134 Objectives The failing human heart is related with a selective reduction in β1-adrenoceptor. We designed radiolabeled esmolol, is known to be a cardioselective β1 receptor blocker in the sympathetic nervous system. A new 99mTc-labeld esmolol derivative (99mTc-EDA-ESM) was prepared and its binding and biokinetic characteristics in normal rat for the noninvasive measurement of cardiac β1-adrenoceptor density. Methods 99mTc-EDA-ESM was prepared by reacting 99mTcO4- with the precursor in the presence of SnF2, ascorbic acid, and mannitol at room temperature for 30 sec. To optimize the labeling condition, a variety of attempts were investigated with different reducing agents and anti-oxidants. For assessment of heart and major organ uptake of radiotracer, serial SPECT/CT images of 99mTc-EDA-ESM (74 MBq) in normal rat were obtained in 12 projections over a 10-min period and blocking experiment was performed with esmolol or atenolol. Results 99mTc-EDA-ESM was synthesized in 95% radiochemical yield with over 98% of radiochemical purity. Mass and NMR data of Re-EDA-ESM were used for the speculation of 99mTc-EDA-ESM structure. In serial SPECT images, radiotracer showed high accumulation in the heart and kidneys, while radio-uptake was relatively low in the liver and lung. ROIs were drawn in the lung, the liver and the heart, and their radioactivity were shown as 0.38±0.04, 1.10±0.20, and 1.88±0.20%ID/g at 5 min post-injection and 0.21±0.03, 0.85±0.22, and 1.02±0.15%ID/g at 25 min post-injection, respectively. In vivo blocking with excess esmolol or atenolol resulted in significantly reduced radioactivity uptake in the heart by 92% and 76%, respectively. Conclusions Our results demonstrate that 99mTc-EDA-ESM exhibits specific β1-adrenergic receptor binding and favorable in vivo biokinetic characteristics, making it a promising SPECT radiotracer for the imaging of β1-adrenoceptors.
Purpose: To report the efficacy of toric orthokeratology lenses in patients with astigmatism within 1.5 D having difficulty in wearing spherical orthokeratology lenses due to the limbus-to-limbus corneal astigmatism. Methods: Twenty-three eyes of 16 patients with limbus-to-limbus corneal astigmatism who had been wearing toric orthokeratology lenses for more than 6 months were recruited. The uncorrected visual acuity (UCVA), refractive error, and keratometric changes including eccentricity before and after wearing lenses were compared, and the correlations between corneal astigmatism as well as refractive astigmatism and lens toricity were assessed. Results: After wearing the lens, UCVA (log MAR) significantly improved from 0.61 ± 0.22 to 0.05 ± 0.08 (p < 0.001). Myopia and spherical equivalent were also reduced significantly (p < 0.001 and p < 0.001, respectively). While Simulated K (Sim K) tended to be more flattened (p < 0.001) and the eccentricity showed significant decrease (p < 0.001), corneal and refractive astigmatism were not changed significantly (p = 0.330 and p = 0.124, respectively). Correlations between corneal and refractive astigmatism and lens toricity were not statistically significant (r = 0.244, p = 0.300; r = -0.051, p = 0.832). No patients showed lens decentration or visual discomfort. Conclusions: Corneal topography was essential in patients who had difficulty in wearing spherical orthokeratology lenses due to the limbus-to-limbus corneal astigmatism. Toric orthokeratology lenses may be an effective treatment option in patients with limbus-to-limbus corneal astigmatism. J Korean Ophthalmol Soc 2015;56(7):980-984
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