone maintenance treatmentMethadone maintenance programMaintenance treatmentOutpatient clinicTime of inductionOutpatient settingCommunity clinicsBuprenorphinePatientsMore cliniciansAgonistsDisordersClinicCliniciansDoseWithdrawalIncreased length-dependent activation of human engineered heart tissue after chronic treatment with alpha-1A-adrenergic agonist
Rupert C, Cortez-Toledo E, Lopez J, Chesler N, Simpson P, Campbell S, Baker A. Increased length-dependent activation of human engineered heart tissue after chronic treatment with alpha-1A-adrenergic agonist. Biophysical Journal 2022, 121: 397a-398a. DOI: 10.1016/j.bpj.2021.11.785.Peer-Reviewed Original Research
This site is protected by hCaptcha and its Privacy Policy and Terms of Service apply