18 research outputs found
The first total synthesis of (±)-herbertenones A and B
The first total synthesis of (±)-herbertenones A and B, employing Claisen rearrangement-metathesis reaction based approaches, is described
The First Total Synthesis of ()-Herbertenones A and B
The first total synthesis of ()-herbertenones A and B, employing Claisen rearrangement-metathesis reaction based approaches, is describe
A Domino Approach of Heck Coupling for the Synthesis of β-Trifluoromethylstyrenes
A domino approach of Heck coupling was used to synthesize β-trifluoromethylstyrene derivatives from iodoarenes and 1-iodo-3,3,3-trifluoropropane in moderate to good yields. This method avoids the use of low-boiling, gaseous reagents such as 3,3,3-trifluoropropene, and additives and phosphines in the catalytic system
Preclinical PET Neuroimaging of [ 11
Activation of retinoid X receptors (RXRs) has been proposed as a therapeutic mechanism for the treatment of neurodegeneration, including Alzheimer's and Parkinson's diseases. We previously reported radiolabeling of a Food and Drug Administration-approved RXR agonist, bexarotene, by copper-mediated [ 11 C]CO 2 fixation and preliminary positron emission tomography (PET) neuroimaging that demonstrated brain permeability in nonhuman primate with regional binding distribution consistent with RXRs. In this study, the brain uptake and saturability of [ 11 C]bexarotene were studied in rats and nonhuman primates by PET imaging under baseline and greater target occupancy conditions. [ 11 C]Bexarotene displays a high proportion of nonsaturable uptake in the brain and is unsuitable for RXR occupancy measurements in the central nervous system
Preclinical PET Neuroimaging of [C]Bexarotene
Activation of retinoid X receptors (RXRs) has been proposed as a therapeutic mechanism for the treatment of neurodegeneration, including Alzheimer's and Parkinson's diseases. We previously reported radiolabeling of a Food and Drug Administration-approved RXR agonist, bexarotene, by copper-mediated [ 11 C]CO 2 fixation and preliminary positron emission tomography (PET) neuroimaging that demonstrated brain permeability in nonhuman primate with regional binding distribution consistent with RXRs. In this study, the brain uptake and saturability of [ 11 C]bexarotene were studied in rats and nonhuman primates by PET imaging under baseline and greater target occupancy conditions. [ 11 C]Bexarotene displays a high proportion of nonsaturable uptake in the brain and is unsuitable for RXR occupancy measurements in the central nervous system
Radiocaine: An Imaging Marker of Neuropathic Injury
Voltage-gated sodium channels (Navs) play
a crucial
electrical signaling role in neurons. Nav-isoforms present
in peripheral sensory neurons and dorsal root ganglia of the spinal
cord are critically involved in pain perception and transmission.
While these isoforms, particularly Nav1.7, are implicated
in neuropathic pain disorders, changes in the functional state and
expression levels of these channels have not been extensively studied
in vivo. Radiocaine, a fluorine-18 radiotracer based on the local
anesthetic lidocaine, a non-selective Nav blocker, has
previously been used for cardiac Nav1.5 imaging using positron-emission
tomography (PET). In the present study, we used Radiocaine to visualize
changes in neuronal Nav expression after neuropathic injury.
In rats that underwent unilateral spinal nerve ligation, PET/MR imaging
demonstrated significantly higher uptake of Radiocaine into the injured
sciatic nerve, as compared to the uninjured sciatic nerve, for up
to 32 days post-surgery. Radiocaine, due to its high translational
potential, may serve as a novel diagnostic tool for neuropathic pain
conditions using PET imaging