2024
First-in-Human Study of 18F-SynVesT-2: An SV2A PET Imaging Probe with Fast Brain Kinetics and High Specific Binding
Drake L, Wu Y, Naganawa M, Asch R, Zheng C, Najafzadeh S, Pracitto R, Lindemann M, Li S, Ropchan J, Labaree D, Emery P, Dias M, Henry S, Nabulsi N, Matuskey D, Hillmer A, Gallezot J, Carson R, Cai Z, Huang Y. First-in-Human Study of 18F-SynVesT-2: An SV2A PET Imaging Probe with Fast Brain Kinetics and High Specific Binding. Journal Of Nuclear Medicine 2024, 65: jnumed.123.266470. PMID: 38360052, PMCID: PMC10924160, DOI: 10.2967/jnumed.123.266470.Peer-Reviewed Original ResearchFirst-in-human studyPlasma free fractionTime-activity curvesCentrum semiovaleNonhuman primate's resultsFirst-in-humanFree fractionNondisplaceable binding potentialRegional time-activity curvesLow nonspecific uptakeRegional distribution volumesHigh-resolution research tomograph scannerTest-retest reproducibilityCerebral blood flowSynaptic vesicle glycoprotein 2AHealthy volunteersArterial input functionNonspecific uptakePET imaging probeDistribution volumeSynapse densityIndividual MR imagesHighest specific bindingMR imagingPET imaging
2022
P-304 The synthesis and bioevaluation of a novel and brain penetrable PARP1 tracer [18F]Pamiparib in rodents and nonhuman primates
Tong J, Chen B, Gu J, Alluri S, Zheng M, Zheng C, Felchner Z, Gao H, Zhang L, Kapinos M, Labaree D, Ropchan J, Nabulsi N, Carson R, Huang Y, Cai Z. P-304 The synthesis and bioevaluation of a novel and brain penetrable PARP1 tracer [18F]Pamiparib in rodents and nonhuman primates. Nuclear Medicine And Biology 2022, 108: s214-s215. DOI: 10.1016/s0969-8051(22)00440-1.Peer-Reviewed Original ResearchP-303 Synthesis and preclinical evaluation of PD-L1 PET tracer [18F]FDHPA in mice
Tong J, Chen B, Alluri S, Gu J, Zheng M, Zheng C, Felchner Z, Gao H, Zhang L, Kapinos M, Labaree D, Ropchan J, Nabulsi N, Marquez-Nostra B, Carson R, Huang Y, Cai Z. P-303 Synthesis and preclinical evaluation of PD-L1 PET tracer [18F]FDHPA in mice. Nuclear Medicine And Biology 2022, 108: s214. DOI: 10.1016/s0969-8051(22)00439-5.Peer-Reviewed Original Research
2014
Synthesis of 11β-ether-17α-ethinyl-3,17β-estradiols with strong ER antagonist activities
Zhang J, Labaree D, Hochberg R. Synthesis of 11β-ether-17α-ethinyl-3,17β-estradiols with strong ER antagonist activities. Chinese Chemical Letters 2014, 25: 567-570. DOI: 10.1016/j.cclet.2014.01.015.Peer-Reviewed Original Research
2013
ChemInform Abstract: Synthesis and Evaluation of 4‐(Substituted styryl/alkenyl)‐3,5‐bis(4‐hydroxyphenyl)‐isoxazoles as Ligands for the Estrogen Receptor.
Haddad T, Gershman R, Dilis R, Labaree D, Hochberg R, Hanson R. ChemInform Abstract: Synthesis and Evaluation of 4‐(Substituted styryl/alkenyl)‐3,5‐bis(4‐hydroxyphenyl)‐isoxazoles as Ligands for the Estrogen Receptor. ChemInform 2013, 44: no-no. DOI: 10.1002/chin.201301119.Peer-Reviewed Original Research
2012
ChemInform Abstract: Synthesis and Evaluation of 17α‐E‐20‐(Heteroaryl)norpregn‐1,3,5 (10),20‐tetraene‐3,17β‐diols [17α‐(Heteroaryl)vinyl Estradiols] as Ligands for the Estrogen Receptor‐α Ligand Binding Domain (ERα‐LBD).
Olmsted S, Tongcharoensirikul P, McCaskill E, Gandiaga K, Labaree D, Hochberg R, Hanson R. ChemInform Abstract: Synthesis and Evaluation of 17α‐E‐20‐(Heteroaryl)norpregn‐1,3,5 (10),20‐tetraene‐3,17β‐diols [17α‐(Heteroaryl)vinyl Estradiols] as Ligands for the Estrogen Receptor‐α Ligand Binding Domain (ERα‐LBD). ChemInform 2012, 43: no-no. DOI: 10.1002/chin.201242199.Peer-Reviewed Original ResearchSynthesis and evaluation of 4-(substituted styryl/alkenyl)-3,5-bis(4-hydroxyphenyl)-isoxazoles as ligands for the estrogen receptor
Haddad T, Gershman R, Dilis R, Labaree D, Hochberg RB, Hanson RN. Synthesis and evaluation of 4-(substituted styryl/alkenyl)-3,5-bis(4-hydroxyphenyl)-isoxazoles as ligands for the estrogen receptor. Bioorganic & Medicinal Chemistry Letters 2012, 22: 5999-6003. PMID: 22906893, PMCID: PMC3444814, DOI: 10.1016/j.bmcl.2012.06.097.Peer-Reviewed Original ResearchSynthesis and evaluation of 11β-(4-Substituted phenyl) estradiol analogs: Transition from estrogen receptor agonists to antagonists
Hanson RN, Hua E, Hendricks JA, Labaree D, Hochberg RB. Synthesis and evaluation of 11β-(4-Substituted phenyl) estradiol analogs: Transition from estrogen receptor agonists to antagonists. Bioorganic & Medicinal Chemistry 2012, 20: 3768-3780. PMID: 22608920, PMCID: PMC3581310, DOI: 10.1016/j.bmc.2012.04.041.Peer-Reviewed Original ResearchConceptsSynthetic strategyNew compoundsERα-LBDPotential drug delivery systemPrevious synthetic studiesSeries of compoundsDrug delivery systemsClass of compoundsSynthetic methodTerminal groupsFacile accessSynthetic studiesDrug conjugationSpecific structural featuresCompetitive ligandCompoundsSteroidal agonistsDelivery systemRepresentative scaffoldsStructural featuresERβ-LBDSubtype selectivityActive groupAnaloguesScaffoldsTargeting the estrogen receptor with metal-carbonyl derivatives of estradiol
Hanson RN, Kirss R, McCaskill E, Hua E, Tongcharoensirikul P, Olmsted SL, Labaree D, Hochberg RB. Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol. Bioorganic & Medicinal Chemistry Letters 2012, 22: 1670-1673. PMID: 22277281, PMCID: PMC3274643, DOI: 10.1016/j.bmcl.2011.12.111.Peer-Reviewed Original Research
2010
[11C]GR103545: novel one-pot radiosynthesis with high specific activity
Nabulsi NB, Zheng MQ, Ropchan J, Labaree D, Ding YS, Blumberg L, Huang Y. [11C]GR103545: novel one-pot radiosynthesis with high specific activity. Nuclear Medicine And Biology 2010, 38: 215-221. PMID: 21315277, DOI: 10.1016/j.nucmedbio.2010.08.014.Peer-Reviewed Original ResearchImaging drug-induced dopamine release in rhesus monkeys with [11C]PHNO versus [11C]raclopride PET
Cosgrove K, Gallezot J, Weinzimmer D, Fowles K, Labaree D, Zheng M, Lim K, Carson R, Morris E. Imaging drug-induced dopamine release in rhesus monkeys with [11C]PHNO versus [11C]raclopride PET. NeuroImage 2010, 52: s79. DOI: 10.1016/j.neuroimage.2010.04.063.Peer-Reviewed Original ResearchPharmacokinetic characterization of compounds with increased target residence times using PET
Salinas C, Weinzimmer D, Searle G, Labaree D, Ding Y, Huang Y, Rabiner E, Carson R, Gunn R. Pharmacokinetic characterization of compounds with increased target residence times using PET. NeuroImage 2010, 52: s210-s211. DOI: 10.1016/j.neuroimage.2010.04.172.Peer-Reviewed Original ResearchImaging the kappa opioid receptor in humans with [11C]LY2795050: Tracer evaluation and test–retest reproducibility study
Huang Y, Williams W, Tomasi G, Zheng M, Lin S, Ropchan J, Labaree D, Olsen J, Tabriz M, Planeta-Wilson B, Tauscher J, Ding Y, Carson R, Neumeister A. Imaging the kappa opioid receptor in humans with [11C]LY2795050: Tracer evaluation and test–retest reproducibility study. NeuroImage 2010, 52: s199. DOI: 10.1016/j.neuroimage.2010.04.161.Peer-Reviewed Original ResearchKinetic modeling of [11C]PHNO in rhesus monkeys using the Focus 220 PET scanner
Gallezot J, Weinzimmer D, Fowles K, Labaree D, Cosgrove K, Ding Y, Morris E, Carson R. Kinetic modeling of [11C]PHNO in rhesus monkeys using the Focus 220 PET scanner. NeuroImage 2010, 52: s173. DOI: 10.1016/j.neuroimage.2010.04.141.Peer-Reviewed Original ResearchA correction algorithm for carryover of tracer in paired C-11 studies: Application to the H-3 receptor antagonist [C-11]GSK189254
Planeta-Wilson B, Labaree D, Gallezot J, Lin S, Nabulsi N, Williams W, McCarthy T, Ding Y, Huang Y, Carson R. A correction algorithm for carryover of tracer in paired C-11 studies: Application to the H-3 receptor antagonist [C-11]GSK189254. NeuroImage 2010, 52: s166. DOI: 10.1016/j.neuroimage.2010.04.135.Peer-Reviewed Original ResearchImaging the cannabinoid CB1 receptor in humans with [11C]OMAR: Test–retest reproducibility and gender differences
Normandin M, Zheng M, Ropchan J, Labaree D, Najafzadeh S, Hull R, Qian W, Henry S, Williams W, Carson R, Huang Y, Neumeister A. Imaging the cannabinoid CB1 receptor in humans with [11C]OMAR: Test–retest reproducibility and gender differences. NeuroImage 2010, 52: s82-s83. DOI: 10.1016/j.neuroimage.2010.04.066.Peer-Reviewed Original ResearchModeling analysis of the CB1 PET tracer [11C]OMAR in rhesus monkeys and humans
Normandin M, Weinzimmer D, Ropchan J, Labaree D, Lin K, Mason N, Carson R, D'Souza D, Neumeister A, Huang Y. Modeling analysis of the CB1 PET tracer [11C]OMAR in rhesus monkeys and humans. NeuroImage 2010, 52: s13. DOI: 10.1016/j.neuroimage.2010.04.198.Peer-Reviewed Original Research
2008
PET Imaging of serotonin transporter as a biomarker for axon damage and regeneration in spinal cord injury
Huang Y, Nabulsi N, Weinzimmer D, Fung E, Ropchan J, Labaree D, Wang X, Gould G, Frost J, Carson R, Strittmatter S. PET Imaging of serotonin transporter as a biomarker for axon damage and regeneration in spinal cord injury. NeuroImage 2008, 41: t154. DOI: 10.1016/j.neuroimage.2008.04.122.Peer-Reviewed Original ResearchFirst in human evaluation of [11C]AFM, a novel PET tracer for the serotonin transporter
Williams W, Neumeister A, Nabulsi N, Ropchan J, Labaree D, Planeta-Wilson B, Najafzadeh S, Carson R, Huang Y. First in human evaluation of [11C]AFM, a novel PET tracer for the serotonin transporter. NeuroImage 2008, 41: t42. DOI: 10.1016/j.neuroimage.2008.04.216.Peer-Reviewed Original ResearchPET imaging of norepinephrine transporter in cocaine abuser using (S,S)-[11C]MRB
Singhal T, Planeta-Wilson B, Gallezot J, Henry S, Nabulsi N, Labaree D, Ropchan J, Carson R, Neumeister A, Malison R, Ding Y. PET imaging of norepinephrine transporter in cocaine abuser using (S,S)-[11C]MRB. NeuroImage 2008, 41: t195. DOI: 10.1016/j.neuroimage.2008.04.162.Peer-Reviewed Original Research