Aditya Bade1, Howard Gendelman1, and Yutong Liu2
1Pharmacology and Exp Neuroscience, University of Nebraska Medical Center, Omaha, NE, United States, 2Radiology, University of Nebraska Medical Center, Omaha, NE, United States
1Pharmacology and Exp Neuroscience, University of Nebraska Medical Center, Omaha, NE, United States, 2Radiology, University of Nebraska Medical Center, Omaha, NE, United States
1) The CEST effects of antiretroviral drugs 3TC (lamivudine) and FTC (emtricitabine) were detected at 1 and 2 ppm. 2) In mice administered with 3TC, MRI data was analyzed using Lorentzian functions, and CEST signal of amino protons of 3TC was detected at ~ 2 ppm on thalamus region.
Figure 1. CEST
signals of 3TC. (A) Chemical structure of 3TC. The hydroxyl group is in red
circle, and the amino group in blue circle. (B) MTR plots of 3TC in PBS at 37oC. MTR increases at 2 ppm with the 3TC
concentration. (C) MTR@2ppm increases linearly with 3TC concentration (R2 = 0.95). (D) Pixel-by-pixel color maps
of 3TC samples.
Figure 3. (A) Lorentzian functions of CEST signals
of amino protons on thalamus from a mouse scanned before 3TC administration
(baseline), 6 hours after 1st drug administration and after 5 days of daily
administration. (B) CEST signal integrals of 3TC on thalamus. (C) Color maps of
CEST signal integrals of 3TC superimposed on anatomical images of the mouse
brain.