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U. 195 INSERM, Faculty of Medicine and Centre Jean Perrin, University of Clermont-Ferrand, France
Correspondence: For reprints contact: Nicole Moins, U. 195 INSERM, Dept. of Pharmacology, Faculty of Medicine, B.P. 38, 63001 Clermont-Ferrand Cédex, France.
ABSTRACT
Thallium-201 myocardial imaging was performed in dogs after pretreatment with grisorixin, which appeared to increase the myocardial uptake of Tl-201. This effect of grisorixin was found to be dose dependent, with an optimal dose of 60 µg/kg. The myocardial-to-background ratio, which was 1.92 in the control dogs, rose to 4.45. The increase in the absolute myocardial uptake was demonstrated in guinea pigs that received Tl-201 after similar pretreatment with grisorixin, in the animals treated with 500 µg/kg, the uptake of Tl-201 by the heart was 35% over the control value. With 60 µg/kg grisorixin, the coronary blood flow increased from 40 to 176 ml/min 5 min after the injection. This dose, optimal for imaging, induced the maximum vasodilator effect with only a very slight concomitant increase in the left-ventricular pressure and myocardial contractility. Above 60 µg/kg, grisorixin appeared to be a potent inotropic agent, whereas below this dose it showed only coronary vasodilator properties. Some evidence for an ionophore effect of this compound was found in dogs pretreated with 60 µg/kg. In these the radionuclide was injected when the coronary vasodilatation had become insignificant, but a significant improvement of the M/B ratio was still evident.
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