• The Korean Journal of Physiology
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• v.19 no.1
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• pp.25-33
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• 1985

Renal arterial infusion of renotropic agents has been a very useful technique in the renal function studies. This type of experiments have usually been conducted in the large animals such as dogs and sheep. In these animals a catheter can be placed in the site without much disturbances of renal blood flow. Rabbits as an experimental model, however, caused a disturbances of renal blood flow by a catheterization of renal artery by its properties. Therefore we have developed a new technique that allows a simple and selective access to one side of renal arteries and the other as a control, without any disturbances of renal function. The distance between the both bifurcations of renal arteries on abdominal aorta is about 7 mm. To locate the tip of catheter on one side renal artery, ascending cannulation performed via femoral artery was done. We did an experiment with the technique to clarify the effect of calmodulin inhibitor on the renal function. One of the phenothiazine derivatives, trifluoperazine known as a powerful calmodulin inhibitor. Trifluoperazine, actual dose ranges of $2.76-5.20\;ug\;{\cdot}\;kg^{-1}\;{\cdot}\;min^{-1}$, increased urine volume and glomerular filtration rate significantly. Significant increases in urinary excretion of sodium, chloride and potassium were found. Fractional excretion of sodium and free water clearance increased significantly. These data suggest that this new technique is very useful in field of renal physiology and that striking effect of trifluoperazine on the renal function may be caused by increasing the renal hemodynamics, and by the inhibition of sodium, chloride and potassium reabsorption in the renal tubules.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.6 no.2
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• pp.75-91
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• 2020

[^99mTc]Tc-Hexamethylpropylene amine oxime (HMPAO) is currently used as a regional cerebral blood flow imaging agent for single photon emission computed tomography (SPECT). The HMPAO ligand exists in two isomeric forms: d,l and meso showing different properties in vivo. Later studies indicated that brain uptake patterns of ^99mTc-complexes formed from separated enantiomers differed. Separation of enantiomers is difficult by fractional crystallizations method. Usually, the substance is obtained in low chemical yield in a time-consuming procedure. Furthermore, the final product still contains some impurity. So we have developed new efficient route for synthesis of R,R- and S,S-HMPAO enantiomeric compounds in 6-steps. Nucleophilic substitution (S_N2) reactions of 2,2-dimethylpropane-1,3-diamine either with S- (1a) or R-methyl2-chloropropanoate (1b) were performed to produce compounds R,R- (2a) or S,S-isomer (2b) derivatives protected with benzylchloroformate (Cbz), respectively. And then Weinreb amide and methylation reaction using Grignard reagent, oxime formation with ketone group and deprotectiion of Cbz group by hydrogenolysis gave S,S- (7a) or R,R-HMPAO (7b), respectively. Entaniomeric compounds were synthesied with high yield and purity without any undesired product. The 7a or 7b kits containing 10 ㎍ SnCl₂-2H₂O were labeled with ^99mTc with high radiolabeling yield (90%).