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Aug. 2014 Using radioligand binding and cell-based functional assays, we have characterized tianeptine, an atypical antidepressant, as a opiod receptor (MOR) agonist. We propose that activation of MOR could be the initial molecular event responsible for triggering many of the known effects of this agent, including its antidepressant actions. Read about our work in Transl. Psychiatry. [html] [pdf]
June 2014 CONGRATULATIONS to Paolomi Merchant on successfully submitting and defending her dissertation and thesis! Welcome to the family of Ph.D. holders!
May 2014 Using our false fluorescent neurotransmitters (FFNs), in conjunction with in vitro amperometric and micro dialysis techniques, we showed that cocaine and methylphenidate induce marked depression of synaptic release of dopamine (DA) in mouse striatum. We show that cocaine and methylphenidate can not only increase DA neurotransmission by blocking DA reuptake, as is widely known, but can also block or decrease DA neurotransmission by reducing excocytotic DA release. This biphasic effect on DA neurotransmission could have implications in the observed differential behavioral effects of psychostimulants in treatment of ADHD. Check out our work in J. Biol. Chem. [html] [pdf]
Oct. 2013 CONGRATULATIONS to Rich Karpowicz on the successful submission and defense of his dissertation and thesis! Welcome to the family of Ph.D. holders!
July 2013 We have just published a study that represents a first step toward establishing a chemical toolkit (chemotransformations) that can selectively oxidize C-H bonds in complex pharmaceuticals and rapidly deliver drug metabolites. Rapid access to oxidized drugs could facilitate metabolite identification and enable early pharmacology and toxicity studies. Check out our work in JACS. [Abstract] [pdf]
We have just reported the synthesis and characterization of a new fluorescent probe, FFN206, an excellent VMAT2 substrate capable of detecting VMAT2 activity in intact cells with high selectivity using fluorescence microscopy! We also report the development and validation of a cell-based fluorescence assay amenable to high-throughput screening using VMAT2-transfected HEK cells. Read about this work in ACS Chemical Biology. [Abstract] [pdf]
May 2013 Congratulations to Richard Karpowicz, Matt Dunn, Dali and our collaborator David Sulzer on their two recently published ACS Chemical Neuroscience articles! In the ACS Chemical Neuroscience Viewpoint article, they discuss recent advancements towards the goal of imaging neurotransmitter secretion in the brain with high spatial resolution; visualization of neurotransmitter release in brain tissue with the spatial resolution of individual synapses; and suggest future directions, challenges, and impact of neurotransmitter imaging on neuroscience.
In the main article, they discuss the potential use of the fluorescent pyridinium dye APP+, an analogue of the dopaminergic neurotoxin MPP+, as a probe for identifying catecholaminergic innervations in the brain, but not as a candidate for the development of a novel group of FFNs. Check out this work in ACS Chemical Neuroscience! [Abstract] [pdf]
Feb. 2013 CONGRATULATIONS to Teresa Jacques on successfully submitting her dissertation and defending her thesis! Welcome to the family of Ph.D. holders!
Jan. 2013 Our recently developed fluorescent false neurotransmitters (FFNs) can be used as optical tracers to visualize neurotransmitter release at individual presynaptic terminals. We describe, here, a pH-responsive FFN probe, FFN102, that enables the optical measurement of individual synaptic terminal activity, as well as evoked release of synaptic vesicle content into the extracellular space, by monitoring fluorescence loss upon vesicle stimulation. This work is published in PNAS [Abstract] [pdf]
Jan. 2013 We have just published a paper in which we describe a general approach for the synthesis of complex 1,2,4-triazoles via regioselective C-H- bond arylation, and the development of the SEM and THP switch as well as trans-N-alkylation for sequential triazole ring arylation! Check out our work in J. Org. Chem. [Abstract] [pdf]
Jan. 2013 We would like to welcome our newest member Umed T Boltaev to the group!
Aug. 2012 One of our recently published articles (J. Org. Chem. ASAP) has been selected by the Editorial Board of SYNFACTS for its important contributions to the field of chemistry! SYNFACTS is a monthly publication aimed at highlighting the most significant recent developments and future trends in synthetic chemistry. Congratulations to Paul, Ignacio, and Dali! You can view the electronic reprint in the SYNFACTS September 2012 issue. [html].
July 2012 C-H bond functionalization is an active area of research and is very important for the synthesis of organic molecules. Many such reactions, however, suffer from poor compatibility with Lewis basic functional groups, especially amines. We have just reported the development of two mild protocols using PtCl4 or Au(PPh3Cl/AgSbF6 for use with an enhanced substrate scope, as synthetic tools for the structure-activity examination of FFN neuroimaging probes, as well as for the general synthesis of complex coumarins. This work has been published in J. Org. Chem. [Abstract] [pdf]
June 2012 We have just reported a study of the highly stereoselective intramolecular amination of sp3 C-H bonds via hydride transfer cyclization of N-tosylamines (HT-amination). This work has been published in the Journal of Organic Chemistry as the featured article! Check out our work in J. Org. Chem. ASAP [Abstract] [Full Text]
Jan. 2012 The Sames group would like to welcome Madalee Gassaway to the group!
Sep. 2011 We report here a new protocol for highly selective C-H arylation of pyridines containing readily available and synthetically versatile electron-withdrawing substituents. This work expands the scope of catalytic azine functionalization as well as complements existing methods for C-H arylation and Ir-catalyzed borylation of pyridines, and has been published in J. Am. Chem. Soc. [Abstract]
June 2011 The Sames group welcomes new members:

  • Matthew R. Dunn - Graduate Student
  • Ekeoma C. Nwadibia - Graduate Student
  • Andrew C. Kruegel - Graduate Student
  • Dr. Souvik Rakshit - Post Doc
  • Dr. Yves Meyer - Post Doc
  • Dr. Adam Henke - Post Doc
  • Feb. 2011 Intramolecular energy transfer from carbostyril 124-sensitized Tb3+ to Eu3+ in aqueous aggregates is reported here to show the first example of imaging this phenomenon on the cellular membrane of HEK-293T cells. Our work serves as an example for the applicability of this energy transfer probe for imaging biological systems. Check out our work in Org. Lett. [Abstract]
    Sep. 2010 We describe a novel optical approach for measuring the changes of metabolic fluxes in cells, based on a two-substrate competition between a physiological substrate and a fluorogenic reporter substrate. This work has been published in ACS Chem. Biol. [Abstract]
    July 2010 We developed a general and comprehensive approach for the synthesis of complex aryl imidazoles, where all three C-H bonds of the imidazole core can be arylated in a regioselective and sequential manner. This work has been published as a featured article in J. Org. Chem. [Abstract]
    June 2010 We introduce pH-responsive fluorescent false neurotransmitters (pH-responsive FFNs) as novel probes that act as vesicular monoamine transporter (VMAT) substrates and ratiometric fluorescent pH sensors. This work has been published in J. Am. Chem. Soc. [Abstract]
    Nov. 2009 Our work on fluorescent false neurotransmitters that enabled us to observe neurotransmitter uptake and release from individual presynaptic terminals directly has been published in Journal of Visualized Experiments, a video journal for biological research. Click here to play the video. [html]
    Oct. 2009 The scope of the through-space hydride transfer reactions has been expanded to include terminal alkynes as the hydride acceptors. This work has been published in J. Am. Chem. Soc. [Abstract]
    June 2009 The hydride transfer initiated cyclization of aryl alkyl ethers leads to the formation of dihydrobenzopyrans. Check out our latest work on C-H bond functionalization in Org. Lett. [Abstract] [html] This article has been selected by the Editorial Board of Synfacts. [PDF]
    May 2009 Our study of the nervous system using fluorescent false neurotransmitters has been published in Science. [Abstract] This work has been featured in Chemical & Engineering News. [html] This work has been also reviewed by Nature Methods [html] [pdf] and Physiology [pdf].
    Feb. 2009 The group's latest work on regioselective direct C-arylation of pyrazoles has been published in J. Am. Chem. Soc. [Abstract]
    Jan. 2009 The group's latest work on C-H bond functionalization via hydride transfer has been published in J. Am. Chem. Soc. [Abstract] This article was summarized in Synfacts. [PDF]
    Oct. 2008 The group's latest work on imaging induction of cytoprotective enzymes in intact human cells has appeared in J. Am. Chem. Soc. [Abstact] This article was featured as a "Spotlight" in Chemical Research in Toxicology. [Abstract]
    Aug. 2008 Congratulations to Dali and Professor David Sulzer of the Department of Neuroscience on receiving a 2008-2009 McKnight Foundation Technical Innovations in Neuroscience Award for their project "Development of Fluorescent False Neurotransmitters: Novel Probes for Direct Visualization of Neurotransmitter Release from Individual Presynaptic Terminals."
    Last Updated: July 2013